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Assay Detail

CHEMBL857417

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

Binding
Inhibition of Proto-oncogene tyrosine-protein kinase Kit
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mast/stem cell growth factor receptor Kit (CHEMBL1936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinical candidate CEP-7055.
Gingrich DE, Reddy DR, Iqbal MA, Singh J, Aimone LD, Angeles TS, Albom M, Yang S, Ator MA, Meyer SL, Robinson C, Ruggeri BA, Dionne CA, Vaught JL, Mallamo JP, Hudkins RL.
J Med Chem (2003) 46 : 5375 -5388
PubMed 14640546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.24 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL150894 CEP-5214 1.0 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL150894 CEP-5214 IC50 = 57.0 nM 7.24