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Assay Detail

CHEMBL4775184

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Binding
Inhibition of recombinant full length NS3/4A protease in Hepatitis C virus subtype 1b replicon infected in human HuH7 cells preincubated for 3 days followed by substrate addition and measured after 2 hrs by renilla luciferase reporter gene assay
ChEMBL ↗
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 1b
Cell Type Huh-7
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Discovery of BMS-986144, a Third-Generation, Pan-Genotype NS3/4A Protease Inhibitor for the Treatment of Hepatitis C Virus Infection.
Sun LQ,Mull E,D'Andrea S,Zheng B,Hiebert S,Gillis E,Bowsher M,Kandhasamy S,Baratam VR,Puttaswamy S,Pulicharla N,Vishwakrishnan S,Reddy S,Trivedi R,Sinha S,Sivaprasad S,Rao A,Desai S,Ghosh K,Anumula R,Kumar A,Rajamani R,Wang YK,Fang H,Mathur A,Rampulla R,Zvyaga TA,Mosure K,Jenkins S,Falk P,Tagore DM,Chen C,Rendunchintala K,Loy J,Meanwell NA,McPhee F,Scola PM
J Med Chem (2020) 63 : 14740 -14760
PubMed 33226226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 9.21 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4782410 — — 1 9.60
CHEMBL4786865 — — 1 9.52
CHEMBL4799494 — — 1 9.52
CHEMBL4794324 — — 1 9.52
CHEMBL4794931 — — 1 9.40
CHEMBL4776606 — — 1 9.40
CHEMBL4776571 — — 1 9.33
CHEMBL4789428 — — 1 9.32
CHEMBL4783608 — — 1 9.30
CHEMBL4784672 — — 1 9.30
CHEMBL4776577 — — 1 9.22
CHEMBL4779370 — — 1 9.22
CHEMBL4800520 — — 1 9.15
CHEMBL4787795 — — 1 8.96
CHEMBL2105735 ASUNAPREVIR 4.0 1 8.92
CHEMBL4780975 — — 1 8.89
CHEMBL4782586 — — 1 8.82
CHEMBL4798960 — — 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4782410 — EC50 = 0.25 nM 9.60
CHEMBL4786865 — EC50 = 0.3 nM 9.52
CHEMBL4799494 — EC50 = 0.3 nM 9.52
CHEMBL4794324 — EC50 = 0.3 nM 9.52
CHEMBL4794931 — EC50 = 0.4 nM 9.40
CHEMBL4776606 — EC50 = 0.4 nM 9.40
CHEMBL4776571 — EC50 = 0.47 nM 9.33
CHEMBL4789428 — EC50 = 0.48 nM 9.32
CHEMBL4783608 — EC50 = 0.5 nM 9.30
CHEMBL4784672 — EC50 = 0.5 nM 9.30
CHEMBL4776577 — EC50 = 0.6 nM 9.22
CHEMBL4779370 — EC50 = 0.6 nM 9.22
CHEMBL4800520 — EC50 = 0.7 nM 9.15
CHEMBL4787795 — EC50 = 1.1 nM 8.96
CHEMBL2105735 ASUNAPREVIR EC50 = 1.2 nM 8.92
CHEMBL4780975 — EC50 = 1.3 nM 8.89
CHEMBL4782586 — EC50 = 1.5 nM 8.82
CHEMBL4798960 — EC50 = 4.0 nM 8.40