Assay Detail
Functional
CHEMBL5053796
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Antiproliferative activity against human KM12 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
17
Total Activities
17
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
Design and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.51 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5076428 | — | — | 1 | 7.38 |
| CHEMBL5089809 | — | — | 1 | 7.25 |
| CHEMBL5082243 | — | — | 1 | 7.15 |
| CHEMBL5079032 | — | — | 1 | 7.02 |
| CHEMBL5092254 | — | — | 1 | 6.90 |
| CHEMBL5090252 | — | — | 1 | 6.64 |
| CHEMBL5077640 | — | — | 1 | 6.55 |
| CHEMBL5085280 | — | — | 1 | 6.49 |
| CHEMBL5075551 | — | — | 1 | 6.49 |
| CHEMBL5081247 | — | — | 1 | 6.38 |
| CHEMBL5075005 | — | — | 1 | 6.31 |
| CHEMBL5083023 | — | — | 1 | 5.90 |
| CHEMBL5081859 | — | — | 1 | 5.82 |
| CHEMBL5070298 | — | — | 1 | 5.69 |
| CHEMBL5093039 | — | — | 1 | 5.62 |
| CHEMBL4864729 | — | — | 1 | - |
| CHEMBL5089615 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5076428 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5089809 | — | IC50 | = | 56.4 | nM | 7.25 |
| CHEMBL5082243 | — | IC50 | = | 70.2 | nM | 7.15 |
| CHEMBL5079032 | — | IC50 | = | 95.5 | nM | 7.02 |
| CHEMBL5092254 | — | IC50 | = | 125.2 | nM | 6.90 |
| CHEMBL5090252 | — | IC50 | = | 227.9 | nM | 6.64 |
| CHEMBL5077640 | — | IC50 | = | 283.3 | nM | 6.55 |
| CHEMBL5085280 | — | IC50 | = | 323.7 | nM | 6.49 |
| CHEMBL5075551 | — | IC50 | = | 323.7 | nM | 6.49 |
| CHEMBL5081247 | — | IC50 | = | 411.8 | nM | 6.38 |
| CHEMBL5075005 | — | IC50 | = | 492.7 | nM | 6.31 |
| CHEMBL5083023 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL5081859 | — | IC50 | = | 1523.0 | nM | 5.82 |
| CHEMBL5070298 | — | IC50 | = | 2022.0 | nM | 5.69 |
| CHEMBL5093039 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4864729 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5089615 | — | IC50 | > | 10000.0 | nM | - |