Assay Detail

CHEMBL1262280

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Binding

Displacement of [3H]GSK304649 from Human immunodeficiency virus 1 integrase by scintillation proximity assay

ChEMBL ↗

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Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471) ↗

Open DB target context

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Human immunodeficiency virus type 1 integrase (CHEMBL3471) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Human immunodeficiency virus type 1 integrase

CHEMBL3471

Anchored from Assay target.

Protein identity Human immunodeficiency virus type 1 integrase

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	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

The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.

Garvey EP, Johns BA, Gartland MJ, Foster SA, Miller WH, Ferris RG, Hazen RJ, Underwood MR, Boros EE, Thompson JB, Weatherhead JG, Koble CS, Allen SH, Schaller LT, Sherrill RG, Yoshinaga T, Kobayashi M, Wakasa-Morimoto C, Miki S, Nakahara K, Noshi T, Sato A, Fujiwara T.
Antimicrob Agents Chemother (2008) 52 : 901 -908
PubMed 18160521 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	1	7.58	7.58

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1256978	GSK-364735	2.0	1	7.58

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1256978	GSK-364735	Kd	=	26.0	nM	7.58