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Assay Detail

CHEMBL834355

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Effective concentration against human immunodeficiency virus type 1 G190S mutant strain
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Intermediate

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
Janssen PA, Lewi PJ, Arnold E, Daeyaert F, de Jonge M, Heeres J, Koymans L, Vinkers M, Guillemont J, Pasquier E, Kukla M, Ludovici D, Andries K, de Béthune MP, Pauwels R, Das K, Clark AD, Frenkel YV, Hughes SH, Medaer B, De Knaep F, Bohets H, De Clerck F, Lampo A, Williams P, Stoffels P.
J Med Chem (2005) 48 : 1901 -1909
PubMed 15771434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.82 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175691 RILPIVIRINE 4.0 1 10.00
CHEMBL70663 DAPIVIRINE 3.0 1 8.70
CHEMBL223228 EFAVIRENZ 4.0 1 6.56
CHEMBL57 NEVIRAPINE 4.0 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175691 RILPIVIRINE EC50 = 0.1 nM 10.00
CHEMBL70663 DAPIVIRINE EC50 = 2.0 nM 8.70
CHEMBL223228 EFAVIRENZ EC50 = 275.0 nM 6.56
CHEMBL57 NEVIRAPINE EC50 = 1000.0 nM 6.00