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Assay Detail

CHEMBL878537

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

Binding
Inhibitory activity against HIV-1 Reverse transcriptase (RT) was determined
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

The synthesis of a dipyrido[3,2-b:3,4-e][1,4]diazepinone: Convenient access to a C-ring isomer of the HIV-1 reverse transcriptase inhibitor nevirapine
Proudfoot JR
Bioorg Med Chem Lett (1995) 5 : 163 -166
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.22 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57 NEVIRAPINE 4.0 1 7.08
CHEMBL37343 1 6.90
CHEMBL289038 1 6.46
CHEMBL298243 1 5.89
CHEMBL42656 1 5.80
CHEMBL46562 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57 NEVIRAPINE IC50 = 84.0 nM 7.08
CHEMBL37343 IC50 = 125.0 nM 6.90
CHEMBL289038 IC50 = 350.0 nM 6.46
CHEMBL298243 IC50 = 1300.0 nM 5.89
CHEMBL42656 IC50 = 1600.0 nM 5.80
CHEMBL46562 IC50 = 6400.0 nM 5.19