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Assay Detail

CHEMBL3240531

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

ADMET
Inhibition of CYP3A4 (unknown origin)
8
Total Activities
8
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 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
Li Z, Wang X, Eksterowicz J, Gribble MW, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC.
J Med Chem (2014) 57 : 3430 -3449
PubMed 24641103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.64 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237442 1 6.26
CHEMBL3237704 1 5.02
CHEMBL3237443 1 -
CHEMBL3237444 1 -
CHEMBL3237445 1 -
CHEMBL3237448 1 -
CHEMBL3237449 1 -
CHEMBL3237703 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237442 IC50 = 550.0 nM 6.26
CHEMBL3237704 IC50 = 9500.0 nM 5.02
CHEMBL3237443 IC50 > 10000.0 nM -
CHEMBL3237444 IC50 > 10000.0 nM -
CHEMBL3237445 IC50 > 10000.0 nM -
CHEMBL3237448 IC50 > 10000.0 nM -
CHEMBL3237449 IC50 > 10000.0 nM -
CHEMBL3237703 IC50 > 10000.0 nM -