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

CHEMBL3266570

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

Functional
Antiviral activity against HIV1 NL4.3 harboring integrase T124/A125 mutant by cell based luciferase reporter gene assay
12
Total Activities
12
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

Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.
Fader LD, Malenfant E, Parisien M, Carson R, Bilodeau F, Landry S, Pesant M, Brochu C, Morin S, Chabot C, Halmos T, Bousquet Y, Bailey MD, Kawai SH, Coulombe R, LaPlante S, Jakalian A, Bhardwaj PK, Wernic D, Schroeder P, Amad M, Edwards P, Garneau M, Duan J, Cordingley M, Bethell R, Mason SW, Bös M, Bonneau P, Poupart MA, Faucher AM, Simoneau B, Fenwick C, Yoakim C, Tsantrizos Y.
ACS Med Chem Lett (2014) 5 : 422 -427
PubMed 24900852 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.09 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3259906 1 7.68
CHEMBL3259902 1 7.66
CHEMBL3259903 1 7.66
CHEMBL3259904 1 7.54
CHEMBL3259896 1 7.16
CHEMBL3259899 1 7.04
CHEMBL3259898 1 6.96
CHEMBL3259900 1 6.92
CHEMBL3259901 1 6.89
CHEMBL3259897 1 6.80
CHEMBL3259905 1 6.52
CHEMBL3259895 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3259906 EC50 = 21.0 nM 7.68
CHEMBL3259902 EC50 = 22.0 nM 7.66
CHEMBL3259903 EC50 = 22.0 nM 7.66
CHEMBL3259904 EC50 = 29.0 nM 7.54
CHEMBL3259896 EC50 = 70.0 nM 7.16
CHEMBL3259899 EC50 = 91.0 nM 7.04
CHEMBL3259898 EC50 = 110.0 nM 6.96
CHEMBL3259900 EC50 = 120.0 nM 6.92
CHEMBL3259901 EC50 = 130.0 nM 6.89
CHEMBL3259897 EC50 = 160.0 nM 6.80
CHEMBL3259905 EC50 = 300.0 nM 6.52
CHEMBL3259895 EC50 = 610.0 nM 6.21