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Assay Detail

CHEMBL3297622

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Binding
Apparent binding affinity to Trx-His-tagged HIV integrase
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.
Fader LD, Carson R, Morin S, Bilodeau F, Chabot C, Halmos T, Bailey MD, Kawai SH, Coulombe R, Laplante S, Mekhssian K, Jakalian A, Garneau M, Duan J, Mason SW, Simoneau B, Fenwick C, Tsantrizos Y, Yoakim C.
ACS Med Chem Lett (2014) 5 : 711 -716
PubMed 24944749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 12 7.47 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3287916 1 7.77
CHEMBL3287920 1 7.62
CHEMBL3287922 1 7.58
CHEMBL3287915 1 7.57
CHEMBL3287923 1 7.55
CHEMBL3287913 1 7.51
CHEMBL3287921 1 7.46
CHEMBL3287912 1 7.40
CHEMBL3287924 1 7.40
CHEMBL3287925 1 7.30
CHEMBL3287918 1 7.28
CHEMBL3287917 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3287916 Kd = 17.0 nM 7.77
CHEMBL3287920 Kd = 24.0 nM 7.62
CHEMBL3287922 Kd = 26.0 nM 7.58
CHEMBL3287915 Kd = 27.0 nM 7.57
CHEMBL3287923 Kd = 28.0 nM 7.55
CHEMBL3287913 Kd = 31.0 nM 7.51
CHEMBL3287921 Kd = 35.0 nM 7.46
CHEMBL3287912 Kd = 40.0 nM 7.40
CHEMBL3287924 Kd = 40.0 nM 7.40
CHEMBL3287925 Kd = 50.0 nM 7.30
CHEMBL3287918 Kd = 52.0 nM 7.28
CHEMBL3287917 Kd = 59.0 nM 7.23