Assay Detail

CHEMBL1693526

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Functional

Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT 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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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Human immunodeficiency virus 1
Cell Type	HeLa-T4
Confidence	1 — Organism
Curated By	Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378) ↗

Type	ORGANISM
Organism	Human immunodeficiency virus 1

Publication

Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.

Koh Y, Haim H, Engelman A.
Antimicrob Agents Chemother (2011) 55 : 42 -49
PubMed 21060108 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	6	7.89	8.96
EC95	6	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL223228	EFAVIRENZ	4.0	2	8.96
CHEMBL1486	TENOFOVIR DISOPROXIL FUMARATE	4.0	2	8.54
CHEMBL129	ZIDOVUDINE	4.0	2	8.08
CHEMBL204656	ELVITEGRAVIR	4.0	2	7.52
CHEMBL57	NEVIRAPINE	4.0	2	7.14
CHEMBL254316	RALTEGRAVIR	4.0	2	7.11

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL223228	EFAVIRENZ	EC50	=	1.1	nM	8.96
CHEMBL1486	TENOFOVIR DISOPROXIL FUMARATE	EC50	=	2.9	nM	8.54
CHEMBL129	ZIDOVUDINE	EC50	=	8.4	nM	8.08
CHEMBL204656	ELVITEGRAVIR	EC50	=	30.0	nM	7.52
CHEMBL57	NEVIRAPINE	EC50	=	73.0	nM	7.14
CHEMBL254316	RALTEGRAVIR	EC50	=	77.0	nM	7.11
CHEMBL223228	EFAVIRENZ	EC95	=	0.008	uM	-
CHEMBL1486	TENOFOVIR DISOPROXIL FUMARATE	EC95	=	0.037	uM	-
CHEMBL129	ZIDOVUDINE	EC95	=	0.09	uM	-
CHEMBL204656	ELVITEGRAVIR	EC95	=	0.5	uM	-
CHEMBL57	NEVIRAPINE	EC95	=	0.68	uM	-
CHEMBL254316	RALTEGRAVIR	EC95	=	0.81	uM	-