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Assay Detail

CHEMBL883395

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Functional
Inhibitory concentration against IL-3 independent Ba/F3 Kit cell line with SCF (kit-ligand)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
Vendôme J, Letard S, Martin F, Svinarchuk F, Dubreuil P, Auclair C, Le Bret M.
J Med Chem (2005) 48 : 6194 -6201
PubMed 16190746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.99 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26559 1 8.00
CHEMBL16699 ELLIPTINIUM 2.0 1 8.00
CHEMBL197585 DATELLIPTIUM 2.0 1 8.00
CHEMBL123 ELLIPTECINE 1 6.70
CHEMBL197610 1 6.60
CHEMBL194474 1 6.52
CHEMBL941 IMATINIB 4.0 1 6.40
CHEMBL279472 1 6.40
CHEMBL19954 1 6.30
CHEMBL282444 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26559 IC50 = 10.0 nM 8.00
CHEMBL16699 ELLIPTINIUM IC50 = 10.0 nM 8.00
CHEMBL197585 DATELLIPTIUM IC50 = 10.0 nM 8.00
CHEMBL123 ELLIPTECINE IC50 = 200.0 nM 6.70
CHEMBL197610 IC50 = 250.0 nM 6.60
CHEMBL194474 IC50 = 300.0 nM 6.52
CHEMBL941 IMATINIB IC50 = 400.0 nM 6.40
CHEMBL279472 IC50 = 400.0 nM 6.40
CHEMBL19954 IC50 = 500.0 nM 6.30
CHEMBL282444 IC50 < 10.0 nM -