Assay Detail
Binding
CHEMBL1825977
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Inhibition of human recombinant ALK assessed as phosphorylated product using PLC-gamma/GST substrate by modified ELISA method
18
Total Activities
18
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 |
Publication
2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.58 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1822521 | — | — | 1 | 8.42 |
| CHEMBL1822520 | — | — | 1 | 8.30 |
| CHEMBL1822527 | — | — | 1 | 8.15 |
| CHEMBL1821735 | — | — | 1 | 8.15 |
| CHEMBL1822523 | — | — | 1 | 8.06 |
| CHEMBL1822519 | — | — | 1 | 8.05 |
| CHEMBL1822524 | — | — | 1 | 8.05 |
| CHEMBL1822522 | — | — | 1 | 8.05 |
| CHEMBL1822525 | — | — | 1 | 8.00 |
| CHEMBL1822526 | — | — | 1 | 7.82 |
| CHEMBL1822515 | — | — | 1 | 7.70 |
| CHEMBL1822514 | — | — | 1 | 7.42 |
| CHEMBL1822513 | — | — | 1 | 7.32 |
| CHEMBL1822511 | — | — | 1 | 6.67 |
| CHEMBL1822518 | — | — | 1 | 6.58 |
| CHEMBL1822516 | — | — | 1 | 6.14 |
| CHEMBL1822517 | — | — | 1 | 6.05 |
| CHEMBL1822512 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1822521 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1822520 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1822527 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1821735 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1822523 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL1822519 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1822524 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1822522 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1822525 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1822526 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1822515 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1822514 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1822513 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1822511 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL1822518 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1822516 | — | IC50 | = | 726.0 | nM | 6.14 |
| CHEMBL1822517 | — | IC50 | = | 883.0 | nM | 6.05 |
| CHEMBL1822512 | — | IC50 | > | 2000.0 | nM | - |