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Assay Detail

CHEMBL4386502

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

Binding
Inhibition of human c-KIT A loop exon 17 D816V single mutant using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay
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 Autocuration

Target

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

Publication

Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants.
Wu TS, Lin WH, Tsai HJ, Hsueh CC, Hsu T, Wang PC, Lin HY, Peng YH, Lu CT, Lee LC, Tu CH, Kung FC, Shiao HY, Yeh TK, Song JS, Chang JY, Su YC, Chen LT, Chen CT, Jiaang WT, Wu SY.
J Med Chem (2019) 62 : 3940 -3957
PubMed 30968693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.07 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4448433 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4448433 IC50 = 8.56 nM 8.07