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Assay Detail

CHEMBL874564

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

Binding
Concentration required to inhibit in vitro RNA-dependent DNA polymerase activity of reverse transcriptase
9
Total Activities
9
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 Expert

Target

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

Publication

Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.
Barreca ML, Rao A, De Luca L, Zappalà M, Monforte AM, Maga G, Pannecouque C, Balzarini J, De Clercq E, Chimirri A, Monforte P.
J Med Chem (2005) 48 : 3433 -3437
PubMed 15857150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.83 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL393003 1 5.54
CHEMBL370921 1 5.28
CHEMBL192976 1 5.12
CHEMBL362924 1 4.90
CHEMBL192499 1 4.79
CHEMBL192310 1 4.70
CHEMBL53554 THIAZOLOBENZIMIDAZOLE 1 4.61
CHEMBL366202 1 4.30
CHEMBL191692 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL393003 IC50 = 2860.0 nM 5.54
CHEMBL370921 IC50 = 5200.0 nM 5.28
CHEMBL192976 IC50 = 7500.0 nM 5.12
CHEMBL362924 IC50 = 12700.0 nM 4.90
CHEMBL192499 IC50 = 16200.0 nM 4.79
CHEMBL192310 IC50 = 20000.0 nM 4.70
CHEMBL53554 THIAZOLOBENZIMIDAZOLE IC50 = 24570.0 nM 4.61
CHEMBL366202 IC50 = 50000.0 nM 4.30
CHEMBL191692 IC50 = 60000.0 nM 4.22