Assay Detail
Binding
CHEMBL873572
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Inhibitory concentration against c-Kit D816V type expressed in recombinant baculovirus
11
Total Activities
11
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
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.92 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL197585 | DATELLIPTIUM | 2.0 | 1 | 6.52 |
| CHEMBL26559 | — | — | 1 | 6.40 |
| CHEMBL16699 | ELLIPTINIUM | 2.0 | 1 | 6.40 |
| CHEMBL19954 | — | — | 1 | 6.22 |
| CHEMBL282444 | — | — | 1 | 5.92 |
| CHEMBL197610 | — | — | 1 | 5.72 |
| CHEMBL279472 | — | — | 1 | 5.70 |
| CHEMBL55137 | — | — | 1 | 5.44 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.00 |
| CHEMBL123 | ELLIPTECINE | — | 1 | - |
| CHEMBL194474 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL197585 | DATELLIPTIUM | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL26559 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL16699 | ELLIPTINIUM | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL19954 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL282444 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL197610 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL279472 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL55137 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL941 | IMATINIB | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL123 | ELLIPTECINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL194474 | — | IC50 | > | 10000.0 | nM | - |