Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4123648

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

Binding
Inhibition of HIV1 integrase strand transfer activity
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
IC50 16 8.31 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4126686 1 8.70
CHEMBL4126165 1 8.70
CHEMBL4127891 1 8.52
CHEMBL4127663 1 8.52
CHEMBL4126289 1 8.52
CHEMBL4129717 1 8.52
CHEMBL4128240 1 8.40
CHEMBL4127923 1 8.30
CHEMBL4127873 1 8.30
CHEMBL4128890 1 8.22
CHEMBL4126659 1 8.22
CHEMBL4130102 1 8.05
CHEMBL4126840 1 8.00
CHEMBL4128715 1 8.00
CHEMBL4130252 1 7.96
CHEMBL4128924 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4126686 IC50 = 2.0 nM 8.70
CHEMBL4126165 IC50 = 2.0 nM 8.70
CHEMBL4127891 IC50 = 3.0 nM 8.52
CHEMBL4127663 IC50 = 3.0 nM 8.52
CHEMBL4126289 IC50 = 3.0 nM 8.52
CHEMBL4129717 IC50 = 3.0 nM 8.52
CHEMBL4128240 IC50 = 4.0 nM 8.40
CHEMBL4127923 IC50 = 5.0 nM 8.30
CHEMBL4127873 IC50 = 5.0 nM 8.30
CHEMBL4128890 IC50 = 6.0 nM 8.22
CHEMBL4126659 IC50 = 6.0 nM 8.22
CHEMBL4130102 IC50 = 9.0 nM 8.05
CHEMBL4126840 IC50 = 10.0 nM 8.00
CHEMBL4128715 IC50 = 10.0 nM 8.00
CHEMBL4130252 IC50 = 11.0 nM 7.96
CHEMBL4128924 IC50 = 11.0 nM 7.96