Assay Detail
Binding
CHEMBL2434542
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2 (unknown origin)
25
Total Activities
25
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
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| 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 | 25 | 8.16 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2430248 | — | — | 1 | 9.00 |
| CHEMBL2430251 | — | — | 1 | 8.96 |
| CHEMBL2430262 | — | — | 1 | 8.96 |
| CHEMBL2430258 | — | — | 1 | 8.80 |
| CHEMBL2180602 | TAFETINIB | 1.0 | 1 | 8.64 |
| CHEMBL2430266 | — | — | 1 | 8.64 |
| CHEMBL2430250 | — | — | 1 | 8.60 |
| CHEMBL2430264 | — | — | 1 | 8.59 |
| CHEMBL2430247 | — | — | 1 | 8.57 |
| CHEMBL2430261 | — | — | 1 | 8.52 |
| CHEMBL2430249 | — | — | 1 | 8.42 |
| CHEMBL2430265 | — | — | 1 | 8.41 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.40 |
| CHEMBL2430259 | — | — | 1 | 8.37 |
| CHEMBL2430252 | — | — | 1 | 8.10 |
| CHEMBL2430263 | — | — | 1 | 8.03 |
| CHEMBL2430260 | — | — | 1 | 8.01 |
| CHEMBL2430198 | — | — | 1 | 7.94 |
| CHEMBL2430253 | — | — | 1 | 7.93 |
| CHEMBL2430256 | — | — | 1 | 7.82 |
| CHEMBL2430267 | — | — | 1 | 7.61 |
| CHEMBL2430254 | — | — | 1 | 7.59 |
| CHEMBL2430257 | — | — | 1 | 6.95 |
| CHEMBL2430255 | — | — | 1 | 6.78 |
| CHEMBL2429872 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2430248 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2430251 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2430262 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2430258 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2180602 | TAFETINIB | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2430266 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2430250 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2430264 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2430247 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL2430261 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2430249 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2430265 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL535 | SUNITINIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2430259 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL2430252 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2430263 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL2430260 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL2430198 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL2430253 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL2430256 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2430267 | — | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL2430254 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL2430257 | — | IC50 | = | 112.4 | nM | 6.95 |
| CHEMBL2430255 | — | IC50 | = | 167.2 | nM | 6.78 |
| CHEMBL2429872 | — | IC50 | = | 330.3 | nM | 6.48 |