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Assay Detail

CHEMBL1039956

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Binding
Inhibition of HIV1 JRFL gp120/CD4 interaction in human HeLa67 cells assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HeLa67
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug candidate that demonstrates antiviral activity in HIV-1-infected subjects.
Wang T, Yin Z, Zhang Z, Bender JA, Yang Z, Johnson G, Yang Z, Zadjura LM, D'Arienzo CJ, DiGiugno Parker D, Gesenberg C, Yamanaka GA, Gong YF, Ho HT, Fang H, Zhou N, McAuliffe BV, Eggers BJ, Fan L, Nowicka-Sans B, Dicker IB, Gao Q, Colonno RJ, Lin PF, Meanwell NA, Kadow JF.
J Med Chem (2009) 52 : 7778 -7787
PubMed 19769332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.25 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL238103 1 9.06
CHEMBL337301 1 8.83
CHEMBL585487 1 8.80
CHEMBL442078 1 8.77
CHEMBL567570 1 8.40
CHEMBL583867 1 7.67
CHEMBL585498 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL238103 EC50 = 0.88 nM 9.06
CHEMBL337301 EC50 = 1.47 nM 8.83
CHEMBL585487 EC50 = 1.6 nM 8.80
CHEMBL442078 EC50 = 1.7 nM 8.77
CHEMBL567570 EC50 = 4.0 nM 8.40
CHEMBL583867 EC50 = 21.6 nM 7.67
CHEMBL585498 EC50 = 575.9 nM 6.24