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Assay Detail

CHEMBL5323328

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

ADMET
Inhibition of CYP2C9 (unknown origin)
18
Total Activities
18
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 pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Moore F, Wang W, Zhao G, Mignone J, Meng W, Chu CH, Ma Z, Azzara A, Cullen MJ, Pelleymounter MA, Appiah K, Cvijic ME, Dierks E, Chang S, Foster K, Kopcho L, O'Malley K, Li YX, Khandelwal P, Whaley JM, Mathur A, Hou X, Wu DR, Robl JA, Cheng D, Devasthale P.
Bioorg Med Chem Lett (2023) 91 : 129362 -129362
PubMed 37295614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.28 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5406388 1 6.10
CHEMBL5434664 1 5.72
CHEMBL5411014 1 5.68
CHEMBL5403293 1 5.57
CHEMBL5439792 1 5.22
CHEMBL5401316 1 5.22
CHEMBL5402503 1 5.12
CHEMBL5423898 1 5.03
CHEMBL5408210 1 4.96
CHEMBL5413599 1 4.96
CHEMBL5405560 1 4.92
CHEMBL5411971 1 4.89
CHEMBL5427661 1 -
CHEMBL5435045 1 -
CHEMBL5431177 1 -
CHEMBL5415437 1 -
CHEMBL5434977 1 -
CHEMBL5395875 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5406388 IC50 = 800.0 nM 6.10
CHEMBL5434664 IC50 = 1900.0 nM 5.72
CHEMBL5411014 IC50 = 2100.0 nM 5.68
CHEMBL5403293 IC50 = 2700.0 nM 5.57
CHEMBL5439792 IC50 = 6000.0 nM 5.22
CHEMBL5401316 IC50 = 6000.0 nM 5.22
CHEMBL5402503 IC50 = 7500.0 nM 5.12
CHEMBL5423898 IC50 = 9300.0 nM 5.03
CHEMBL5408210 IC50 = 11000.0 nM 4.96
CHEMBL5413599 IC50 = 11000.0 nM 4.96
CHEMBL5405560 IC50 = 12000.0 nM 4.92
CHEMBL5411971 IC50 = 13000.0 nM 4.89
CHEMBL5427661 IC50 > 20000.0 nM -
CHEMBL5435045 IC50 > 20000.0 nM -
CHEMBL5431177 IC50 > 20000.0 nM -
CHEMBL5415437 IC50 > 6900.0 nM -
CHEMBL5434977 IC50 > 20000.0 nM -
CHEMBL5395875 IC50 > 6700.0 nM -