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Assay Detail

CHEMBL897349

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

Binding
Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase
5
Total Activities
5
Compounds Tested
1
Activity Types
0
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 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
Barreca ML, Rao A, De Luca L, Iraci N, Monforte AM, Maga G, De Clercq E, Pannecouque C, Balzarini J, Chimirri A.
Bioorg Med Chem Lett (2007) 17 : 1956 -1960
PubMed 17276064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.29 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 8.40
CHEMBL234401 1 8.30
CHEMBL234400 1 6.82
CHEMBL57 NEVIRAPINE 4.0 1 6.75
CHEMBL393003 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ IC50 = 4.0 nM 8.40
CHEMBL234401 IC50 = 5.0 nM 8.30
CHEMBL234400 IC50 = 150.0 nM 6.82
CHEMBL57 NEVIRAPINE IC50 = 180.0 nM 6.75
CHEMBL393003 IC50 = 700.0 nM 6.16