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Assay Detail

CHEMBL797517

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

Binding
In vitro ability to inhibit wild type resistant (WT) reverse transcriptase
5
Total Activities
5
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 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
Genin MJ, Biles C, Keiser BJ, Poppe SM, Swaney SM, Tarpley WG, Yagi Y, Romero DL.
J Med Chem (2000) 43 : 1034 -1040
PubMed 10715167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.96 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL929 DELAVIRDINE MESYLATE 4.0 1 6.58
CHEMBL268871 L-697661 1 6.10
CHEMBL269591 1 5.64
CHEMBL57 NEVIRAPINE 4.0 1 5.51
CHEMBL8971 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL929 DELAVIRDINE MESYLATE IC50 = 260.0 nM 6.58
CHEMBL268871 L-697661 IC50 = 800.0 nM 6.10
CHEMBL269591 IC50 = 2310.0 nM 5.64
CHEMBL57 NEVIRAPINE IC50 = 3100.0 nM 5.51
CHEMBL8971 IC50 > 50000.0 nM -