Assay Detail

CHEMBL3266575

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Functional

Antiviral activity against HIV1 NL4.3 harboring integrase A124/T125 mutant by cell based luciferase reporter gene assay

ChEMBL ↗

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Target

Human immunodeficiency virus 1 (CHEMBL378) ↗

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Primary target Human immunodeficiency virus 1

CHEMBL378

Anchored from Assay target.

Protein identity Human immunodeficiency virus 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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	1	7.96	7.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3259907	BI-224436	1.0	1	7.96

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3259907	BI-224436	EC50	=	11.0	nM	7.96