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Assay Detail

CHEMBL798996

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

Binding
HIV-1 reverse transcriptase (RT) activity using Poly (rC)/oligo (dG) as template/primer and [3H]dGTP
11
Total Activities
11
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

Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents.
Barreca ML, Balzarini J, Chimirri A, De Clercq E, De Luca L, Höltje HD, Höltje M, Monforte AM, Monforte P, Pannecouque C, Rao A, Zappalà M.
J Med Chem (2002) 45 : 5410 -5413
PubMed 12431069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.99 5.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48427 1 5.65
CHEMBL50019 1 5.55
CHEMBL296589 1 5.54
CHEMBL359315 1 5.54
CHEMBL151152 1 5.38
CHEMBL150025 1 5.38
CHEMBL625 THIABENDAZOLE 4.0 1 4.84
CHEMBL346225 1 4.37
CHEMBL357261 1 4.25
CHEMBL357713 1 4.21
CHEMBL150149 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48427 IC50 = 2240.0 nM 5.65
CHEMBL50019 IC50 = 2840.0 nM 5.55
CHEMBL296589 IC50 = 2900.0 nM 5.54
CHEMBL359315 IC50 = 2850.0 nM 5.54
CHEMBL151152 IC50 = 4120.0 nM 5.38
CHEMBL150025 IC50 = 4120.0 nM 5.38
CHEMBL625 THIABENDAZOLE IC50 = 14600.0 nM 4.84
CHEMBL346225 IC50 = 42400.0 nM 4.37
CHEMBL357261 IC50 = 56600.0 nM 4.25
CHEMBL357713 IC50 = 61400.0 nM 4.21
CHEMBL150149 IC50 = 67000.0 nM 4.17