GSK5852
GSK5852 (GSK2485852) is an HCV NS5B polymerase inhibitor, with an IC50 value of 50 nM. GSK5852 displays antiviral activity and inhibits HCV with EC50s of 3.0 nM (genotype 1a, GT1a) and 1.7 nM (GT1b), respectively.
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- CAS No.: 1331942-30-3
- Formule: C27H25BF2N2O6S
- Masse moléculaire:554.37
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Target: 50 nM (NS5B, HCV)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | EC50 |
1.4 nM
Compound: 3, GSK5852
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Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316Y mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316Y mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
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[PMID: 23672667] |
| Huh-7 | EC50 |
1.7 nM
Compound: 3, GSK5852
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Antiviral activity against wild type Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
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[PMID: 23672667] |
| Huh-7 | EC50 |
1.9 nM
Compound: 3, GSK5852
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Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316N mutant infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316N mutant infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
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[PMID: 23672667] |
| Huh-7 | EC50 |
3 nM
Compound: 3, GSK5852
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Antiviral activity against wild type Hepatitis C virus genotype 1a infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1a infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
|
[PMID: 23672667] |
| Huh-7 | EC50 |
3.2 nM
Compound: 3, GSK5852
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Antiviral activity against wild type Hepatitis C virus genotype 1a harboring C316Y mutant infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1a harboring C316Y mutant infected in human HuH7 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
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[PMID: 23672667] |
| Huh-7 | EC50 |
3.8 nM
Compound: 3, GSK5852
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Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316F mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring C316F mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
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[PMID: 23672667] |
| Huh-7 | EC50 |
4.2 nM
Compound: 3, GSK5852
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Antiviral activity against wild type Hepatitis C virus genotype 1b harboring S365T mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
Antiviral activity against wild type Hepatitis C virus genotype 1b harboring S365T mutant infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by Bright-glo luciferase reporter gene assay
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[PMID: 23672667] |
Nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp) is a component of HCV, for researching HCV infection-related diseases[1].
GSK5852 (compound 87) inhibits aggregation by two mechanisms: 1) stabilizing β-flap in a closed inactive state to inhibit the initiation step of the RdRp RNA replication cycle; 2) disruption of RNA processing channels through direct spatial contact[1].
GSK5852 is a non-nucleoside NS5B inhibitor and exhibits inhibitory effect on HCV mutant variants with EC50s of 3.2 nM (GT1a C316Y), 1.9 nM (GT1b C316N), respectively[1].
GSK5852 displays an excellent resistance profile and shows a <5-fold potency loss across the clinically important NS5B resistance mutations[2].
GSK5852 shows no cross-resistance against known resistance mutations in NS5B[2].
GSK5852 (compound 3) (0-10 μM) blocks the initiation step of NS5B polymerase cycle[3].
GSK5852 (0.6, 10 μM; 0-75 h) shows slow binding kinetics with isolated GT1b 316N protein, and with a dissociation half-life of >40 hours[3].
GSK5852 (0.6, 10 μM; 15 min) inhibits NS5B∆21 1b 316N with an IC50 value of 130 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCV NS5B
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Concentration:0, 0.016, 0.08, 0.4, 2, 10 μM
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Incubation Time:
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Result:Resulted migration of CTP substrate (at 10 μM), decreased pCpG reaction product with increasing concentrations and significantly decreased at a dosage >2 μM.
Indicated blocking NS5B initiation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1331942-30-3
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Masse moléculaire 554.37
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Formule C27H25BF2N2O6S
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SMILES
FC1=CC(CN(C2=CC3=C(C=C2C4CC4)C(C(NC)=O)=C(C5=CC=C(C=C5)F)O3)S(C)(=O)=O)=CC=C1B(O)O
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Synonyms
GSK2485852
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Zhou Z, et al. Small molecule NS5B RdRp non-nucleoside inhibitors for the treatment of HCV infection: A medicinal chemistry perspective. Eur J Med Chem. 2022 Jul 8. 240:114595. [Content Brief]
[2]. Voitenleitner C, et al. In vitro characterization of GSK2485852, a novel hepatitis C virus polymerase inhibitor. Antimicrob Agents Chemother. 2013 Nov;57(11):5216-24. [Content Brief]
[3]. Maynard A, et al. Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase. J Med Chem. 2014 Mar 13;57(5):1902-13. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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