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Assay Detail

CHEMBL2214224

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Functional
Antiviral activity against HIV1
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Inhibition of HIV-1 capsid assembly: optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold.
Tremblay M, Bonneau P, Bousquet Y, DeRoy P, Duan J, Duplessis M, Gagnon A, Garneau M, Goudreau N, Guse I, Hucke O, Kawai SH, Lemke CT, Mason SW, Simoneau B, Surprenant S, Titolo S, Yoakim C.
Bioorg Med Chem Lett (2012) 22 : 7512 -7517
PubMed 23122820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.03 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203999 1 7.57
CHEMBL2204010 1 7.55
CHEMBL2204009 1 7.21
CHEMBL2204008 1 7.04
CHEMBL2204005 1 6.58
CHEMBL2204004 1 6.58
CHEMBL2204007 1 6.23
CHEMBL2204003 1 6.20
CHEMBL2204014 1 6.19
CHEMBL2204013 1 5.58
CHEMBL2204012 1 5.46
CHEMBL2204015 1 5.46
CHEMBL2204002 1 5.21
CHEMBL2204000 1 5.19
CHEMBL2204001 1 5.00
CHEMBL2204016 1 4.89
CHEMBL2204011 1 4.55
CHEMBL2204006 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203999 EC50 = 27.0 nM 7.57
CHEMBL2204010 EC50 = 28.0 nM 7.55
CHEMBL2204009 EC50 = 62.0 nM 7.21
CHEMBL2204008 EC50 = 91.0 nM 7.04
CHEMBL2204005 EC50 = 260.0 nM 6.58
CHEMBL2204004 EC50 = 260.0 nM 6.58
CHEMBL2204007 EC50 = 590.0 nM 6.23
CHEMBL2204003 EC50 = 630.0 nM 6.20
CHEMBL2204014 EC50 = 640.0 nM 6.19
CHEMBL2204013 EC50 = 2600.0 nM 5.58
CHEMBL2204012 EC50 = 3500.0 nM 5.46
CHEMBL2204015 EC50 = 3500.0 nM 5.46
CHEMBL2204002 EC50 = 6100.0 nM 5.21
CHEMBL2204000 EC50 = 6400.0 nM 5.19
CHEMBL2204001 EC50 = 10000.0 nM 5.00
CHEMBL2204016 EC50 = 13000.0 nM 4.89
CHEMBL2204011 EC50 = 28000.0 nM 4.55
CHEMBL2204006 EC50 > 46000.0 nM -