Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3362715

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

Binding
Inhibition of wild type HIV1 reverse transcriptase M184V mutant assessed as inhibition of DNA primer extension using [8-3H(N)]-dATP by scintillation proximity assay
4
Total Activities
4
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

Modular assembly of purine-like bisphosphonates as inhibitors of HIV-1 reverse transcriptase.
Lacbay CM, Mancuso J, Lin YS, Bennett N, Götte M, Tsantrizos YS.
J Med Chem (2014) 57 : 7435 -7449
PubMed 25144111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.89 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3327156 1 6.22
CHEMBL666 FOSCARNET 4.0 1 6.10
CHEMBL3327153 1 5.85
CHEMBL3327158 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3327156 IC50 = 600.0 nM 6.22
CHEMBL666 FOSCARNET IC50 = 800.0 nM 6.10
CHEMBL3327153 IC50 = 1400.0 nM 5.85
CHEMBL3327158 IC50 = 4200.0 nM 5.38