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Assay Detail

CHEMBL872994

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

Binding
Inhibitory activity against HIV-1 Mutant Reverse transcriptase P236L
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous 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 nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.
Klunder JM, Hoermann M, Cywin CL, David E, Brickwood JR, Schwartz R, Barringer KJ, Pauletti D, Shih CK, Erickson DA, Sorge CL, Joseph DP, Hattox SE, Adams J, Grob PM.
J Med Chem (1998) 41 : 2960 -2971
PubMed 9685235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.64 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57 NEVIRAPINE 4.0 1 7.10
CHEMBL100056 1 7.05
CHEMBL102113 1 6.72
CHEMBL100833 1 6.60
CHEMBL321544 1 6.26
CHEMBL102192 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57 NEVIRAPINE IC50 = 80.0 nM 7.10
CHEMBL100056 IC50 = 90.0 nM 7.05
CHEMBL102113 IC50 = 190.0 nM 6.72
CHEMBL100833 IC50 = 250.0 nM 6.60
CHEMBL321544 IC50 = 550.0 nM 6.26
CHEMBL102192 IC50 = 840.0 nM 6.08