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Assay Detail

CHEMBL4046663

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

Functional
Antiviral activity against HCV genotype 1b Con1 expressing NS3 protease infected in human Huh-7 cells assessed as reduction in viral RNA replication after 72 hrs by luciferase reporter gene assay
42
Total Activities
42
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

The discovery of IDX21437: Design, synthesis and antiviral evaluation of 2'-α-chloro-2'-β-C-methyl branched uridine pronucleotides as potent liver-targeted HCV polymerase inhibitors.
Alexandre FR, Badaroux E, Bilello JP, Bot S, Bouisset T, Brandt G, Cappelle S, Chapron C, Chaves D, Convard T, Counor C, Da Costa D, Dukhan D, Gay M, Gosselin G, Griffon JF, Gupta K, Hernandez-Santiago B, La Colla M, Lioure MP, Milhau J, Paparin JL, Peyronnet J, Parsy C, Pierra Rouvière C, Rahali H, Rahali R, Salanson A, Seifer M, Serra I, Standring D, Surleraux D, Dousson CB.
Bioorg Med Chem Lett (2017) 27 : 4323 -4330
PubMed 28835346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 5.71 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061885 1 7.15
CHEMBL4061368 1 7.14
CHEMBL4084420 1 6.80
CHEMBL4082078 1 6.73
CHEMBL3793161 1 6.69
CHEMBL4098752 1 6.61
CHEMBL4100083 1 6.59
CHEMBL1259059 SOFOSBUVIR 4.0 1 6.55
CHEMBL4070509 1 6.54
CHEMBL4072765 1 6.46
CHEMBL4066255 1 6.38
CHEMBL4070281 1 6.29
CHEMBL4084595 1 6.28
CHEMBL4072334 1 6.09
CHEMBL4071553 1 6.07
CHEMBL4091302 1 6.02
CHEMBL4070366 1 5.96
CHEMBL4099034 1 5.94
CHEMBL4088893 1 5.90
CHEMBL1259058 1 5.68
CHEMBL4093100 1 5.66
CHEMBL4089948 1 5.60
CHEMBL4082826 1 5.59
CHEMBL4096581 1 5.44
CHEMBL4060667 1 5.40
CHEMBL4070042 1 5.40
CHEMBL4100808 1 5.37
CHEMBL4075092 1 5.09
CHEMBL4092334 1 5.02
CHEMBL4063741 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061885 EC50 = 71.0 nM 7.15
CHEMBL4061368 EC50 = 73.0 nM 7.14
CHEMBL4084420 EC50 = 158.0 nM 6.80
CHEMBL4082078 EC50 = 185.0 nM 6.73
CHEMBL3793161 EC50 = 203.0 nM 6.69
CHEMBL4098752 EC50 = 248.0 nM 6.61
CHEMBL4100083 EC50 = 257.0 nM 6.59
CHEMBL1259059 SOFOSBUVIR EC50 = 284.0 nM 6.55
CHEMBL4070509 EC50 = 291.0 nM 6.54
CHEMBL4072765 EC50 = 351.0 nM 6.46
CHEMBL4066255 EC50 = 417.0 nM 6.38
CHEMBL4070281 EC50 = 508.0 nM 6.29
CHEMBL4084595 EC50 = 528.0 nM 6.28
CHEMBL4072334 EC50 = 819.0 nM 6.09
CHEMBL4071553 EC50 = 845.0 nM 6.07
CHEMBL4091302 EC50 = 953.0 nM 6.02
CHEMBL4070366 EC50 = 1108.0 nM 5.96
CHEMBL4099034 EC50 = 1159.0 nM 5.94
CHEMBL4088893 EC50 = 1269.0 nM 5.90
CHEMBL1259058 EC50 = 2080.0 nM 5.68
CHEMBL4093100 EC50 = 2180.0 nM 5.66
CHEMBL4089948 EC50 = 2486.0 nM 5.60
CHEMBL4082826 EC50 = 2548.0 nM 5.59
CHEMBL4096581 EC50 = 3610.0 nM 5.44
CHEMBL4060667 EC50 = 3990.0 nM 5.40
CHEMBL4070042 EC50 = 4022.0 nM 5.40
CHEMBL4100808 EC50 = 4283.0 nM 5.37
CHEMBL4075092 EC50 = 8136.0 nM 5.09
CHEMBL4092334 EC50 = 9600.0 nM 5.02
CHEMBL4063741 EC50 = 12030.0 nM 4.92
CHEMBL4103415 EC50 = 12596.0 nM 4.90
CHEMBL2031681 EC50 = 30000.0 nM 4.52
CHEMBL4091014 EC50 = 31834.0 nM 4.50
CHEMBL4085344 EC50 = 37400.0 nM 4.43
CHEMBL4080706 EC50 = 42299.0 nM 4.37
CHEMBL510394 EC50 = 50000.0 nM 4.30
CHEMBL3833371 UPRIFOSBUVIR EC50 = 56800.0 nM 4.25
CHEMBL4059905 EC50 = 57000.0 nM 4.24
CHEMBL4104180 EC50 > 100000.0 nM -
CHEMBL4101761 EC50 > 100000.0 nM -
CHEMBL4085484 EC50 > 100000.0 nM -
CHEMBL4097676 EC50 > 100000.0 nM -