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Assay Detail

CHEMBL800045

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

Binding
Inhibitory effect on HIV-1 RT activity using template primer,poly (rA)-oligo (dT)
8
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Human immunodeficiency virus type 1 protease (CHEMBL243)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
Hanasaki Y, Watanabe H, Katsuura K, Takayama H, Shirakawa S, Yamaguchi K, Sakai S, Ijichi K, Fujiwara M, Konno K.
J Med Chem (1995) 38 : 2038 -2040
PubMed 7540208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.82 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 2 8.22
CHEMBL37624 LOVIRIDE 2.0 2 6.30
CHEMBL62905 2 5.77
CHEMBL62196 1 5.47
CHEMBL60314 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE IC50 = 6.0 nM 8.22
CHEMBL37624 LOVIRIDE IC50 = 500.0 nM 6.30
CHEMBL62905 IC50 = 1700.0 nM 5.77
CHEMBL62196 IC50 = 3400.0 nM 5.47
CHEMBL60314 IC50 = 5800.0 nM 5.24
CHEMBL62905 IC50 = 12000.0 nM 4.92
CHEMBL37624 LOVIRIDE IC50 = 16000.0 nM 4.80
CHEMBL129 ZIDOVUDINE IC50 > 50000.0 nM -