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Assay Detail

CHEMBL984537

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

ADMET
Inhibition of CYP2C9
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
Guay D, Boulet L, Friesen RW, Girard M, Hamel P, Huang Z, Laliberté F, Laliberté S, Mancini JA, Muise E, Pon D, Styhler A.
Bioorg Med Chem Lett (2008) 18 : 5554 -5558
PubMed 18835163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.31 4.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485629 MK-0873 2.0 1 4.39
CHEMBL485620 1 4.23
CHEMBL372575 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485629 MK-0873 IC50 = 41000.0 nM 4.39
CHEMBL485620 IC50 = 59000.0 nM 4.23
CHEMBL372575 IC50 <= 1000.0 nM -