Assay Detail
Binding
CHEMBL4199571
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human KDR using cisbio TK biotin-peptide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by HTRF assay
15
Total Activities
15
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
Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.32 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4205803 | — | — | 1 | 8.23 |
| CHEMBL4218563 | — | — | 1 | 8.10 |
| CHEMBL4218127 | — | — | 1 | 7.99 |
| CHEMBL4205243 | — | — | 1 | 7.93 |
| CHEMBL4203429 | — | — | 1 | 7.69 |
| CHEMBL4218013 | — | — | 1 | 7.68 |
| CHEMBL3355010 | — | — | 1 | 7.40 |
| CHEMBL4206308 | — | — | 1 | 7.16 |
| CHEMBL4214146 | — | — | 1 | 7.04 |
| CHEMBL4210670 | — | — | 1 | 7.02 |
| CHEMBL3355009 | GSK-3179106 | 1.0 | 1 | 6.96 |
| CHEMBL4213626 | — | — | 1 | 6.87 |
| CHEMBL4212513 | — | — | 1 | 6.67 |
| CHEMBL4209229 | — | — | 1 | 5.74 |
| CHEMBL4215099 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4205803 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4218563 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4218127 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL4205243 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4203429 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL4218013 | — | IC50 | = | 20.8 | nM | 7.68 |
| CHEMBL3355010 | — | IC50 | = | 40.1 | nM | 7.40 |
| CHEMBL4206308 | — | IC50 | = | 68.5 | nM | 7.16 |
| CHEMBL4214146 | — | IC50 | = | 91.7 | nM | 7.04 |
| CHEMBL4210670 | — | IC50 | = | 95.3 | nM | 7.02 |
| CHEMBL3355009 | GSK-3179106 | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4213626 | — | IC50 | = | 136.6 | nM | 6.87 |
| CHEMBL4212513 | — | IC50 | = | 215.8 | nM | 6.67 |
| CHEMBL4209229 | — | IC50 | = | 1830.3 | nM | 5.74 |
| CHEMBL4215099 | — | IC50 | > | 1000.0 | nM | - |