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Assay Detail

CHEMBL3266569

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

Functional
Antiviral activity against HIV1 HxB2 harboring integrase A124/T125 mutant by cell based luciferase reporter gene assay
23
Total Activities
23
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 23 6.87 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3259903 1 8.70
CHEMBL3259906 1 8.22
CHEMBL3259902 1 8.15
CHEMBL3259907 BI-224436 1.0 1 7.96
CHEMBL3259901 1 7.89
CHEMBL3259898 1 7.64
CHEMBL3259899 1 7.58
CHEMBL3259897 1 7.57
CHEMBL3259896 1 7.55
CHEMBL3259900 1 7.51
CHEMBL3259905 1 7.47
CHEMBL3259895 1 7.11
CHEMBL3259894 1 6.89
CHEMBL3259893 1 6.35
CHEMBL3259890 1 6.04
CHEMBL3259891 1 6.00
CHEMBL3259889 1 4.89
CHEMBL3259887 1 4.80
CHEMBL3259886 1 4.70
CHEMBL3259892 1 4.33
CHEMBL1422607 1 -
CHEMBL3259888 1 -
CHEMBL3259885 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3259903 EC50 = 2.0 nM 8.70
CHEMBL3259906 EC50 = 6.0 nM 8.22
CHEMBL3259902 EC50 = 7.0 nM 8.15
CHEMBL3259907 BI-224436 EC50 = 11.0 nM 7.96
CHEMBL3259901 EC50 = 13.0 nM 7.89
CHEMBL3259898 EC50 = 23.0 nM 7.64
CHEMBL3259899 EC50 = 26.0 nM 7.58
CHEMBL3259897 EC50 = 27.0 nM 7.57
CHEMBL3259896 EC50 = 28.0 nM 7.55
CHEMBL3259900 EC50 = 31.0 nM 7.51
CHEMBL3259905 EC50 = 34.0 nM 7.47
CHEMBL3259895 EC50 = 78.0 nM 7.11
CHEMBL3259894 EC50 = 130.0 nM 6.89
CHEMBL3259893 EC50 = 450.0 nM 6.35
CHEMBL3259890 EC50 = 920.0 nM 6.04
CHEMBL3259891 EC50 = 990.0 nM 6.00
CHEMBL3259889 EC50 = 13000.0 nM 4.89
CHEMBL3259887 EC50 = 16000.0 nM 4.80
CHEMBL3259886 EC50 = 20000.0 nM 4.70
CHEMBL3259892 EC50 = 47000.0 nM 4.33
CHEMBL1422607 EC50 > 40000.0 nM -
CHEMBL3259888 EC50 > 43000.0 nM -
CHEMBL3259885 EC50 > 33000.0 nM -