Assay Detail

CHEMBL1245535

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Functional

Antiviral activity against Human immunodeficiency virus 1 subtype AE infected in human MT4 cells assessed as reduction in virus induced cytopathicity

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	MT4
Confidence	1 — Organism
Curated By	Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378) ↗

Type	ORGANISM
Organism	Human immunodeficiency virus 1

Publication

TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.

Azijn H, Tirry I, Vingerhoets J, de Béthune MP, Kraus G, Boven K, Jochmans D, Van Craenenbroeck E, Picchio G, Rimsky LT.
Antimicrob Agents Chemother (2010) 54 : 718 -727
PubMed 19933797 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	4	9.05	9.68

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL175691	RILPIVIRINE	4.0	1	9.68
CHEMBL223228	EFAVIRENZ	4.0	1	9.28
CHEMBL308954	ETRAVIRINE	4.0	1	9.19
CHEMBL57	NEVIRAPINE	4.0	1	8.05

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL175691	RILPIVIRINE	EC50	=	0.21	nM	9.68
CHEMBL223228	EFAVIRENZ	EC50	=	0.53	nM	9.28
CHEMBL308954	ETRAVIRINE	EC50	=	0.65	nM	9.19
CHEMBL57	NEVIRAPINE	EC50	=	8.94	nM	8.05