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Assay Detail

CHEMBL4123649

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

Binding
Inhibition of HIV-1 integrase strand transfer activity assessed as reduction in viral replication in presence of 10% fetal bovine serum
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor.
Naidu BN, Walker MA, Sorenson ME, Ueda Y, Matiskella JD, Connolly TP, Dicker IB, Lin Z, Bollini S, Terry BJ, Higley H, Zheng M, Parker DD, Wu D, Adams S, Krystal MR, Meanwell NA.
Bioorg Med Chem Lett (2018) 28 : 2124 -2130
PubMed 29779976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 8.52 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4127663 1 9.00
CHEMBL4128240 1 9.00
CHEMBL4130102 1 8.70
CHEMBL4130252 1 8.70
CHEMBL4127923 1 8.70
CHEMBL4127891 1 8.70
CHEMBL4126289 1 8.70
CHEMBL4127873 1 8.70
CHEMBL4129717 1 8.70
CHEMBL4126840 1 8.52
CHEMBL4128890 1 8.52
CHEMBL4128924 1 8.52
CHEMBL4126659 1 8.52
CHEMBL4126165 1 8.30
CHEMBL4126686 1 7.68
CHEMBL4128715 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4127663 EC50 = 1.0 nM 9.00
CHEMBL4128240 EC50 = 1.0 nM 9.00
CHEMBL4130102 EC50 = 2.0 nM 8.70
CHEMBL4130252 EC50 = 2.0 nM 8.70
CHEMBL4127923 EC50 = 2.0 nM 8.70
CHEMBL4127891 EC50 = 2.0 nM 8.70
CHEMBL4126289 EC50 = 2.0 nM 8.70
CHEMBL4127873 EC50 = 2.0 nM 8.70
CHEMBL4129717 EC50 = 2.0 nM 8.70
CHEMBL4126840 EC50 = 3.0 nM 8.52
CHEMBL4128890 EC50 = 3.0 nM 8.52
CHEMBL4128924 EC50 = 3.0 nM 8.52
CHEMBL4126659 EC50 = 3.0 nM 8.52
CHEMBL4126165 EC50 = 5.0 nM 8.30
CHEMBL4126686 EC50 = 21.0 nM 7.68
CHEMBL4128715 EC50 = 53.0 nM 7.28