Assay Detail
Binding
CHEMBL2434540
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of c-KIT (unknown origin)
24
Total Activities
24
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
Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.00 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2430262 | — | — | 1 | 8.85 |
| CHEMBL2430258 | — | — | 1 | 8.70 |
| CHEMBL2430251 | — | — | 1 | 8.68 |
| CHEMBL2430265 | — | — | 1 | 8.64 |
| CHEMBL2180602 | TAFETINIB | 1.0 | 1 | 8.62 |
| CHEMBL2430264 | — | — | 1 | 8.57 |
| CHEMBL2430250 | — | — | 1 | 8.39 |
| CHEMBL2430266 | — | — | 1 | 8.39 |
| CHEMBL2430259 | — | — | 1 | 8.24 |
| CHEMBL2430248 | — | — | 1 | 8.24 |
| CHEMBL2430261 | — | — | 1 | 8.18 |
| CHEMBL2430254 | — | — | 1 | 8.16 |
| CHEMBL2430260 | — | — | 1 | 8.13 |
| CHEMBL2430252 | — | — | 1 | 8.11 |
| CHEMBL2430253 | — | — | 1 | 8.07 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.05 |
| CHEMBL2430247 | — | — | 1 | 8.00 |
| CHEMBL2430249 | — | — | 1 | 7.97 |
| CHEMBL2430267 | — | — | 1 | 7.45 |
| CHEMBL2430198 | — | — | 1 | 7.42 |
| CHEMBL2430256 | — | — | 1 | 7.37 |
| CHEMBL2430257 | — | — | 1 | 6.74 |
| CHEMBL2430255 | — | — | 1 | 6.59 |
| CHEMBL2429872 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2430262 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2430258 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2430251 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2430265 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2180602 | TAFETINIB | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2430264 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL2430250 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2430266 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2430259 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL2430248 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL2430261 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2430254 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL2430260 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL2430252 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL2430253 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL535 | SUNITINIB | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL2430247 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL2430249 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL2430267 | — | IC50 | = | 35.5 | nM | 7.45 |
| CHEMBL2430198 | — | IC50 | = | 37.7 | nM | 7.42 |
| CHEMBL2430256 | — | IC50 | = | 43.1 | nM | 7.37 |
| CHEMBL2430257 | — | IC50 | = | 180.8 | nM | 6.74 |
| CHEMBL2430255 | — | IC50 | = | 255.7 | nM | 6.59 |
| CHEMBL2429872 | — | IC50 | = | 397.6 | nM | 6.40 |