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receptor binding site

" in MedChemExpress (MCE) Product Catalog:

200

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4

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1

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7

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24

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6

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22

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100714A
    D-AP5
    25+ Cited Publications

    D-APV; D-2-Amino-5-phosphonovaleric acid

    		 iGluR Neurological Disease
    D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors .
    D-AP5
  • HY-15084B
    Dizocilpine
    Maximum Cited Publications
    44 Publications Verification

    MK-801

    		 iGluR Neurological Disease
    Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
    Dizocilpine
  • HY-102064
    SR 57227A
    1 Publications Verification

    		 5-HT Receptor Neurological Disease
    SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .
    SR 57227A
  • HY-100815B
    (RS)-AMPA

    (±)-AMPA

    		 iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA
  • HY-15419
    RS-127445 hydrochloride
    3 Publications Verification

    		 5-HT Receptor Neurological Disease
    RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
    RS-127445 hydrochloride
  • HY-122422
    Gepirone

    		5-HT Receptor Others
    Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .
    Gepirone
  • HY-I0096
    Indole-2-carboxylic acid

    		iGluR HIV HIV Integrase Neurological Disease
    Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (Ki=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg 2+ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection .
    Indole-2-carboxylic acid
  • HY-18698
    L-701324

    		iGluR Neurological Disease
    L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
    L-701324
  • HY-P0185
    Endomorphin 1
    3 Publications Verification

    		 Opioid Receptor Neurological Disease
    Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
    Endomorphin 1
  • HY-107701
    CGP 78608 hydrochloride

    		iGluR Neurological Disease
    CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 hydrochloride acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity .
    CGP 78608 hydrochloride
  • HY-B0115
    Pizotifen
    2 Publications Verification

    Pizotyline; BC-105

    		 5-HT Receptor Neurological Disease
    Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen
  • HY-B0429
    Pancuronium dibromide

    		nAChR Neurological Disease
    Pancuronium dibromide, a bis-quaternary steroid, is a neuromuscular relaxant. Pancuronium dibromide inhibits neuromuscular transmission by competing with acetylcholine for binding sites on nACh receptors. Pancuronium dibromide also inhibits cardiac muscarinic receptors and has a sympathomimetic action .
    Pancuronium dibromide
  • HY-101176
    2-Iodomelatonin
    2 Publications Verification

    		 Melatonin Receptor Cancer
    2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
    2-Iodomelatonin
  • HY-14336A
    SB 271046 Hydrochloride

    SB 271046A

    		 5-HT Receptor Neurological Disease
    SB 271046 Hydrochloride (SB 271046A) is a potent, selective, orally active and BBB-permeable 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM) .
    SB 271046 Hydrochloride
  • HY-P1741
    Fibrinogen-Binding Peptide
    1 Publications Verification

    		 Thrombin Cardiovascular Disease
    Fibrinogen-Binding Peptide (designed by anticomplementarity hypothesis) is a presumptive peptide mimic of the vitronectin binding site on the fibrinogen receptor. Fibrinogen-Binding Peptide binds fibrinogen and inhibits both the adhesion of platelets to fibrinogen and platelet aggregation, and also inhibits the adhesion of platelets to vitronectin .
    Fibrinogen-Binding Peptide
  • HY-101178
    L-689560

    		iGluR Neurological Disease
    L-689560 is a potent N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site. L-689560 is widely used as a radiolabeled ligand in binding studies and used for study the roles of NMDA receptors in normal neurological processes as well as in diseases .
    L-689560
  • HY-B0115A
    Pizotifen malate
    2 Publications Verification

    Pizotyline malate; BC-105 malate

    		 5-HT Receptor Neurological Disease
    Pizotifen malate (Pizotyline malate) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen malate
  • HY-15419A
    RS-127445
    3 Publications Verification

    		 5-HT Receptor Neurological Disease
    RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
    RS-127445
  • HY-136299
    Sepimostat
    2 Publications Verification

    FUT-187 free base

    		 iGluR Neurological Disease
    Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7?μM .
    Sepimostat
  • HY-P1077
    CALP1
    3 Publications Verification

    		 mGluR Phosphodiesterase (PDE) Apoptosis Calmodulin Inflammation/Immunology
    CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity .
    CALP1
  • HY-119437
    FLTX1
    2 Publications Verification

    		 Estrogen Receptor/ERR Cancer
    FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus .
    FLTX1
  • HY-D0871
    CHES

    N-Cyclohexyltaurine

    		 Biochemical Assay Reagents Influenza Virus Infection
    CHES (N-Cyclohexyltaurine) is a biological buffer reagent that binds to influenza virus hemagglutinin (HA). CHES mimics the binding mode of sialic acid to the HA receptor-binding site .
    CHES
  • HY-P0186A
    Endomorphin 2 TFA

    		Opioid Receptor Neurological Disease
    Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
    Endomorphin 2 TFA
  • HY-15404
    Darusentan

    Lu-135252

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM .
    Darusentan
  • HY-P1077A
    CALP1 TFA
    3 Publications Verification

    		 mGluR Phosphodiesterase (PDE) Apoptosis Calmodulin Inflammation/Immunology
    CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity .
    CALP1 TFA
  • HY-122537A
    Arotinolol
    2 Publications Verification

    		 Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites . Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .
    Arotinolol
  • HY-110160
    Pozanicline dihydrochloride

    ABT-089 dihydrochloride

    		 nAChR Neurological Disease
    Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites . Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant .
    Pozanicline dihydrochloride
  • HY-W741573
    N-Biotinyl p-aminophenyl arsenic acid

    		nAChR Neurological Disease
    N-Biotinyl p-aminophenyl arsenic acid is a bifunctional reagent that can bind to both streptavidin and dithiols. N-Biotinyl p-aminophenyl arsenic acid decreases the Rbungarotoxin-binding sites in reduced Torpedo nicotinic receptors (IC50 is 10-300 nM), and protects the receptor from irreversible alkylation by bromoacetylcholine .
    N-Biotinyl p-aminophenyl arsenic acid
  • HY-P991246
    VRC01LS

    		Virus Protease HIV Infection
    VRC01LS is a humanized monoclonal antibody inhibitor targeting the CD4-binding site of HIV-1 envelope glycoprotein (Env). VRC01LS blocks the binding of HIV-1 to host cell CD4 receptor, inhibiting viral entry. VRC01LS is promising for research of HIV-1 infection .
    VRC01LS
  • HY-136280
    Panamesine

    EMD 57445

    		 Sigma Receptor Neurological Disease
    Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
    Panamesine
  • HY-59384
    MOMBA

    		Free Fatty Acid Receptor Metabolic Disease Inflammation/Immunology
    MOMBA is a selective FFA2 (Free Fatty Acid Receptor 2) orthosteric agonist that activates receptor signaling pathways by binding to the orthosteric site of FFA2 with high specificity. MOMBA holds potential for research on metabolic and inflammatory diseases .
    MOMBA
  • HY-15419R
    RS-127445 hydrochloride (Standard)

    		5-HT Receptor Neurological Disease
    RS-127445 (hydrochloride) (Standard) is the analytical standard of RS-127445 (hydrochloride). This product is intended for research and analytical applications. RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
    RS-127445 hydrochloride (Standard)
  • HY-106969A
    ZD 9379 sodium

    		Glycine Receptor (GlyR) iGluR Cardiovascular Disease Neurological Disease
    ZD 9379 sodium is a competitive glycine/NMDA receptor antagonist, with an IC50 value of 75 nM (glutamate site). ZD 9379 sodium selectively antagonizes the glycine binding site (GlyB site) on the NMDA receptor, inhibiting the binding of glycine to the NMDA receptor and alleviating excitotoxicity. ZD 9379 sodium reduces the frequency of cortical spreading depression (SDs), alleviates energy depletion in the ischemic penumbra, and delays the expansion of infarction. ZD 9379 sodium reduces the infarct volume and improves neurological function in mouse models. ZD 9379 sodium can be used in studies of acute ischemic stroke, etc .
    ZD 9379 sodium
  • HY-P1741A
    Fibrinogen-Binding Peptide TFA
    1 Publications Verification

    		 Integrin Cardiovascular Disease
    Fibrinogen-Binding Peptide TFA (designed by anticomplementarity hypothesis) is a presumptive peptide mimic of the vitronectin binding site on the fibrinogen receptor. Fibrinogen-Binding Peptide TFA binds fibrinogen and inhibits both the adhesion of platelets to fibrinogen and platelet aggregation, and also inhibits the adhesion of platelets to vitronectin .
    Fibrinogen-Binding Peptide TFA
  • HY-121082
    (-)-Dihydroalprenolol

    L-Dihydroalprenolol

    		 Adrenergic Receptor Endocrinology
    (-)-Dihydroalprenolol (L-Dihydroalprenolol) is a β-adrenergic antagonist that inhibits the activity of β-adrenergic receptors. (-)-Dihydroalprenolol can cause desensitization of approximately 60% of β-adrenergic receptor binding sites. (-)-Dihydroalprenolol has also been shown to reduce the binding capacity of specific β-adrenergic ligands. (-)-Dihydroalprenolol may affect the ability to stimulate membrane-bound adenylate acylase .
    (-)-Dihydroalprenolol
  • HY-157712
    08:0 PI(4,5)P2 ammonium

    		Biochemical Assay Reagents Others
    08:0 PI(4,5)P2 ammonium is suitable for identifying its binding site at the transient receptor potential vanilloid 4 (TRPV 4 N) terminus .
    08:0 PI(4,5)P2 ammonium
  • HY-P0186
    Endomorphin 2

    		Opioid Receptor Neurological Disease
    Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
    Endomorphin 2
  • HY-100815C
    (RS)-AMPA hydrobromide

    (±)-AMPA hydrobromide

    		 iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) hydrobromide is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA hydrobromide
  • HY-136299A
    Sepimostat dimethanesulfonate

    FUT-187

    		 iGluR Neurological Disease
    Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM .
    Sepimostat dimethanesulfonate
  • HY-10050
    CJ-17493

    		Neurokinin Receptor Neurological Disease
    CJ-17493 is a neurokinin-1 (NK1) receptor antagonist, with a Ki of 0.2 nM. CJ-17493 shows moderate affinity for the verapamil-binding site of L-type Ca 2+ channels (IC50 = 164 nM) and site 2 of sodium channels (IC50 = 48 nM). CJ-17493 can be used for the study of neurological diseases .
    CJ-17493
  • HY-108507
    MRT-10

    		Smo Cancer
    MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer .
    MRT-10
  • HY-P0185A
    Endomorphin 1 acetate
    3 Publications Verification

    		 Opioid Receptor Neurological Disease
    Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
    Endomorphin 1 acetate
  • HY-122422A
    Gepirone hydrochloride

    		5-HT Receptor Neurological Disease
    Gepirone is a selective 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .
    Gepirone hydrochloride
  • HY-129517
    UBP714

    		iGluR Neurological Disease
    UBP714 exhibts agonistic activity for recombinant GluN1/GluN2 receptor by binding to the positive allosteric site (PAM) of NMDARs. UBP714 enhances NMDAR-mediated field excitatory postsynaptic potentials (f-EPSPs) in Xenopus oocytes .
    UBP714
  • HY-122537
    Arotinolol hydrochloride

    		Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol hydrochloride also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites . Arotinolol hydrochloride is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .
    Arotinolol hydrochloride
  • HY-101344
    Cyanopindolol fumarate

    		5-HT Receptor Neurological Disease
    Cyanopindolol fumarate is a 5-HT receptor antagonist .
    Cyanopindolol fumarate
  • HY-162659
    β2AR ligand 1

    		Adrenergic Receptor Others
    β2AR ligand 1 (Compound 4) is a homobivalent bitopic ligand for β2 adrenergic receptor (β2AR) on the orthosteric binding site (OBS) and the metastable binding sites (MBS) .
    β2AR ligand 1
  • HY-120524
    CGP 31358

    		iGluR Neurological Disease
    CGP 31358 is an anticonvulsant agent that binds to a site on the NMDA receptor complex that is coupled to both the transmitter recognition site and to the channel domain. CGP 31358 inhibits the binding of L-Glutamate to the NMDA receptor complex with an IC50 of 53 μM .
    CGP 31358
  • HY-100143
    Pentiapine

    CGS 10746

    		 Dopamine Receptor Neurological Disease
    Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites .
    Pentiapine
  • HY-120020
    LY-395153

    		iGluR Others
    LY-395153 is an AMPA receptor enhancer with the activity of binding to AMPA receptors. LY-395153 can bind to natural and recombinant AMPA receptors, and its binding is affected by AMPA receptor agonists and can be competitively or non-competitively inhibited by some compounds. It is a useful probe for marking unique regulatory sites of AMPA receptors.
    LY-395153

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