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Assay Detail

CHEMBL1074499

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

Binding
Inhibition of HIV1 reverse transcriptase K103N mutant by RNA-dependent DNA polymerase activity assay
12
Total Activities
12
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

Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Monforte AM, Logoteta P, De Luca L, Iraci N, Ferro S, Maga G, De Clercq E, Pannecouque C, Chimirri A.
Bioorg Med Chem (2010) 18 : 1702 -1710
PubMed 20097079 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.65 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 6.70
CHEMBL234401 1 6.40
CHEMBL600615 1 6.05
CHEMBL601219 1 5.58
CHEMBL600411 1 5.55
CHEMBL57 NEVIRAPINE 4.0 1 5.40
CHEMBL603275 1 5.17
CHEMBL592877 1 5.00
CHEMBL601866 1 4.96
CHEMBL601007 1 -
CHEMBL603276 1 -
CHEMBL601867 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ IC50 = 200.0 nM 6.70
CHEMBL234401 IC50 = 400.0 nM 6.40
CHEMBL600615 IC50 = 900.0 nM 6.05
CHEMBL601219 IC50 = 2610.0 nM 5.58
CHEMBL600411 IC50 = 2800.0 nM 5.55
CHEMBL57 NEVIRAPINE IC50 = 4000.0 nM 5.40
CHEMBL603275 IC50 = 6700.0 nM 5.17
CHEMBL592877 IC50 = 10000.0 nM 5.00
CHEMBL601866 IC50 = 10920.0 nM 4.96
CHEMBL601007 IC50 > 40000.0 nM -
CHEMBL603276 IC50 > 40000.0 nM -
CHEMBL601867 IC50 > 40000.0 nM -