Assay Detail

CHEMBL4618969

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ADMET

Inhibition of recombinant CYP2C8 (unknown origin)

ChEMBL ↗

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Target

Cytochrome P450 2C8 (CHEMBL3721) ↗

Open DB target context

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Cytochrome P450 2C8 (CHEMBL3721) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cytochrome P450 2C8

CHEMBL3721

Anchored from Assay target.

Protein identity Cytochrome P450 2C8

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.

Cherney RJ, Cornelius LAM, Srivastava A, Weigelt CA, Marcoux D, Duan JJ, Shi Q, Batt DG, Liu Q, Yip S, Wu DR, Ruzanov M, Sack J, Khan J, Wang J, Yarde M, Cvijic ME, Mathur A, Li S, Shuster D, Khandelwal P, Borowski V, Xie J, Obermeier M, Fura A, Stefanski K, Cornelius G, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM.
ACS Med Chem Lett (2020) 11 : 1221 -1227
PubMed 32551004 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	4.80	4.80

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4634542	BMS-986251	1.0	1	4.80

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4634542	BMS-986251	IC50	=	16000.0	nM	4.80