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Assay Detail

CHEMBL2353871

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

Binding
Competitive inhibition of C-Terminal histidine-tagged wild type heterodimeric HIV-1 reverse transcriptase p66/p51 assessed as inhibition of dTTP incorporation after 15 mins by PAGE
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

Bifunctional inhibition of human immunodeficiency virus type 1 reverse transcriptase: mechanism and proof-of-concept as a novel therapeutic design strategy.
Bailey CM, Sullivan TJ, Iyidogan P, Tirado-Rives J, Chung R, Ruiz-Caro J, Mohamed E, Jorgensen WL, Hunter R, Anderson KS.
J Med Chem (2013) 56 : 3959 -3968
PubMed 23659183 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.05 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2348625 1 8.52
CHEMBL72335 1 7.89
CHEMBL2348624 1 6.91
CHEMBL485652 STAVUDINE TRIPHOSPHATE -1.0 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2348625 IC50 = 3.0 nM 8.52
CHEMBL72335 IC50 = 13.0 nM 7.89
CHEMBL2348624 IC50 = 122.0 nM 6.91
CHEMBL485652 STAVUDINE TRIPHOSPHATE IC50 = 13000.0 nM 4.89