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

CHEMBL3266567

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

Binding
Binding affinity to HIV1 integrase by displacement assay
9
Total Activities
9
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 Autocuration

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
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
Kd 9 6.88 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3259901 1 7.40
CHEMBL3259897 1 7.32
CHEMBL3259898 1 7.31
CHEMBL3259896 1 7.21
CHEMBL3259899 1 7.17
CHEMBL3259900 1 6.85
CHEMBL3259895 1 6.82
CHEMBL3259894 1 6.55
CHEMBL3259893 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3259901 Kd = 40.0 nM 7.40
CHEMBL3259897 Kd = 48.0 nM 7.32
CHEMBL3259898 Kd = 49.0 nM 7.31
CHEMBL3259896 Kd = 61.0 nM 7.21
CHEMBL3259899 Kd = 68.0 nM 7.17
CHEMBL3259900 Kd = 140.0 nM 6.85
CHEMBL3259895 Kd = 150.0 nM 6.82
CHEMBL3259894 Kd = 280.0 nM 6.55
CHEMBL3259893 Kd = 4700.0 nM 5.33