Assay Detail

CHEMBL3624318

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ADMET

Inhibition of CYP3A4 in human liver microsomes

ChEMBL ↗

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Target

Cytochrome P450 3A4 (CHEMBL340) ↗

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Cytochrome P450 3A4 (CHEMBL340) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cytochrome P450 3A4

CHEMBL340

Anchored from Assay target.

Protein identity Cytochrome P450 3A4

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
Tissue	Liver
Subcellular	Microsomes
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Cytochrome P450 3A4 (CHEMBL340) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

Wan H, Schroeder GM, Hart AC, Inghrim J, Grebinski J, Tokarski JS, Lorenzi MV, You D, Mcdevitt T, Penhallow B, Vuppugalla R, Zhang Y, Gu X, Iyer R, Lombardo LJ, Trainor GL, Ruepp S, Lippy J, Blat Y, Sack JS, Khan JA, Stefanski K, Sleczka B, Mathur A, Sun JH, Wong MK, Wu DR, Li P, Gupta A, Arunachalam PN, Pragalathan B, Narayanan S, K C N, Kuppusamy P, Purandare AV.
ACS Med Chem Lett (2015) 6 : 850 -855
PubMed 26288683 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	5.52	5.52

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3545215	BMS-911543	2.0	1	5.52

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3545215	BMS-911543	IC50	=	3000.0	nM	5.52