Assay Detail
Binding
CHEMBL1114167
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Inhibition of c-Kit by HTRF method
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Three dimensional pharmacophore modelling for c-Kit receptor tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 62 | 7.12 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL374752 | — | — | 1 | 8.30 |
| CHEMBL196363 | — | — | 1 | 8.22 |
| CHEMBL371329 | — | — | 1 | 8.05 |
| CHEMBL219887 | — | — | 1 | 8.00 |
| CHEMBL374044 | — | — | 1 | 8.00 |
| CHEMBL375670 | — | — | 1 | 7.89 |
| CHEMBL365784 | — | — | 1 | 7.82 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.80 |
| CHEMBL374330 | — | — | 1 | 7.77 |
| CHEMBL220057 | — | — | 1 | 7.77 |
| CHEMBL371206 | — | — | 1 | 7.72 |
| CHEMBL371889 | — | — | 1 | 7.72 |
| CHEMBL220049 | — | — | 1 | 7.70 |
| CHEMBL382517 | — | — | 1 | 7.66 |
| CHEMBL223790 | — | — | 1 | 7.58 |
| CHEMBL425749 | — | — | 1 | 7.57 |
| CHEMBL370545 | — | — | 1 | 7.55 |
| CHEMBL219998 | — | — | 1 | 7.55 |
| CHEMBL372174 | — | — | 1 | 7.54 |
| CHEMBL223528 | — | — | 1 | 7.50 |
| CHEMBL196499 | — | — | 1 | 7.48 |
| CHEMBL223583 | — | — | 1 | 7.47 |
| CHEMBL371510 | — | — | 1 | 7.42 |
| CHEMBL219727 | — | — | 1 | 7.41 |
| CHEMBL424943 | — | — | 1 | 7.39 |
| CHEMBL376307 | — | — | 1 | 7.38 |
| CHEMBL221053 | — | — | 1 | 7.38 |
| CHEMBL426004 | — | — | 1 | 7.38 |
| CHEMBL195828 | — | — | 1 | 7.37 |
| CHEMBL194236 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL374752 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL196363 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL371329 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL219887 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL374044 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL375670 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL365784 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL223360 | LINIFANIB | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL374330 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL220057 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL371206 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL371889 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL220049 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL382517 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL223790 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL425749 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL370545 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL219998 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL372174 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL223528 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL196499 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL223583 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL371510 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL219727 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL424943 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL376307 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL426004 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL221053 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL195828 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL194236 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL223304 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL445394 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL223478 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL376245 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL196615 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL219774 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL438653 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL438797 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL222728 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL371225 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL376077 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL194321 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL370325 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL223361 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL222315 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL197635 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL381034 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL194366 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL381207 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL1081022 | — | IC50 | = | 200.0 | nM | 6.70 |