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Assay Detail

CHEMBL3128634

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiviral activity against Hepatitis C virus genotype 1b Con1 after 4 days by cell-based replicon assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Hepacivirus hominis
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatitis C virus (CHEMBL379)
Type ORGANISM
Organism Hepacivirus hominis

Publication

Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F.
J Med Chem (2014) 57 : 1708 -1729
PubMed 24555570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 48 7.04 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3125124 1 8.70
CHEMBL2403888 1 8.55
CHEMBL414993 1 8.40
CHEMBL3125127 1 8.40
CHEMBL3128332 1 8.05
CHEMBL3125121 1 7.92
CHEMBL3125126 1 7.75
CHEMBL3125106 1 7.72
CHEMBL414994 1 7.70
CHEMBL3125129 1 7.66
CHEMBL3125110 1 7.60
CHEMBL3125108 1 7.60
CHEMBL3125112 1 7.58
CHEMBL3128327 1 7.58
CHEMBL2203631 1 7.54
CHEMBL3125140 1 7.50
CHEMBL3125131 1 7.48
CHEMBL3125109 1 7.40
CHEMBL3128333 1 7.39
CHEMBL3125125 1 7.38
CHEMBL3125105 1 7.30
CHEMBL3128331 1 7.22
CHEMBL3125113 1 7.19
CHEMBL3125119 1 7.17
CHEMBL3125130 1 7.16
CHEMBL3125111 1 7.03
CHEMBL2203630 1 7.01
CHEMBL3125116 1 7.00
CHEMBL3125122 1 7.00
CHEMBL3125120 1 6.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3125124 EC50 = 2.0 nM 8.70
CHEMBL2403888 EC50 = 2.8 nM 8.55
CHEMBL3125127 EC50 = 4.0 nM 8.40
CHEMBL414993 EC50 = 4.0 nM 8.40
CHEMBL3128332 EC50 = 9.0 nM 8.05
CHEMBL3125121 EC50 = 12.0 nM 7.92
CHEMBL3125126 EC50 = 18.0 nM 7.75
CHEMBL3125106 EC50 = 19.0 nM 7.72
CHEMBL414994 EC50 = 20.0 nM 7.70
CHEMBL3125129 EC50 = 22.0 nM 7.66
CHEMBL3125110 EC50 = 25.0 nM 7.60
CHEMBL3125108 EC50 = 25.0 nM 7.60
CHEMBL3128327 EC50 = 26.0 nM 7.58
CHEMBL3125112 EC50 = 26.0 nM 7.58
CHEMBL2203631 EC50 = 29.0 nM 7.54
CHEMBL3125140 EC50 = 32.0 nM 7.50
CHEMBL3125131 EC50 = 33.0 nM 7.48
CHEMBL3125109 EC50 = 40.0 nM 7.40
CHEMBL3128333 EC50 = 41.0 nM 7.39
CHEMBL3125125 EC50 = 42.0 nM 7.38
CHEMBL3125105 EC50 = 50.0 nM 7.30
CHEMBL3128331 EC50 = 60.0 nM 7.22
CHEMBL3125113 EC50 = 64.0 nM 7.19
CHEMBL3125119 EC50 = 67.0 nM 7.17
CHEMBL3125130 EC50 = 70.0 nM 7.16
CHEMBL3125111 EC50 = 94.0 nM 7.03
CHEMBL2203630 EC50 = 97.0 nM 7.01
CHEMBL3125116 EC50 = 100.0 nM 7.00
CHEMBL3125122 EC50 = 100.0 nM 7.00
CHEMBL3125120 EC50 = 117.0 nM 6.93
CHEMBL3125135 EC50 = 133.0 nM 6.88
CHEMBL2203632 EC50 = 170.0 nM 6.77
CHEMBL3125117 EC50 = 209.0 nM 6.68
CHEMBL3125136 EC50 = 210.0 nM 6.68
CHEMBL3128330 EC50 = 268.0 nM 6.57
CHEMBL3128329 EC50 = 267.0 nM 6.57
CHEMBL3125137 EC50 = 437.0 nM 6.36
CHEMBL3125123 EC50 = 500.0 nM 6.30
CHEMBL3125133 EC50 = 550.0 nM 6.26
CHEMBL3125118 EC50 = 586.0 nM 6.23
CHEMBL3125134 EC50 = 600.0 nM 6.22
CHEMBL3125115 EC50 = 833.0 nM 6.08
CHEMBL3125139 EC50 = 860.0 nM 6.07
CHEMBL3125138 EC50 = 893.0 nM 6.05
CHEMBL3125107 EC50 = 966.0 nM 6.01
CHEMBL3125132 EC50 = 2000.0 nM 5.70
CHEMBL3125114 EC50 = 11000.0 nM 4.96
CHEMBL3128328 EC50 = 25000.0 nM 4.60