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Assay Detail

CHEMBL5117644

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

ADMET
Inhibition of CYP2C9 (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel biphenyl-substituted pyridone derivatives as potent non-nucleoside reverse transcriptase inhibitors with promising oral bioavailability.
Zhao LM, Wang S, Pannecouque C, De Clercq E, Piao HR, Chen FE.
Eur J Med Chem (2022) 240 : 114581 -114581
PubMed 35797898 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.76 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175691 RILPIVIRINE 4.0 1 6.46
CHEMBL782 TOLBUTAMIDE 4.0 1 6.39
CHEMBL5194948 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175691 RILPIVIRINE IC50 = 346.0 nM 6.46
CHEMBL782 TOLBUTAMIDE IC50 = 404.0 nM 6.39
CHEMBL5194948 IC50 = 38300.0 nM 4.42