Search Result
Results for "AHR antagonist 3" in MCE Product Catalog:
1918
Inhibitors & Agonists
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-103652
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- HY-103649
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- HY-131349
-
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CCR4 antagonist 3
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CCR
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Cancer
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CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.
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- HY-136152
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- HY-135773
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- HY-101264
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- HY-137093
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- HY-101915
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- HY-U00322
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- HY-125820
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- HY-135830
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AHR antagonist 4
|
Aryl Hydrocarbon Receptor
|
Cancer
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AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC50 of 82.2 nM. AHR antagonist 4 has anti-cancer effects.
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- HY-135831
-
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AHR antagonist 2
|
Aryl Hydrocarbon Receptor
|
Cancer
|
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AHR antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, extracted from patent WO2019101641A1, compound example 1, with IC50s of 0.885 and 2.03 nM for human and mouse AhR.
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- HY-136220
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AHR antagonist 5
|
Aryl Hydrocarbon Receptor
|
Cancer
|
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AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
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- HY-111449
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- HY-135671
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- HY-17357
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- HY-B0678
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- HY-129995A
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- HY-135829
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BAY 2416964
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Aryl Hydrocarbon Receptor
|
Cancer
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BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY 2416964 has the potential for solid tumors treatment.
|
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- HY-17357S
-
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Nepafenac D5
AHR-9434 D5; AL-6515 D5
|
COX
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Others
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Nepafenac D5 (AHR-9434 D5) is the deuterium labeled Nepafenac, which is a selective COX-2 inhibitor.
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- HY-W014502
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D-Kynurenine
|
Aryl Hydrocarbon Receptor
Endogenous Metabolite
|
Cancer
|
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D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR).
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- HY-130270
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- HY-101745
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- HY-102023
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GNF351
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Aryl Hydrocarbon Receptor
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Others
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GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes.
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- HY-15001
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- HY-117102
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ANI-7
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Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
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Cancer
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ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
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- HY-111500A
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- HY-111500
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- HY-15015A
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- HY-112264
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- HY-103650
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- HY-U00320
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- HY-U00330
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- HY-112262
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- HY-P1185
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Antagonist G
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Vasopressin Receptor
Apoptosis
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Cancer
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Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
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- HY-15015
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- HY-112562
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- HY-136437
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- HY-112265
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- HY-18075
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- HY-101536
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- HY-103651
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- HY-U00334
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- HY-U00375
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- HY-111443
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- HY-136922
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- HY-U00331
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- HY-112263
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- HY-112792
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- HY-100331
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- HY-100321
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- HY-U00359
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- HY-126217
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- HY-112629
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- HY-112430
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- HY-111494
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- HY-130845
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AR antagonist 1
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Ligand for E3 Ligase
|
Cancer
|
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AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
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- HY-114193
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- HY-114194
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- HY-130261
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- HY-100261
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- HY-136459
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NMDA receptor antagonist 2
|
iGluR
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Neurological Disease
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NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
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- HY-113973
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LPA2 antagonist 2
|
LPL Receptor
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Cancer
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LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM).
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- HY-P1185A
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- HY-124759
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- HY-100274
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- HY-12684
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CH-223191
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Aryl Hydrocarbon Receptor
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Cancer
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CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR).
CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
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- HY-136645
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- HY-138501
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- HY-114017
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- HY-U00397
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- HY-U00408
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- HY-120588
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- HY-12545
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Brevetoxin-3
PbTx-3
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Sodium Channel
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Inflammation/Immunology
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Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
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- HY-18076
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- HY-100170
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- HY-U00360
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- HY-129636
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(E)-GABAB receptor antagonist 1
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GABA Receptor
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Neurological Disease
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(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
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- HY-130992
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- HY-50159
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- HY-106659
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- HY-116649
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- HY-U00368
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- HY-129357
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- HY-102037
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- HY-18619
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YL-109
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Aryl Hydrocarbon Receptor
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Cancer
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YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness.
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- HY-U00365
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- HY-101913
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- HY-114191
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- HY-129636A
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GABAB receptor antagonist 1
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GABA Receptor
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Neurological Disease
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GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
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- HY-111501
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- HY-113960
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ERRα antagonist-1
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Estrogen Receptor/ERR
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Cancer
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ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
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- HY-111669
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- HY-P2268
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RAGE antagonist peptide
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Amyloid-β
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|
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RAGE antagonist peptide is an antagonist of Receptor for advanced glycation end products (RAGE). RAGE blocks S100P, S100A4 and HMGB-1 mediated RAGE activation. RAGE antagonist peptide inhibits growth and metastasis of rat glioma tumors. RAGE antagonist peptide also reduces cell growth and RAGE-mediated NF-κB activity in human PDAC cell lines.
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- HY-U00286
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- HY-B0845
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Prochloraz
BTS 40542
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Fungal
Estrogen Receptor/ERR
Androgen Receptor
Aryl Hydrocarbon Receptor
|
Infection
|
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Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50=40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s=25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50=1 μM).
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- HY-133123
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- HY-101695
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- HY-114191A
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- HY-101116
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- HY-U00321
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- HY-125821
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Sigma-1 receptor antagonist 1
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Sigma Receptor
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Neurological Disease
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Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.
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- HY-114025
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- HY-133555
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- HY-125819
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- HY-137175
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TMBIM6 antagonist-1
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mTOR
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Cancer
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TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+.
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- HY-131016
-
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IHR-Cy3
|
Smo
|
Cancer
|
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IHR-Cy3 is a potent fluorescent Smo antagonist with an IC50 of 100 nM.
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- HY-135976
-
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P2X3 antagonist 34
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
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P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.
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- HY-U00382
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- HY-101704
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- HY-108323
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CCR2 antagonist 4
Teijin compound 1
|
CCR
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Inflammation/Immunology
|
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CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
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- HY-103362
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CCR2 antagonist 4 hydrochloride
Teijin compound 1 hydrochloride
|
CCR
|
Inflammation/Immunology
|
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CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
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- HY-129995
-
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TSHR antagonist S37b
|
TSH Receptor
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Endocrinology
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TSHR antagonist S37b is the less effective enantiomer of TSHR antagonist S37a (HY-129995A). TSHR antagonist S37b shows only a minor effect for thyrotropin receptor (TSHR) inhibition. TSHR antagonist S37b can be used for the research of thyroid function.
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- HY-100692
-
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Lin28-let-7a antagonist 1
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MicroRNA
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Cancer
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Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction.
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- HY-19317
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- HY-102024
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- HY-103009
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MSX-127
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CXCR
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Cancer
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MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis.
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- HY-103010
-
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MSX-130
|
CXCR
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Cancer
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MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis.
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- HY-P1376
-
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G-Protein antagonist peptide
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mAChR
Adrenergic Receptor
|
Endocrinology
|
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G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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- HY-16692
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- HY-122136
-
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S26131
|
Melatonin Receptor
|
Neurological Disease
|
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S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.
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- HY-101802
-
-
- HY-U00010
-
-
- HY-101622
-
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- HY-110203
-
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R-7050
TNF-α antagonist III
|
TNF Receptor
|
Cancer
|
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R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
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- HY-129946
-
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- HY-P1376A
-
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G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
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G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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- HY-15108
-
-
- HY-W014325
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- HY-110303
-
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- HY-130256
-
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β-NF-JQ1
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
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β-NF-JQ1 is a PROTAC that recruits AhR E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
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- HY-N4095
-
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- HY-12451
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- HY-133533
-
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- HY-133112
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- HY-100242
-
-
- HY-N0178
-
-
- HY-100382
-
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FPTQ
|
mGluR
|
Others
|
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FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.
|
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- HY-N0279
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-
- HY-111441
-
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- HY-135750
-
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VAF347
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
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VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14 +CD11b + monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.
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- HY-112050
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-
- HY-130269
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β-Naphthoflavone-CH2-OH
β-NF-CH2-OH
|
Ligand for E3 Ligase
|
Cancer
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β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-112627
-
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- HY-135147
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ONC206
|
Dopamine Receptor
|
Cancer
Neurological Disease
|
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ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
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- HY-P1321
-
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GR231118
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
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GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8).
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- HY-P1321A
-
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GR231118 TFA
1229U91 TFA; GW1229 TFA
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Neuropeptide Y Receptor
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Neurological Disease
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GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8).
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- HY-P1276
-
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- HY-16474
-
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Relugolix
TAK-385
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GnRH Receptor
|
Cancer
Endocrinology
|
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Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
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- HY-109044
-
-
- HY-14407
-
-
- HY-14407A
-
-
- HY-P1276A
-
-
- HY-12397
-
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ZK159222
|
VD/VDR
|
Endocrinology
|
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ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character.
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- HY-N6932
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-
- HY-15484
-
-
- HY-N6264
-
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27-Deoxyactein
|
Others
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Metabolic Disease
|
|
27-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 27-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels.
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- HY-16031
-
-
- HY-12028
-
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PD98059
|
MEK
ERK
Aryl Hydrocarbon Receptor
Autophagy
|
Cancer
|
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PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy.
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- HY-17038A
-
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Agomelatine hydrochloride
S-20098 hydrochloride
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
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- HY-17038
-
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Agomelatine
S-20098
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
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|
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
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- HY-17038B
-
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Agomelatine (L(+)-Tartaric acid)
S-20098 L(+)-Tartaric acid
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
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- HY-B0311A
-
|
Carbidopa monohydrate
(S)-(-)-Carbidopa monohydrate
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
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- HY-B0311
-
|
Carbidopa
(S)-(-)-Carbidopa
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-N0170
-
-
- HY-101198
-
|
Clobenpropit dihydrobromide
|
Histamine Receptor
Apoptosis
|
Cancer
Neurological Disease
|
|
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
|
-
- HY-101283
-
|
HCH6-1
|
Others
|
Inflammation/Immunology
|
|
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases.
|
-
- HY-130842
-
-
- HY-19826
-
-
- HY-A0083
-
|
Methacholine chloride
Acetyl-β-methylcholine chloride
|
mAChR
|
Others
|
|
Methacholine (Acetyl-β-methylcholine) chloride acts a muscarinic M3 receptor agonist in the parasympathetic nervous system. Methacholine chloride acts directly on acetylcholine receptors on smooth muscle causing contraction and airway narrowing. Methacholine challenges are widely used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
|
-
- HY-103575A
-
|
MFZ 10-7 hydrochloride
|
mGluR
|
Neurological Disease
|
|
MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.
|
-
- HY-W011338
-
|
Benzyl butyl phthalate
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs).
|
-
- HY-10036
-
-
- HY-50158
-
-
- HY-128781
-
-
- HY-100122
-
-
- HY-22437
-
-
- HY-118844
-
-
- HY-U00121
-
-
- HY-B1439B
-
-
- HY-50713
-
-
- HY-B0918
-
-
- HY-107430
-
|
Oxythiamine
Hydroxythiamin
|
Others
|
Cancer
|
|
Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
|
-
- HY-110037
-
-
- HY-B1205A
-
|
Atropine sulfate
Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
|
mAChR
|
Neurological Disease
|
|
Atropine (Tropine tropate) sulfate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist.
|
-
- HY-117793
-
-
- HY-15257A
-
-
- HY-104059
-
-
- HY-B0548S1
-
-
- HY-121186
-
-
- HY-117153
-
-
- HY-111484
-
-
- HY-70002B
-
-
- HY-N1163
-
-
- HY-N3610
-
|
Coclaurine
|
nAChR
|
Neurological Disease
|
|
Coclaurine is a class of tetrahydroisoquinoline alkaloids isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist.
|
-
- HY-15540
-
-
- HY-18668
-
-
- HY-B2111
-
-
- HY-100648
-
-
- HY-100649
-
-
- HY-100248
-
-
- HY-Z0816
-
-
- HY-U00067
-
-
- HY-101685
-
-
- HY-15066
-
|
CNQX
FG9065
|
iGluR
|
Neurological Disease
|
|
CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist. CNQX blocks the expression of fear-potentiated startle in rats.
|
-
- HY-112056
-
-
- HY-15277
-
-
- HY-101638
-
-
- HY-19638A
-
|
Cangrelor tetrasodium
|
P2Y Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist.
|
-
- HY-16991
-
-
- HY-B1547A
-
-
- HY-100266
-
-
- HY-19223
-
-
- HY-101658
-
-
- HY-101817
-
-
- HY-U00017
-
-
- HY-70050AS
-
-
- HY-B0524A
-
-
- HY-131449
-
-
- HY-D0237
-
-
- HY-B0524
-
-
- HY-12503
-
-
- HY-12195
-
-
- HY-15066A
-
|
CNQX disodium
FG9065 disodium
|
iGluR
|
Neurological Disease
|
|
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.
|
-
- HY-19818A
-
-
- HY-19705B
-
-
- HY-N2189
-
-
- HY-109139
-
-
- HY-13242
-
|
Taladegib
LY2940680
|
Smo
|
Cancer
|
|
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
|
-
- HY-15372
-
-
- HY-106910
-
-
- HY-100850
-
-
- HY-B1589A
-
-
- HY-B1014
-
-
- HY-101574
-
-
- HY-101594
-
-
- HY-U00062
-
-
- HY-101675
-
-
- HY-101707
-
-
- HY-B1240
-
-
- HY-105117
-
-
- HY-111755
-
-
- HY-16346S
-
-
- HY-128878
-
-
- HY-17039S
-
-
- HY-G0014B
-
-
- HY-G0014A
-
-
- HY-101534
-
-
- HY-U00247
-
-
- HY-B0768A
-
-
- HY-U00245
-
-
- HY-13202
-
-
- HY-U00202
-
-
- HY-B0460
-
-
- HY-100173
-
-
- HY-100903
-
-
- HY-N0219
-
-
- HY-B1165
-
-
- HY-B0462A
-
-
- HY-U00110
-
-
- HY-103531
-
-
- HY-B0325
-
-
- HY-16635
-
-
- HY-U00119
-
-
- HY-101691
-
-
- HY-B0547A
-
-
- HY-B1303A
-
-
- HY-13209
-
-
- HY-110254
-
-
- HY-B2154
-
-
- HY-A0019
-
|
Paliperidone
9-Hydroxyrisperidone
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
|
-
- HY-B0561
-
-
- HY-131256
-
-
- HY-P1025
-
-
- HY-N2079
-
-
- HY-N6628
-
-
- HY-U00234
-
-
- HY-A0027
-
-
- HY-100255
-
-
- HY-110110
-
-
- HY-U00139
-
-
- HY-A0250
-
-
- HY-100454
-
-
- HY-112620
-
-
- HY-B0205
-
-
- HY-B1283
-
-
- HY-B1303
-
-
- HY-103184
-
-
- HY-100668
-
-
- HY-100292
-
-
- HY-15539
-
-
- HY-101743
-
-
- HY-B0286A
-
-
- HY-B1164
-
-
- HY-17465
-
-
- HY-P1329
-
-
- HY-100191
-
-
- HY-112248
-
-
- HY-19733
-
-
- HY-14276A
-
|
Gallopamil hydrochloride
Methoxyverapamil hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-14276
-
|
Gallopamil
Methoxyverapamil
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-112730
-
|
PEO-IAA
2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid
|
Others
|
Others
|
|
PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
|
-
- HY-14778
-
-
- HY-16168A
-
-
- HY-15085
-
-
- HY-17037
-
-
- HY-B2168
-
-
- HY-19732
-
-
- HY-16763
-
-
- HY-B0009
-
-
- HY-P1329A
-
-
- HY-10164
-
-
- HY-101632
-
-
- HY-U00019
-
-
- HY-101600
-
-
- HY-101618
-
-
- HY-15073
-
-
- HY-B0895
-
-
- HY-18555
-
|
TMPA
|
Others
|
Others
|
|
TMPA is an antagonist of nuclear receptor Nur77 and LKB1 interaction.
|
-
- HY-18101A
-
-
- HY-U00040
-
-
- HY-102004
-
-
- HY-42849
-
-
- HY-15487
-
-
- HY-13021
-
-
- HY-17582
-
-
- HY-100471
-
-
- HY-19737A
-
-
- HY-101502A
-
-
- HY-12710A
-
-
- HY-16509
-
-
- HY-112703
-
-
- HY-14538A
-
-
- HY-P0061
-
-
- HY-13439
-
-
- HY-12114
-
-
- HY-50663
-
-
- HY-42849A
-
-
- HY-109077
-
-
- HY-101797
-
-
- HY-A0066
-
-
- HY-15758
-
-
- HY-U00018
-
-
- HY-19243
-
-
- HY-101668
-
-
- HY-15105
-
-
- HY-101679
-
-
- HY-19163
-
-
- HY-103099
-
-
- HY-100153
-
-
- HY-14284
-
-
- HY-14656
-
-
- HY-14538
-
-
- HY-N0096
-
-
- HY-B1416A
-
-
- HY-103213
-
-
- HY-12881
-
|
Eliprodil
SL-820715
|
iGluR
|
Neurological Disease
|
|
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
|
-
- HY-103476
-
|
Ro15-4513
|
GABA Receptor
|
Neurological Disease
|
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect.
|
-
- HY-N0607
-
-
- HY-13706A
-
|
CAY10471
TM30089
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model.
|
-
- HY-100405
-
|
FTIDC
|
mGluR
|
Neurological Disease
|
|
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.
|
-
- HY-100637
-
|
Hydroxybupropion
|
Adrenergic Receptor
nAChR
|
Neurological Disease
|
|
Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .
|
-
- HY-A0066A
-
-
- HY-17492
-
-
- HY-B0774
-
-
- HY-76520
-
-
- HY-15709
-
-
- HY-110095
-
-
- HY-18697
-
-
- HY-112604
-
-
- HY-15574
-
-
- HY-19768
-
-
- HY-102093
-
-
- HY-12426
-
-
- HY-12380
-
-
- HY-B1487
-
-
- HY-B0004
-
-
- HY-12380A
-
-
- HY-16732
-
-
- HY-U00363
-
-
- HY-A0075
-
-
- HY-A0145
-
|
Phenprocoumon
|
Others
|
Others
|
|
Phenprocoumon is a coumarin derivative that acts as a long acting oral anticoagulant and an antagonist of vitamin K.
|
-
- HY-16701
-
|
BV6
|
IAP
|
Cancer
|
|
BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
|
-
- HY-12510
-
-
- HY-15574A
-
-
- HY-P0264
-
-
- HY-U00086
-
-
- HY-U00026
-
-
- HY-19684
-
-
- HY-14390
-
-
- HY-101706
-
-
- HY-101830
-
-
- HY-101721
-
-
- HY-50912
-
-
- HY-P0209
-
-
- HY-U00283
-
-
- HY-15702
-
|
HJC0350
|
Others
|
Cancer
|
|
HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.
|
-
- HY-U00404
-
-
- HY-U00188
-
-
- HY-U00207
-
-
- HY-50691
-
-
- HY-A0019A
-
|
Paliperidone palmitate
9-Hydroxyrisperidone palmitate
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia.
|
-
- HY-100607A
-
-
- HY-U00443
-
-
- HY-B1438
-
-
- HY-112667
-
-
- HY-U00263
-
-
- HY-B0682A
-
-
- HY-B0355
-
-
- HY-101527
-
|
20-HEDE
WIT 002
|
Others
|
Cancer
|
|
20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
|
-
- HY-10259
-
-
- HY-110110A
-
-
- HY-13541
-
|
ADH-1
|
Others
|
Cancer
|
|
ADH-1, an N-cadherin antagonist, inhibits N-cadherin mediated cell adhesion.
|
-
- HY-14423
-
-
- HY-A0033
-
-
- HY-B0500
-
-
- HY-B0298A
-
-
- HY-B1108
-
-
- HY-U00212
-
-
- HY-101177
-
-
- HY-11103
-
-
- HY-14369
-
-
- HY-18611A
-
-
- HY-14770
-
-
- HY-107765
-
-
- HY-108324
-
-
- HY-10259A
-
-
- HY-14130
-
-
- HY-N1378
-
-
- HY-14447
-
-
- HY-18611
-
-
- HY-101683
-
-
- HY-14129
-
-
- HY-19855
-
-
- HY-15853
-
-
- HY-14367
-
-
- HY-15640
-
-
- HY-13004
-
-
- HY-13796
-
-
- HY-118861A
-
-
- HY-103533
-
-
- HY-14432
-
-
- HY-101407
-
-
- HY-14277A
-
-
- HY-105201
-
|
Fabesetron
FK1052 free base
|
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.
|
-
- HY-B0569
-
|
Hexamethonium Bromide
|
nAChR
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models.
|
-
- HY-32329
-
|
Setiptiline
Org-8282
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-14263
-
|
Pericyazine
Propericiazine; RP 8909
|
Dopamine Receptor
|
Neurological Disease
|
|
Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis. Pericyazine is a selective D2-dopamine receptor antagonist. Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects.
|
-
- HY-B0781
-
-
- HY-114452
-
|
LY-2940094
|
Opioid Receptor
|
Neurological Disease
|
|
LY-2940094 is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY-2940094 reduces ethanol self-administration in animal models.
|
-
- HY-110155A
-
|
(Rac)-LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
|
-
- HY-103200
-
-
- HY-100672
-
-
- HY-112558
-
-
- HY-13541A
-
-
- HY-N0184
-
-
- HY-B0192A
-
-
- HY-P0171
-
-
- HY-B0192
-
-
- HY-50669A
-
-
- HY-15412
-
|
HhAntag
|
Smo
|
Cancer
|
|
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
|
-
- HY-16502
-
|
Transcrocetinate disodium
Disodium trans-crocetinate
|
iGluR
|
Cancer
|
|
Transcrocetinate disodium, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
|
-
- HY-14538S
-
-
- HY-10560
-
-
- HY-12635
-
-
- HY-U00253
-
-
- HY-U00106
-
-
- HY-19632
-
-
- HY-B0549A
-
-
- HY-19193
-
-
- HY-100152
-
-
- HY-110136A
-
-
- HY-19391
-
-
- HY-42937
-
|
Transcrocetin meglumine salt
trans-Crocetin meglumine salt
|
iGluR
|
Cancer
|
|
Transcrocetin meglumine salt, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
|
-
- HY-10052
-
-
- HY-19914
-
-
- HY-U00252
-
-
- HY-B0369A
-
-
- HY-B0412
-
-
- HY-12752A
-
-
- HY-43711
-
-
- HY-B1510
-
-
- HY-17001A
-
-
- HY-19654
-
-
- HY-101620
-
-
- HY-101700
-
-
- HY-101669
-
-
- HY-17505
-
-
- HY-B1225
-
-
- HY-101718
-
-
- HY-110136
-
-
- HY-14538S1
-
-
- HY-108997
-
-
- HY-B1613A
-
-
- HY-15319B
-
-
- HY-15129
-
|
O-Phospho-L-serine
L-Serine O-phosphate; L-SOP
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
|
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
|
-
- HY-116637
-
|
Tetrahydromagnolol
Magnolignan
|
Cannabinoid Receptor
GPR55
|
Inflammation/Immunology
|
|
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.
|
-
- HY-103360
-
|
J-113863
|
CCR
|
Inflammation/Immunology
|
|
J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.
|
-
- HY-32329A
-
|
Setiptiline maleate
MO-8282
|
5-HT Receptor
|
Neurological Disease
|
|
Setiptiline (MO-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-100703
-
-
- HY-16978
-
-
- HY-17001
-
-
- HY-B0538A
-
-
- HY-100318
-
-
- HY-A0012
-
-
- HY-B1517A
-
-
- HY-P1558
-
-
- HY-17512
-
-
- HY-15195
-
-
- HY-W018061
-
-
- HY-B1081
-
-
- HY-12426A
-
-
- HY-13059B
-
-
- HY-U00356
-
-
- HY-15462
-
-
- HY-U00392
-
-
- HY-B0539
-
-
- HY-19057A
-
-
- HY-B1435
-
-
- HY-13059
-
-
- HY-B0716
-
-
- HY-18966
-
-
- HY-15411
-
-
- HY-10634
-
-
- HY-U00251
-
-
- HY-12799
-
-
- HY-B1517
-
-
- HY-15835
-
|
CUDC-427
GDC-0917
|
IAP
|
Cancer
|
|
CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.
|
-
- HY-U00084
-
-
- HY-19909
-
|
NRC-2694
|
EGFR
|
Cancer
|
|
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
|
-
- HY-19110
-
-
- HY-U00076
-
-
- HY-19274
-
-
- HY-111398
-
-
- HY-U00105
-
-
- HY-15541
-
-
- HY-12377
-
-
- HY-B0909
-
-
- HY-10064
-
-
- HY-14751
-
-
- HY-125879
-
-
- HY-B1126
-
-
- HY-100308
-
-
- HY-A0295
-
-
- HY-110279
-
|
Ogerin
|
Others
|
Neurological Disease
|
|
Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
|
-
- HY-15403
-
-
- HY-103407A
-
-
- HY-50901
-
-
- HY-13636B
-
|
Fulvestrant (R enantiomer)
ICI 182780 (R enantiomer); ZD 9238 (R enantiomer); ZM 182780 (R enantiomer)
|
Others
|
Cancer
|
|
Fulvestrant R enantiomer (ICI 182780 R enantiomer) is the R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
|
-
- HY-13059A
-
-
- HY-120689
-
-
- HY-B0431A
-
-
- HY-B0478
-
-
- HY-10995
-
-
- HY-19347
-
-
- HY-P1014
-
-
- HY-13534
-
-
- HY-108688
-
-
- HY-A0021
-
-
- HY-14338A
-
-
- HY-16756
-
-
- HY-100882
-
-
- HY-A0018
-
-
- HY-120090
-
-
- HY-13282
-
|
GANT 58
NSC 75503
|
Gli
|
Cancer
|
|
GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM.
|
-
- HY-19489S
-
-
- HY-101105A
-
-
- HY-B0202
-
-
- HY-10486
-
-
- HY-14914
-
-
- HY-B0780
-
-
- HY-105018
-
|
Epelsiban
GSK 557296
|
Oxytocin Receptor
|
Endocrinology
|
|
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
|
-
- HY-17024
-
-
- HY-12428
-
-
- HY-19191
-
-
- HY-12131
-
-
- HY-14938
-
-
- HY-19025
-
-
- HY-19969
-
-
- HY-112710
-
-
- HY-118678
-
-
- HY-13636A
-
|
Fulvestrant (S enantiomer)
ICI 182780 (S enantiomer); ZD 9238 (S enantiomer); ZM 182780 (S enantiomer)
|
Others
|
Cancer
|
|
Fulvestrant S enantiomer (ICI 182780 S enantiomer) is the S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
|
-
- HY-U00143
-
-
- HY-P1572
-
-
- HY-N0145
-
-
- HY-12777
-
-
- HY-U00354
-
-
- HY-12301
-
-
- HY-N2332A
-
-
- HY-12715
-
-
- HY-14561A
-
|
Idazoxan hydrochloride
RX 781094 hydrochloride
|
Adrenergic Receptor
Imidazoline Receptor
|
Neurological Disease
Endocrinology
|
|
Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like drugs (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism.
|
-
- HY-101755
-
-
- HY-15084
-
-
- HY-12339
-
|
NVS-CRF38
|
CRFR
|
Endocrinology
|
|
NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
|
-
- HY-P1017
-
-
- HY-16993
-
-
- HY-15009
-
-
- HY-50175
-
-
- HY-111442
-
|
GC 14
|
Others
|
Metabolic Disease
|
|
GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 35 nM and 200 nM for hTRβ and hTRα, respectively.
|
-
- HY-108251
-
-
- HY-128351
-
-
- HY-19512
-
-
- HY-100717
-
-
- HY-15577
-
|
GSK3787
|
PPAR
|
Cancer
|
|
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
|
-
- HY-A0024
-
|
Tolterodine
(R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
|
mAChR
|
Neurological Disease
|
|
Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-15068
-
|
NBQX
FG9202
|
iGluR
|
Neurological Disease
|
|
NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity.
|
-
- HY-19736
-
-
- HY-19654B
-
-
- HY-B1059
-
-
- HY-B0595
-
-
- HY-W040146
-
-
- HY-15403A
-
-
- HY-A0163
-
-
- HY-B0205S
-
-
- HY-B0325S
-
-
- HY-118180
-
-
- HY-112895
-
|
UT-155
|
Androgen Receptor
|
Cancer
|
|
UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
|
-
- HY-U00402
-
-
- HY-19097
-
-
- HY-U00077
-
-
- HY-19048
-
-
- HY-U00028
-
-
- HY-U00237
-
-
- HY-B1305
-
-
- HY-101022
-
-
- HY-B0354A
-
-
- HY-P0061A
-
-
- HY-14467
-
-
- HY-14249
-
-
- HY-15538
-
-
- HY-N4247
-
-
- HY-B1081A
-
-
- HY-B0394
-
-
- HY-135363
-
-
- HY-18287
-
|
MRT-83
|
Smo
|
Cancer
|
|
MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
|
-
- HY-101986
-
-
- HY-101486
-
|
LF3
|
β-catenin
|
Cancer
|
|
LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.
|
-
- HY-101586
-
-
- HY-12506A
-
|
Naspm trihydrochloride
1-Naphthylacetyl spermine trihydrochloride
|
iGluR
|
Neurological Disease
|
|
Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
|
-
- HY-109565
-
|
ASTX660
|
IAP
|
Cancer
|
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-16985
-
|
Darolutamide
ODM-201; BAY-1841788
|
Androgen Receptor
|
Cancer
|
|
Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
|
-
- HY-12488
-
-
- HY-15726
-
-
- HY-B0686
-
-
- HY-15851
-
-
- HY-12940
-
-
- HY-P0009B
-
-
- HY-N0382
-
|
Galangin
Norizalpinin; 3,5,7-Trihydroxyflavone
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
|
-
- HY-10900
-
-
- HY-P0009A
-
-
- HY-17390
-
-
- HY-U00137
-
-
- HY-109593
-
-
- HY-104020A
-
-
- HY-16060
-
-
- HY-110255
-
-
- HY-18204
-
-
- HY-101395
-
-
- HY-B0686A
-
-
- HY-A0013A
-
-
- HY-13534A
-
-
- HY-101720
-
|
Fradafiban
BIBU-52
|
Integrin
|
Cardiovascular Disease
|
|
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
|
-
- HY-101598
-
-
- HY-101686
-
-
- HY-15853A
-
-
- HY-107437
-
-
- HY-A0013
-
-
- HY-110255A
-
-
- HY-10888
-
-
- HY-17390A
-
-
- HY-15481
-
-
- HY-100407
-
|
JNJ16259685
|
mGluR
|
Neurological Disease
|
|
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
|
-
- HY-P1309A
-
-
- HY-103104
-
|
Fananserin
RP 62203
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
|
-
- HY-124290
-
|
Carotegrast methyl
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of AJM300, is a specific, dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
|
-
- HY-B1510S
-
-
- HY-B0071
-
-
- HY-12506
-
|
Naspm
1-Naphthylacetyl spermine
|
iGluR
|
Neurological Disease
|
|
Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
|
-
- HY-14551
-
-
- HY-107735
-
-
- HY-17428
-
-
- HY-50081
-
-
- HY-13677
-
-
- HY-109002
-
-
- HY-101503
-
|
HTS01037
|
FABP
|
Metabolic Disease
|
|
HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
|
-
- HY-70002
-
-
- HY-119217
-
-
- HY-B0750
-
|
Dolasetron
MDL-73147
|
5-HT Receptor
|
Others
|
|
Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
|
-
- HY-12780S
-
-
- HY-17000
-
-
- HY-100209
-
|
Sufugolix
TAK-013
|
Others
|
Endocrinology
|
|
Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
|
-
- HY-15488
-
-
- HY-B0303A
-
-
- HY-101844
-
-
- HY-15653
-
-
- HY-19900
-
-
- HY-B0071A
-
-
- HY-10487
-
-
- HY-B0322
-
|
Sulfamethoxazole
Ro 4-2130
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamethoxazole (Ro 4-2130) is a sulfonamide bacteriostatic antibiotic, used for bacterial infections. Sulfonamides is a competitive antagonists of para-aminobenzoic acid (PABA).
|
-
- HY-15488A
-
-
- HY-101833
-
|
YM-264
|
Others
|
Inflammation/Immunology
|
|
YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
|
-
- HY-101727
-
-
- HY-12127
-
-
- HY-116408A
-
-
- HY-17351
-
-
- HY-101953
-
-
- HY-105545
-
|
Dexetimide
(+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide
|
mAChR
|
Neurological Disease
|
|
Dexetimide ((+)-Benzetimide) is a high-affinity muscarinic receptor antagonist and a potent and persistent anticholinergic agent used to treat neuroleptic-induced parkinsonism.
|
-
- HY-B0202S
-
-
- HY-108690
-
|
Fluxametamide
|
GABA Receptor
|
Others
|
|
Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
|
-
- HY-14789
-
|
(R)-Elagolix
NBI-56418
|
GnRH Receptor
|
Cancer
Endocrinology
|
|
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
|
-
- HY-A0125A
-
-
- HY-18263C
-
|
Elubrixin tosylate
SB-656933 tosylate
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
|
-
- HY-18263A
-
|
Elubrixin
SB-656933
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
|
-
- HY-16312
-
|
MDL-29951
|
iGluR
|
Neurological Disease
|
|
MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [ 3H]glycine binding in vitro and in vivo.
|
-
- HY-101458
-
-
- HY-101910
-
-
- HY-15443
-
-
- HY-15676
-
-
- HY-P0216
-
-
- HY-15370
-
-
- HY-10857
-
-
- HY-17004
-
-
- HY-101226
-
|
MSOP
|
mGluR
|
Neurological Disease
|
|
MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
|
-
- HY-113534
-
|
MV1
|
IAP
Apoptosis
|
Others
|
|
MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
|
-
- HY-12366
-
-
- HY-17436
-
-
- HY-103361
-
-
- HY-133570
-
|
17-AEP-GA
|
HSP
ADC Cytotoxin
|
Cancer
|
|
17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
|
-
- HY-10388
-
-
- HY-13535A
-
-
- HY-B0377
-
-
- HY-101809
-
-
- HY-101815
-
-
- HY-19477
-
-
- HY-19189
-
-
- HY-19062
-
-
- HY-15068A
-
|
NBQX disodium
FG9202 disodium
|
iGluR
|
Neurological Disease
|
|
NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity.
|
-
- HY-103456
-
-
- HY-13508
-
-
- HY-16582A
-
|
Sonidegib
Erismodegib; LDE225; NVP-LDE225
|
Smo
|
Cancer
|
|
Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
|
-
- HY-101458A
-
-
- HY-U00238
-
-
- HY-B1494
-
-
- HY-15799
-
-
- HY-B1716
-
|
L-5-Hydroxytryptophan
L-5-HTP; Oxitriptan
|
Endogenous Metabolite
|
Metabolic Disease
Neurological Disease
|
|
L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia.
|
-
- HY-B0031S
-
-
- HY-14791A
-
-
- HY-100720
-
-
- HY-N0127
-
-
- HY-112202
-
-
- HY-12525
-
-
- HY-B0750B
-
-
- HY-15421
-
-
- HY-U00185
-
-
- HY-12765S
-
-
- HY-100506
-
|
GLPG0187
|
Integrin
|
Cancer
|
|
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
|
-
- HY-17360
-
|
Tiotropium Bromide
BA679 BR
|
mAChR
|
Neurological Disease
|
|
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-17512A
-
-
- HY-17621
-
-
- HY-100129
-
-
- HY-112840
-
-
- HY-19205A
-
-
- HY-10792
-
-
- HY-B0750A
-
-
- HY-101179
-
-
- HY-16683
-
-
- HY-108634
-
|
Apafant
WEB 2086
|
Others
|
Inflammation/Immunology
|
|
Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
|
-
- HY-P1203
-
-
- HY-U00151
-
-
- HY-P1727
-
|
Super-TDU
|
YAP
|
Cancer
|
|
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model.
|
-
- HY-70002S
-
-
- HY-103449
-
-
- HY-101619
-
-
- HY-19214
-
-
- HY-136596
-
|
Apalutamide-COOH
|
Others
|
Cancer
|
|
Apalutamide-COOH can be used to synthesis Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
|
-
- HY-17458
-
-
- HY-100409
-
|
PHCCC
|
mGluR
|
Cancer
|
|
PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.
|
-
- HY-16704
-
|
ESI-09
|
Virus Protease
|
Cancer
|
|
ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.
|
-
- HY-13274
-
-
- HY-12497
-
-
- HY-128379
-
|
Labetalone hydrochloride
|
Others
|
Others
|
|
Labetalone hydrochloride is an impurity of Labetalol. Labetalol is an orally active adrenoceptor blocking drug which is a competitive antagonist at both alpha- and beta-adrenoceptor sites.
|
-
- HY-10633
-
-
- HY-100619
-
|
BMS-986020
|
LPL Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
BMS-986020 is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
|
-
- HY-100619A
-
|
BMS-986020 sodium
|
LPL Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
|
-
- HY-P1750
-
|
Shepherdin (79-87)
|
HSP
Survivin
|
Cancer
|
|
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity.
|
-
- HY-P2542
-
-
- HY-P1869
-
-
- HY-115506
-
-
- HY-13505
-
-
- HY-I0230
-
-
- HY-14736
-
-
- HY-16040
-
-
- HY-19989A
-
-
- HY-12870A
-
|
AZD9496 maleate
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
|
-
- HY-135588
-
-
- HY-P1203A
-
-
- HY-10794
-
-
- HY-B0164A
-
-
- HY-101924
-
-
- HY-17410A
-
-
- HY-107382
-
-
- HY-13466
-
-
- HY-U00355
-
-
- HY-10011
-
-
- HY-16711
-
-
- HY-B0115
-
-
- HY-101430
-
-
- HY-119433
-
|
Asoprisnil
J867
|
Progesterone Receptor
|
Endocrinology
|
|
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
|
-
- HY-13331
-
|
Clascoterone
Cortexolone 17 alpha-propionate; Cortexolone 17α-propionate; CB-03-01
|
Androgen Receptor
|
Endocrinology
|
|
Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
|
-
- HY-10889
-
-
- HY-136462
-
|
CYM50358
|
LPL Receptor
|
Infection
|
|
CYM50358 is a potent and selective S1PR4 antagonist, with an IC50 of 25 nM. CYM50358 can be used for the research of influenza infection.
|
-
- HY-B0164
-
-
- HY-13206
-
|
MTEP hydrochloride
|
mGluR
|
Neurological Disease
|
|
MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride produces antiparkinsonian-like effects.
|
-
- HY-135103
-
|
Tauro-β-muricholic acid sodium
T-βMCA sodium
|
FXR
|
Cancer
|
|
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
|
-
- HY-U00104
-
|
YM-46303
|
mAChR
|
Endocrinology
|
|
YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
|
-
- HY-30152
-
-
- HY-101736
-
|
AMG9810
|
TRP Channel
|
Neurological Disease
|
|
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
|
-
- HY-103228
-
-
- HY-100562
-
-
- HY-109987
-
|
ISPA-28
|
Parasite
|
Infection
|
|
ISPA-28 is a specific plasmodial surface anion channel (PSAC) antagonist. ISPA-28 binds directly and reversibly to CLAG3.
|
-
- HY-B1541
-
-
- HY-13683
-
-
- HY-12142
-
-
- HY-131914A
-
-
- HY-16582
-
|
Sonidegib diphosphate
Erismodegib diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate
|
Smo
|
Cancer
|
|
Sonidegib diphosphate (Erismodegib diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
|
-
- HY-19084
-
|
Ro-24-0238
|
Others
|
Inflammation/Immunology
|
|
Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
|
-
- HY-U00072
-
-
- HY-112284
-
-
- HY-12870
-
|
AZD9496
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally bioavailable selective oestrogen receptor degrader (SERD).
|
-
- HY-10561
-
|
RU 58841
PSK-3841; HMR-3841
|
Androgen Receptor
|
Endocrinology
|
|
RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen. RU 58841 (PSK-3841) has a dramatic effect on hair regrowth.
|
-
- HY-131277
-
-
- HY-B1655
-
|
Fluspirilene
R 6218; Redeptin
|
Calcium Channel
|
Neurological Disease
|
|
Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.
|
-
- HY-15706
-
-
- HY-119802
-
-
- HY-107382A
-
-
- HY-17410
-
-
- HY-109067
-
|
Opiranserin
|
GlyT
5-HT Receptor
P2X Receptor
|
Neurological Disease
|
|
Opiranserin, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
|
-
- HY-13222
-
-
- HY-B0979
-
|
Lobeline hydrochloride
α-Lobeline hydrochloride; L-Lobeline hydrochloride
|
nAChR
|
Neurological Disease
|
|
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
|
-
- HY-116790A
-
-
- HY-B1789A
-
-
- HY-13556A
-
|
Arzoxifene hydrochloride
LY 353381 HCl; SERM 3
|
Estrogen Receptor/ERR
|
Cancer
|
|
Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
|
-
- HY-15708
-
-
- HY-107649
-
|
Zamifenacin fumarate
UK-76654 fumarate
|
mAChR
|
Metabolic Disease
|
|
Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
|
-
- HY-10388A
-
-
- HY-15418
-
-
- HY-90010
-
|
Tolterodine tartrate
Kabi-2234; PNU-200583E
|
mAChR
|
Neurological Disease
|
|
Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
|
-
- HY-131278
-
-
- HY-19904
-
-
- HY-108522
-
|
PA452
|
RAR/RXR
|
Metabolic Disease
|
|
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.
|
-
- HY-75766S
-
-
- HY-15834A
-
-
- HY-16578
-
|
GW9662
|
PPAR
|
Cancer
|
|
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
|
-
- HY-103088
-
-
- HY-U00433A
-
-
- HY-A0084
-
|
Procainamide hydrochloride
|
Autophagy
|
Cancer
|
|
Procainamide hydrochloride is an anti-arrhythmic agent and is used to treat cardiac arrhythmia; induces rapid block of the batrachotoxin(BTX)-activated sodium channels of the heart muscle and acts as antagonist to long gating closures.
|
-
- HY-101336
-
-
- HY-B0002B
-
|
Ondansetron
GR 38032; SN 307
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron(GR 38032; SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
|
-
- HY-14880B
-
-
- HY-103454
-
-
- HY-N7067
-
|
Revaprazan hydrochloride
|
Bacterial
COX
|
Infection
|
|
Revaprazan hydrochloride is a novel acid pump antagonist (APA). Revaprazan hydrochloride reduces COX-2 expression and has significant anti-inflammatory actions activities in H. pylori infection.
|
-
- HY-19532
-
-
- HY-10871A
-
-
- HY-14537
-
-
- HY-12336
-
-
- HY-12981
-
-
- HY-19902
-
-
- HY-P1233
-
-
- HY-B1552B
-
-
- HY-131274
-
|
Fexofenadine Impurity F
|
Others
|
Others
|
|
Fexofenadine Impurity F is the impurity of Fexofenadine. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial.
|
-
- HY-N2064
-
|
Racanisodamine
|
mAChR
|
Neurological Disease
|
|
Racanisodamine is one of the racemic isomers of anisodamine, resembles anisodamine in pharmacological effect. Racanisodamine is a non-selective muscarinic antagonist, used as a component of eye drops for myopic control.
|
-
- HY-131041
-
|
Ned-K
|
Calcium Channel
|
Cardiovascular Disease
|
|
Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca 2+ oscillations in cardiomyocytes.
|
-
- HY-18347A
-
-
- HY-120261
-
-
- HY-14339
-
-
- HY-16682
-
|
AGN 196996
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).
|
-
- HY-13245
-
-
- HY-123337
-
|
Zamifenacin
UK-76654
|
mAChR
|
Metabolic Disease
|
|
Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
|
-
- HY-111271A
-
-
- HY-17446
-
-
- HY-U00117
-
-
- HY-10871
-
-
- HY-N0546
-
|
Ligustroflavone
Nuezhenoside
|
CaSR
|
Metabolic Disease
|
|
Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice.
|
-
- HY-B0002
-
|
Ondansetron hydrochloride
GR 38032 hydrochloride; SN 307 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron hydrochloride (GR 38032 hydrochloride; SN 307 hydrochloride) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
|
-
- HY-11029
-
-
- HY-108896
-
-
- HY-13677A
-
|
6-Mercaptopurine hydrate
Mercaptopurine hydrate; 6-MP hydrate
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
6-Mercaptopurine hydrate (Mercaptopurine hydrate; 6-MP hydrate) is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
|
-
- HY-B0407A
-
-
- HY-17369
-
-
- HY-19627
-
|
Naldemedine
S-297995
|
Opioid Receptor
|
Neurological Disease
|
|
Naldemedine (S-297995) is an orally active, peripherally acting µ-opioid receptor antagonist. Naldemedine shows potent binding affinities (IC50s = 1.15, 1.11, and 1.5 nM, repectively) and antagonist activities (IC50s= 25.57, 7.09, 16.1 nM, repectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine tempers opioid-induced constipation (OIC) without compromising opioid analgesia.
|
-
- HY-14564A
-
|
GTS-21 dihydrochloride
DMXB-A; DMBX-anabaseine
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
|
-
- HY-124754
-
|
BTRX-335140
CYM-53093
|
Opioid Receptor
|
Metabolic Disease
|
|
BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) .
|
-
- HY-110123
-
-
- HY-17497A
-
-
- HY-135589
-
-
- HY-B0031S1
-
-
- HY-15950
-
-
- HY-108329
-
-
- HY-117819
-
|
TMP920
|
ROR
|
Inflammation/Immunology
|
|
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
|
-
- HY-112302
-
-
- HY-14875
-
-
- HY-13527
-
-
- HY-14545A
-
-
- HY-131276
-
-
- HY-14121
-
-
- HY-B1388
-
|
Homatropine methylbromide
Homatropine methobromide
|
mAChR
|
Neurological Disease
|
|
Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
|
-
- HY-16996A
-
-
- HY-17497S
-
-
- HY-10013A
-
-
- HY-32709
-
|
Telcagepant
MK-0974
|
CGRP Receptor
|
Neurological Disease
|
|
Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
|
-
- HY-107723
-
-
- HY-108463
-
|
A-967079
|
TRP Channel
|
Inflammation/Immunology
|
|
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
|
-
- HY-110322A
-
|
PPTN
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. Anti-inflammatory and immune activity.
|
-
- HY-133080
-
|
BAY-784
|
GnRH Receptor
|
Cancer
|
|
BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively.
|
-
- HY-A0002
-
-
- HY-15498
-
|
Rimegepant
BMS-927711
|
CGRP Receptor
|
Neurological Disease
|
|
Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor.
|
-
- HY-101978
-
|
CPI-444
V81444; ciforadenant
|
Adenosine Receptor
|
Cancer
|
|
CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.
|
-
- HY-14914S
-
|
Azilsartan D5
TAK-536 D5
|
Angiotensin Receptor
|
Others
|
|
Azilsartan D5 (TAK-536 D5) is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist.
|
-
- HY-12294A
-
-
- HY-120691A
-
-
- HY-B0548S
-
-
- HY-14545
-
-
- HY-B0115A
-
-
- HY-116564
-
|
Lotilaner
|
Parasite
GABA Receptor
|
Infection
|
|
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor.
|
-
- HY-B0323
-
-
- HY-111534
-
|
SBI-115
|
GPCR19
|
Others
|
|
SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
|
-
- HY-100760
-
|
Toxoflavin
Xanthothricin; Toxoflavine; PKF-118-310
|
β-catenin
|
Cancer
|
|
Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity.
|
-
- HY-U00449
-
|
AGN 193109
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.
|
-
- HY-B0437
-
-
- HY-N0079
-
-
- HY-N6066
-
-
- HY-B0548AS
-
-
- HY-100316
-
-
- HY-17617
-
-
- HY-131255
-
-
- HY-P1267
-
|
α-Conotoxin PnIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-50697
-
-
- HY-A0081
-
-
- HY-19456
-
-
- HY-B0801A
-
-
- HY-107702
-
|
CGP 37849
|
iGluR
|
Neurological Disease
|
|
CGP 37849 is a potent, competitive and orally active N-methyl-D-aspartate (NMDA) receptor antagonist. CGP 37849 is an anticonvulsant in rodents and has antidepressant and anxiolytic-like effects.
|
-
- HY-109103
-
|
Tegatrabetan
BC2059
|
β-catenin
|
Cancer
|
|
Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).
|
-
- HY-12190A
-
-
- HY-121599
-
|
CGP 36742
SGS-742
|
GABA Receptor
|
Neurological Disease
|
|
CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC50 of 32 μM. CGP 36742 is useful in treatment of depression.
|
-
- HY-105542
-
-
- HY-14365
-
-
- HY-P1479
-
-
- HY-N0471
-
|
L-Hyoscyamine
Daturine
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205).
|
-
- HY-101381
-
|
Otenzepad
AF-DX 116
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
|
-
- HY-101106
-
|
AR7
|
RAR/RXR
|
Cancer
Neurological Disease
|
|
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.
|
-
- HY-A0034
-
|
Solifenacin
YM905 free base
|
mAChR
|
Neurological Disease
|
|
Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- HY-12789
-
|
Etrasimod
APD334
|
LPL Receptor
|
Inflammation/Immunology
|
|
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
|
-
- HY-B1986
-
|
p,p'-DDE
4,4'-DDE; p,p'-Dichlorodiphenyldichloroethylene
|
Androgen Receptor
Drug Metabolite
|
Endocrinology
|
|
p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM.
|
-
- HY-14825A
-
-
- HY-I0021
-
-
- HY-B1486
-
-
- HY-12190
-
-
- HY-P1233A
-
-
- HY-17004S
-
|
Olmesartan D4
RNH-6270 D4
|
Angiotensin Receptor
|
Others
|
|
Olmesartan D4 (RNH-6270 D4) is the deuterium labeled Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
|
-
- HY-Y0313
-
-
- HY-10806
-
-
- HY-15894
-
-
- HY-P1104A
-
|
FC131 TFA
|
CXCR
HIV
|
Infection
|
|
FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
|
-
- HY-121450
-
|
Lavoltidine
Loxtidine; AH-234844
|
Histamine Receptor
|
Cancer
|
|
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
|
-
- HY-10017
-
|
SCH 546738
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
|
-
- HY-P1479A
-
-
- HY-133775
-
-
- HY-N0584A
-
|
Anisodamine hydrobromide
6-Hydroxyhyoscyamine hydrobromide
|
mAChR
|
Inflammation/Immunology
|
|
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties.
|
-
- HY-12100
-
-
- HY-10562
-
-
- HY-131279
-
|
Olmesartan ethyl ester
|
Others
|
Others
|
|
Olmesartan ethyl ester (compound 11) is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to in the high blood pressure study.
|
-
- HY-P1187
-
|
HSDVHK-NH2
|
Integrin
|
Cancer
|
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
|
-
- HY-N0215
-
|
L-Phenylalanine
(S)-2-Amino-3-phenylpropionic acid
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca + channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
|
-
- HY-N3945
-
|
Glaucine
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
Adrenergic Receptor
Dopamine Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca 2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.
|
-
- HY-B1505
-
-
- HY-107051
-
-
- HY-101690
-
-
- HY-101348
-
-
- HY-13955
-
-
- HY-16060S
-
|
Apalutamide D4
ARN-509 D4
|
Androgen Receptor
|
Cancer
|
|
Apalutamide D4 (ARN-509 D4) is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
|
-
- HY-B0674
-
-
- HY-15284
-
|
Prasugrel
PCR 4099
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-12790
-
-
- HY-10805A
-
-
- HY-15069A
-
|
Fanapanel hydrate
ZK200775 hydrate; MPQX hydrate
|
iGluR
|
Neurological Disease
|
|
Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
|
-
- HY-103316
-
|
trans-Ned 19
|
Calcium Channel
|
Cardiovascular Disease
|
|
trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
|
-
- HY-P1187A
-
|
HSDVHK-NH2 TFA
|
Integrin
|
Cancer
|
HSDVHK-NH2 TFA is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
|
-
- HY-131942
-
-
- HY-P0205B
-
-
- HY-B1107
-
|
Naftidrofuryl oxalate
Nafronyl oxalate salt
|
5-HT Receptor
|
Cardiovascular Disease
|
|
Naftidrofuryl oxalate (Nafronyl oxalate salt) is a drug used in the management of peripheral and cerebral vascular disorders as a vasodilator, enhance cellular oxidative capacity, and may also be a 5-HT2 receptor antagonist.
|
-
- HY-108250
-
|
(R)-Bicalutamide
|
Androgen Receptor
|
Cancer
|
|
(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
|
-
- HY-17512S
-
-
- HY-B0068
-
-
- HY-129059
-
|
Odapipam
NNC 756
|
Dopamine Receptor
|
Neurological Disease
|
|
Odapipam (NNC 756) is a selective, high affinity and benzazepine dopamine D1 receptor antagonist with a Kd of 0.18 nM. Odapipam is also a superior positron emission tomography (PET) radiotracer.
|
-
- HY-107568
-
-
- HY-10898
-
-
- HY-B0745
-
-
- HY-B1270
-
-
- HY-10805
-
-
- HY-120478
-
|
ASP6432
|
LPL Receptor
|
Infection
|
|
ASP6432 is a potent and selective type 1 lysophosphatidic acid receptor (LPA1) antagonist with IC50s of 11 nM and 30 nM for human LPA1 and rat LPA1, respectively.
|
-
- HY-14777
-
|
Radiprodil
RGH-896
|
iGluR
|
Neurological Disease
|
|
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.
|
-
- HY-B0716S
-
-
- HY-15043
-
-
- HY-100183
-
-
- HY-104003
-
-
- HY-B0365A
-
-
- HY-P3066
-
|
SKF 100398
d(CH2)5Tyr(Et)VAVP
|
Vasopressin Receptor
|
Metabolic Disease
|
|
SKF 100398 (d(CH2)5Tyr(Et)VAVP) is an arginine vasopressin (AVP) analogue, and acts as a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.
|
-
- HY-19344
-
|
Lifitegrast
SAR 1118; SHP-606
|
Integrin
|
Inflammation/Immunology
|
|
Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
|
-
- HY-P1267A
-
|
α-Conotoxin PnIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-15072
-
|
Zonampanel
YM 872
|
iGluR
|
Metabolic Disease
|
|
Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
|
-
- HY-15284A
-
|
Prasugrel hydrochloride
PCR 4099 hydrochloride
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and prodrug, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-136255
-
|
AZD-9833
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD-9833 is a potent and orally active estrogen receptor (ER) antagonist. AZD-9833 is used for the study of
ER + HER2-advanced breast cancer.
|
-
- HY-B0002A
-
|
Ondansetron hydrochloride dihydrate
GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron hydrochloride dihydrate (GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
|
-
- HY-B0462
-
-
- HY-15069
-
|
Fanapanel
ZK200775; MPQX
|
iGluR
|
Neurological Disease
|
|
Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
|
-
- HY-10302
-
-
- HY-16617
-
|
Auglurant
VU0424238
|
mGluR
|
Neurological Disease
|
|
Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
|
-
- HY-15454
-
|
Xevinapant
AT-406; Debio 1143; SM-406
|
IAP
|
Cancer
|
|
Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
|
-
- HY-100783A
-
|
(-)-Bicuculline methochloride
l-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-111308
-
-
- HY-17572
-
|
Atosiban
RW22164; RWJ22164
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
|
|
Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.
|
-
- HY-105124A
-
-
- HY-103090
-
-
- HY-100208
-
|
HC-067047
|
TRP Channel
|
Cancer
|
|
HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
|
-
- HY-14111
-
-
- HY-50665
-
|
LY518674
LY-674
|
PPAR
|
Metabolic Disease
|
|
LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis.
|
-
- HY-10309
-
|
Sibrafiban
RO 48-3657
|
Integrin
|
Cardiovascular Disease
|
|
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
|
-
- HY-15472
-
-
- HY-B0321
-
|
Tropicamide
Ro 1-7683
|
mAChR
|
Neurological Disease
|
|
Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops.
|
-
- HY-U00367
-
-
- HY-A0015
-
-
- HY-B1205
-
|
Atropine
Tropine tropate; DL-Hyoscyamine
|
mAChR
Endogenous Metabolite
|
Neurological Disease
|
|
Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist, with anti-myopia effect. Atropine blocks the inhibitory effect of ACh on heart rate and contractility, potentially also leading to tachyarrhythmias.
|
-
- HY-B0366A
-
-
- HY-15744
-
-
- HY-100806
-
-
- HY-103473A
-
|
Boc-MLF TFA
Boc-Met-Leu-Phe-OH (TFA)
|
Others
|
Inflammation/Immunology
|
|
Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
|
-
- HY-100783
-
|
(-)-Bicuculline methobromide
l-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-108908
-
-
- HY-10301
-
|
MK-3207
|
CGRP Receptor
|
Neurological Disease
|
|
MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
|
-
- HY-101385
-
-
- HY-101784
-
-
- HY-107512
-
-
- HY-135230
-
|
LY2444296
FP3FBZ
|
Opioid Receptor
|
Neurological Disease
|
|
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.
|
-
- HY-18204S
-
-
- HY-107500
-
|
UVI 3003
|
RAR/RXR
Autophagy
|
Others
|
|
UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
|
-
- HY-108136A
-
|
Bisindolylmaleimide X hydrochloride
BIM-X hydrochloride; Ro31-8425 hydrochloride
|
PKC
CDK
|
Cardiovascular Disease
|
|
Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM.
|
-
- HY-13713
-
-
- HY-18689
-
|
SYM2206
|
iGluR
|
Neurological Disease
|
|
SYM2206 is a potent and non-competitive AMPA receptor antagonist, with an IC50 of 1.6 μM. SYM2206 blocks Nav1.6-mediated persistent currents.
|
-
- HY-B1621A
-
|
Cyclopentolate hydrochloride
DL-Cyclopentolate hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice.
|
-
- HY-124543
-
-
- HY-103090A
-
-
- HY-106441A
-
|
Rislenemdaz
MK-0657; CERC-301
|
iGluR
|
Neurological Disease
|
|
Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
|
-
- HY-115066
-
-
- HY-14185
-
-
- HY-115066A
-
-
- HY-15084A
-
|
(-)-Dizocilpine maleate
(-)-MK-801 maleate
|
iGluR
|
Neurological Disease
|
|
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.
|
-
- HY-P2497
-
-
- HY-B1808A
-
-
- HY-123918
-
|
JMS-17-2
|
Others
|
Cancer
Endocrinology
|
|
JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. JMS-17-2 impairs metastatic seeding and colonization of breast cancer cells.
|
-
- HY-16935
-
|
Mavatrep
JNJ-39439335
|
TRP Channel
|
Others
|
|
Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.
|
-
- HY-N4225
-
-
- HY-135329
-
|
Solifenacin D5 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- HY-11021
-
|
Elinogrel
PRT060128
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects.
|
-
- HY-B0437AS
-
-
- HY-16780
-
-
- HY-117606
-
|
LY3027788
|
mGluR
|
Neurological Disease
|
|
LY3027788, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 has antidepressant efficacy.
|
-
- HY-108908A
-
|
Modipafant
UK-80067
|
Others
|
Inflammation/Immunology
|
|
Modipafant (UK-80067), the (+)-enantiomer of UK-74505, is a potent, orally active, and selective platelet-activating factor (PAF) antagonist. Modipafant exhibits approximately double the intrinsic potency of UK-74505.
|
-
- HY-17369B
-
|
Tirofiban
L700462; MK383
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist
Target: integrin IIb/IIIa
Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
|
-
- HY-B0411
-
|
Domperidone
R33812
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.
|
-
- HY-133113
-
-
- HY-N0471A
-
|
L-Hyoscyamine sulfate
Daturine sulfate
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205).
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-
- HY-13408
-
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(+)-Apogossypol
Apogossypol; NSC736630
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Bcl-2 Family
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Cancer
|
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(+)-Apogossypol is a pan-BCL-2 antagonist. (+)-Apogossypol binds to Mcl-1, Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively.
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- HY-15284B
-
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Prasugrel (Maleic acid)
PCR 4099 (Maleic acid)
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P2Y Receptor
|
Cardiovascular Disease
|
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Prasugrel (PCR 4099) Maleic acid is a thienopyridine and prodrug, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
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- HY-11063
-
-
- HY-N7512
-
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Asimilobine
|
Dopamine Receptor
5-HT Receptor
Parasite
|
Cancer
Infection
|
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Asimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity.
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-
- HY-30234
-
-
- HY-100657
-
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meta-Fexofenadine
meta-MDL-16455; meta-Terfenadine carboxylate
|
Others
|
Inflammation/Immunology
|
|
meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial.
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-
- HY-B0548
-
-
- HY-119093
-
-
- HY-14144
-
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Aclidinium Bromide
LAS 34273; LAS-W 330
|
mAChR
|
Inflammation/Immunology
|
|
Aclidinium Bromide (LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist. Aclidinium Bromide has the potential for chronic obstructive pulmonary disease (COPD) research.
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-
- HY-135387
-
-
- HY-B1470
-
|
Azaperone
R-1929
|
Dopamine Receptor
|
Neurological Disease
|
|
Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
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-
- HY-101731
-
-
- HY-123918A
-
-
- HY-107633
-
|
A 1120
|
Others
|
Metabolic Disease
|
|
A 1120 is a high-affinity nonretinoid retinol-binding protein 4 (RBP4) antagonist with a Ki value of 8.3 nM. A 1120 disrupts the interaction between RBP4 and its binding partner transthyretin.
|
-
- HY-N6969
-
|
Dicentrine
|
Adrenergic Receptor
|
Endocrinology
|
|
Dicentrine is a natural product isolated from the plant Lindera megaphylla with antihypertensive effect. Dicentrine is an α1-adrenoceptor antagonist which has effective against human hyperplastic prostates.
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-
- HY-30234A
-
-
- HY-A0008
-
-
- HY-B1301
-
-
- HY-14184
-
-
- HY-101213
-
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OSW-1
|
Others
|
Cancer
|
|
OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI50s in the nanomolar range in human cancer lines.
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-
- HY-B0140
-
-
- HY-109024
-
-
- HY-135270
-
-
- HY-136338
-
|
Cimetidine sulfoxide
Cimetidine sulphoxide
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Cimetidine sulfoxide (Cimetidine sulphoxide) is a sulfoxide metabolite of Cimetidine. Cimetidine is a histamine H2-receptor antagonist. Cimetidine has the potential for peptic ulcer disease and upper gastrointestinal haemorrhage treatment.
|
-
- HY-13738A
-
|
Raloxifene hydrochloride
Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
|
Estrogen Receptor/ERR
Autophagy
|
Endocrinology
Cancer
|
|
Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
|
-
- HY-108689
-
|
Broflanilide
|
GABA Receptor
|
Neurological Disease
|
|
Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
|
-
- HY-B1019
-
|
Sulpiride
|
Dopamine Receptor
|
Neurological Disease
|
|
Sulpiride is a D2 receptor a antagonist, an atypical antipsychotic drug of the benzamide class, used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression.
|
-
- HY-112359
-
|
C-82
|
β-catenin
Wnt
|
Cancer
|
|
C-82 is a second-generation specific CBP/β-catenin antagonist, which inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.
|
-
- HY-12707
-
-
- HY-B0160
-
-
- HY-13575S1
-
-
- HY-10095A
-
|
Olcegepant hydrochloride
BIBN-4096 hydrochloride; BIBN4096BS hydrochloride
|
CGRP Receptor
|
Neurological Disease
|
|
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
|
-
- HY-P1471
-
-
- HY-112596A
-
-
- HY-P1103
-
|
CTCE-9908
|
CXCR
|
Cancer
|
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
|
-
- HY-133111
-
-
- HY-114244
-
|
USL311
|
CXCR
|
Cancer
Endocrinology
|
|
USL311 is a selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
|
-
- HY-19168
-
|
Perzinfotel
EAA-090
|
iGluR
|
Neurological Disease
|
|
Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC50=30 nM) for the glutamate site.
|
-
- HY-14136
-
-
- HY-14882A
-
-
- HY-P0097A
-
-
- HY-15067
-
|
DNQX
FG 9041
|
iGluR
|
Cancer
|
|
DNQX (FG 9041), a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively).
|
-
- HY-13575S
-
-
- HY-103178
-
|
MRE3008F20
|
Adenosine Receptor
|
Cancer
|
|
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
|
-
- HY-18006
-
