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Assay Detail

CHEMBL5548164

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

Binding
Inhibition of wild type HIV-1 Reverse transcriptase assessed as reduction of biotin-dUTP incorporation into protein using ABTS as substrate preincubated with compound for 1 hr followed by substrate addition in presence of biotin-labeled dNTPs by ELISA analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Discovery of Novel Aryl Triazolone Dihydropyridines (ATDPs) Targeting Highly Conserved Residue W229 as Promising HIV-1 NNRTIs.
Sun Y, Zhou Z, Wang N, Zhao F, Liu Y, Xu X, Wang X, Gou Z, De Clercq E, Pannecouque C, Zhan P, Kang D, Liu X.
J Med Chem (2024) 67 : 6570 -6584
PubMed 38613773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.45 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5593560 1 7.70
CHEMBL5575200 1 7.52
CHEMBL5571067 1 7.52
CHEMBL5573421 1 7.52
CHEMBL5573653 1 7.40
CHEMBL5564750 1 7.40
CHEMBL5575003 1 7.40
CHEMBL5563055 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5593560 IC50 = 20.0 nM 7.70
CHEMBL5575200 IC50 = 30.0 nM 7.52
CHEMBL5571067 IC50 = 30.0 nM 7.52
CHEMBL5573421 IC50 = 30.0 nM 7.52
CHEMBL5573653 IC50 = 40.0 nM 7.40
CHEMBL5564750 IC50 = 40.0 nM 7.40
CHEMBL5575003 IC50 = 40.0 nM 7.40
CHEMBL5563055 IC50 = 80.0 nM 7.10