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Assay Detail

CHEMBL797533

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

Binding
In vitro for inhibition of HIV-1 reverse transcriptase.
16
Total Activities
16
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

Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships and increased metabolic stability of novel substituted pyridine analogs.
Genin MJ, Poel TJ, Yagi Y, Biles C, Althaus I, Keiser BJ, Kopta LA, Friis JM, Reusser F, Adams WJ, Olmsted RA, Voorman RL, Thomas RC, Romero DL.
J Med Chem (1996) 39 : 5267 -5275
PubMed 8978855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.64 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL593 DELAVIRDINE 4.0 1 5.96
CHEMBL149055 1 5.96
CHEMBL151955 1 5.85
CHEMBL356163 1 5.75
CHEMBL151173 1 5.72
CHEMBL151565 1 5.70
CHEMBL358754 1 5.70
CHEMBL356173 1 5.68
CHEMBL424141 1 5.66
CHEMBL124338 1 5.66
CHEMBL151192 1 5.57
CHEMBL338435 1 5.51
CHEMBL147224 1 5.50
CHEMBL151316 1 5.47
CHEMBL148532 1 5.32
CHEMBL280527 ATEVIRDINE MESYLATE 2.0 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL593 DELAVIRDINE IC50 = 1100.0 nM 5.96
CHEMBL149055 IC50 = 1100.0 nM 5.96
CHEMBL151955 IC50 = 1400.0 nM 5.85
CHEMBL356163 IC50 = 1800.0 nM 5.75
CHEMBL151173 IC50 = 1900.0 nM 5.72
CHEMBL151565 IC50 = 2000.0 nM 5.70
CHEMBL358754 IC50 = 2000.0 nM 5.70
CHEMBL356173 IC50 = 2100.0 nM 5.68
CHEMBL424141 IC50 = 2200.0 nM 5.66
CHEMBL124338 IC50 = 2200.0 nM 5.66
CHEMBL151192 IC50 = 2700.0 nM 5.57
CHEMBL338435 IC50 = 3100.0 nM 5.51
CHEMBL147224 IC50 = 3200.0 nM 5.50
CHEMBL151316 IC50 = 3400.0 nM 5.47
CHEMBL148532 IC50 = 4800.0 nM 5.32
CHEMBL280527 ATEVIRDINE MESYLATE IC50 = 5200.0 nM 5.28