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Assay Detail

CHEMBL3240534

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Binding
Binding affinity to human ERG
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

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 3 5.96 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237443 1 6.14
CHEMBL3237713 1 6.04
CHEMBL3237444 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237443 IC50 = 720.0 nM 6.14
CHEMBL3237713 IC50 = 920.0 nM 6.04
CHEMBL3237444 IC50 = 2000.0 nM 5.70