Assay Detail

CHEMBL1262282

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Functional

Antiviral activity against Human immunodeficiency virus 1 Ba-L infected in human PBMCs assessed as inhibition of viral replication

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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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

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
EC50	4	8.66	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1256978	GSK-364735	2.0	1	8.70
CHEMBL254316	RALTEGRAVIR	4.0	1	8.70
CHEMBL204656	ELVITEGRAVIR	4.0	1	8.70
CHEMBL414850	—	—	1	8.52

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1256978	GSK-364735	EC50	=	2.0	nM	8.70
CHEMBL254316	RALTEGRAVIR	EC50	=	2.0	nM	8.70
CHEMBL204656	ELVITEGRAVIR	EC50	=	2.0	nM	8.70
CHEMBL414850	—	EC50	=	3.0	nM	8.52