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Assay Detail

CHEMBL802594

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

Binding
Inhibitory activity against HIV-1 Mutant Reverse transcriptase V106A
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

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. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones.
Cywin CL, Klunder JM, Hoermann M, Brickwood JR, David E, Grob PM, Schwartz R, Pauletti D, Barringer KJ, Shih CK, Sorge CL, Erickson DA, Joseph DP, Hattox SE.
J Med Chem (1998) 41 : 2972 -2984
PubMed 9685236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.06 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319277 1 8.00
CHEMBL102166 1 8.00
CHEMBL321544 1 7.52
CHEMBL103386 1 7.40
CHEMBL102034 1 7.30
CHEMBL102192 1 6.92
CHEMBL99624 1 6.92
CHEMBL320663 1 6.10
CHEMBL57 NEVIRAPINE 4.0 1 5.41
CHEMBL99793 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319277 IC50 = 10.0 nM 8.00
CHEMBL102166 IC50 = 10.0 nM 8.00
CHEMBL321544 IC50 = 30.0 nM 7.52
CHEMBL103386 IC50 = 40.0 nM 7.40
CHEMBL102034 IC50 = 50.0 nM 7.30
CHEMBL102192 IC50 = 120.0 nM 6.92
CHEMBL99624 IC50 = 120.0 nM 6.92
CHEMBL320663 IC50 = 800.0 nM 6.10
CHEMBL57 NEVIRAPINE IC50 = 3930.0 nM 5.41
CHEMBL99793 IC50 = - nM -