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Assay Detail

CHEMBL4351545

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

ADMET
Inhibition of CYP2C8 (unknown origin)
2
Total Activities
2
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 2C8 (CHEMBL3721)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Identification of a Novel, Functionally Subtype Selective GABA<sub>A</sub> Positive Allosteric Modulator (PF-06372865).
Owen RM, Blakemore D, Cao L, Flanagan N, Fish R, Gibson KR, Gurrell R, Huh CW, Kammonen J, Mortimer-Cassen E, Nickolls SA, Omoto K, Owen D, Pike A, Pryde DC, Reynolds DS, Roeloffs R, Rose C, Stead C, Takeuchi M, Warmus JS, Watson C.
J Med Chem (2019) 62 : 5773 -5796
PubMed 30964988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.55 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4545044 1 4.82
CHEMBL3647536 DARIGABAT 2.0 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4545044 IC50 = 15200.0 nM 4.82
CHEMBL3647536 DARIGABAT IC50 = 52000.0 nM 4.28