Assay Detail
Binding
CHEMBL4199570
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Inhibition of human RET using cisbio TK biotin-peptide as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr 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
Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗| 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 | 9.15 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4218013 | — | — | 1 | 10.00 |
| CHEMBL4218563 | — | — | 1 | 9.70 |
| CHEMBL4218127 | — | — | 1 | 9.40 |
| CHEMBL4205243 | — | — | 1 | 9.40 |
| CHEMBL4212513 | — | — | 1 | 9.40 |
| CHEMBL3355010 | — | — | 1 | 9.40 |
| CHEMBL3355009 | GSK-3179106 | 1.0 | 1 | 9.40 |
| CHEMBL4203429 | — | — | 1 | 9.22 |
| CHEMBL4205803 | — | — | 1 | 9.15 |
| CHEMBL4214146 | — | — | 1 | 9.15 |
| CHEMBL4213626 | — | — | 1 | 9.10 |
| CHEMBL4210670 | — | — | 1 | 8.92 |
| CHEMBL4206308 | — | — | 1 | 8.77 |
| CHEMBL4209229 | — | — | 1 | 8.55 |
| CHEMBL4215099 | — | — | 1 | 7.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4218013 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4218563 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4218127 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4205243 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4212513 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3355010 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3355009 | GSK-3179106 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4203429 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4205803 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4214146 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4213626 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4210670 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4206308 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4209229 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4215099 | — | IC50 | = | 22.2 | nM | 7.65 |