Assay Detail
Functional
CHEMBL4618787
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human KM12 cells expressing TPM3-TRKA assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KM12 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
PROTAC Compounds Targeting TRK for Use in Cancer Therapeutics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.61 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4649835 | — | — | 1 | 9.05 |
| CHEMBL4638495 | — | — | 1 | 9.05 |
| CHEMBL4639369 | — | — | 1 | 9.05 |
| CHEMBL4649362 | — | — | 1 | 8.82 |
| CHEMBL4642693 | — | — | 1 | 8.80 |
| CHEMBL4643936 | — | — | 1 | 8.70 |
| CHEMBL4641378 | — | — | 1 | 8.47 |
| CHEMBL4633902 | — | — | 1 | 8.42 |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | 8.37 |
| CHEMBL4646064 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4649835 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4638495 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4639369 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4649362 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4642693 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4643936 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4641378 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4633902 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1983268 | ENTRECTINIB | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4646064 | — | IC50 | = | 46.7 | nM | 7.33 |