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Assay Detail

CHEMBL4427401

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

ADMET
Inhibition of CYP2C19 (unknown origin) preincubated for 10 mins followed by addition of MFC as substrate measured after 30 mins in presence of NADP by fluorescence analysis
1
Total Activities
1
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 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent.
Liu Y, Laufer R, Patel NK, Ng G, Sampson PB, Li SW, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Plotnikova O, Awrey DE, Qiu W, Chirgadze NY, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Fletcher GC, Mak TW, Bray MR, Pauls HW.
ACS Med Chem Lett (2016) 7 : 671 -675
PubMed 27437075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.10 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4469414 LUVIXASERTIB 2.0 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4469414 LUVIXASERTIB IC50 = 8000.0 nM 5.10