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Assay Detail

CHEMBL4676226

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

ADMET
Inhibition of CYP2C8 in human liver microsomes using amodiaquine as substrate by LC-MS/MS analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 2C8 (CHEMBL3721)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Panknin O,Wagenfeld A,Bone W,Bender E,Nowak-Reppel K,Fernández-Montalván AE,Nubbemeyer R,Bäurle S,Ring S,Schmees N,Prien O,Schäfer M,Friedrich C,Zollner TM,Steinmeyer A,Mueller T,Langer G
J Med Chem (2020) 63 : 11854 -11881
PubMed 32960053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.00 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4537788 BAY-784 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4537788 BAY-784 IC50 = 1000.0 nM 6.00