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Assay Detail

CHEMBL5138359

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

Binding
Inhibition of HIV-1 reverse transcriptase K103N mutant assessed as reduction in luciferase reporter activity by single-round assay
3
Total Activities
3
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

Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
Wang Z, Cherukupalli S, Xie M, Wang W, Jiang X, Jia R, Pannecouque C, De Clercq E, Kang D, Zhan P, Liu X.
J Med Chem (2022) 65 : 3729 -3757
PubMed 35175760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 9.10 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175691 RILPIVIRINE 4.0 1 9.70
CHEMBL5187795 1 9.40
CHEMBL5206708 1 8.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175691 RILPIVIRINE EC50 = 0.2 nM 9.70
CHEMBL5187795 EC50 = 0.4 nM 9.40
CHEMBL5206708 EC50 = 6.5 nM 8.19