Assay Detail
Binding
CHEMBL5162128
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human RET kinase using IGF1Rtide as substrate incubated for 40 mins and measured by ADP-Glo assay
31
Total Activities
31
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
Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and development of photoswitchable DFG-Out RET kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.85 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5178384 | — | — | 1 | 8.89 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 8.82 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 8.70 |
| CHEMBL5180040 | — | — | 1 | 8.52 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 8.28 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 8.23 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 8.15 |
| CHEMBL5200675 | — | — | 1 | 8.11 |
| CHEMBL5189744 | — | — | 1 | 8.02 |
| CHEMBL5184072 | — | — | 1 | 7.96 |
| CHEMBL5179230 | — | — | 1 | 7.91 |
| CHEMBL5200720 | — | — | 1 | 7.82 |
| CHEMBL5185302 | — | — | 1 | 7.77 |
| CHEMBL5191715 | — | — | 1 | 7.62 |
| CHEMBL5182347 | — | — | 1 | 7.18 |
| CHEMBL5200195 | — | — | 1 | 7.01 |
| CHEMBL5182833 | — | — | 1 | 6.59 |
| CHEMBL5193068 | — | — | 1 | 6.44 |
| CHEMBL5203860 | — | — | 1 | 6.05 |
| CHEMBL5183486 | — | — | 1 | 5.77 |
| CHEMBL5198379 | — | — | 1 | 5.75 |
| CHEMBL5197023 | — | — | 1 | 5.62 |
| CHEMBL5206567 | — | — | 1 | 5.25 |
| CHEMBL5186048 | — | — | 1 | 5.01 |
| CHEMBL5206370 | — | — | 1 | 4.90 |
| CHEMBL5206634 | — | — | 1 | 4.66 |
| CHEMBL5208770 | — | — | 1 | 4.64 |
| CHEMBL5193272 | — | — | 1 | 4.60 |
| CHEMBL5192538 | — | — | 1 | 4.31 |
| CHEMBL5188742 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5178384 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1946170 | REGORAFENIB | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2029988 | CEP-32496 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5180040 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5200675 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5189744 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL5184072 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5179230 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5200720 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5185302 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5191715 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5182347 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5200195 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5182833 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL5193068 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL5203860 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5183486 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5198379 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5197023 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5206567 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL5186048 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL5206370 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL5206634 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5208770 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL5193272 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5192538 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL5188742 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL5174897 | — | IC50 | > | 500000.0 | nM | - |