Assay Detail
Binding
CHEMBL2162287
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NPM-ALK phosphorylation using 4-MeUP substrate by cell based assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor) (CHEMBL2111387) ↗| Type | CHIMERIC PROTEIN |
| Organism | Homo sapiens |
Publication
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.01 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158531 | — | — | 1 | 7.52 |
| CHEMBL2158527 | — | — | 1 | 7.40 |
| CHEMBL1822525 | — | — | 1 | 7.22 |
| CHEMBL2158525 | — | — | 1 | 7.22 |
| CHEMBL2158526 | — | — | 1 | 7.16 |
| CHEMBL2158529 | — | — | 1 | 7.16 |
| CHEMBL2158518 | — | — | 1 | 7.16 |
| CHEMBL2158519 | — | — | 1 | 7.16 |
| CHEMBL2158530 | — | — | 1 | 7.10 |
| CHEMBL2158516 | — | — | 1 | 7.10 |
| CHEMBL2158528 | — | — | 1 | 7.00 |
| CHEMBL2158511 | — | — | 1 | 7.00 |
| CHEMBL1934334 | — | — | 1 | 7.00 |
| CHEMBL2158586 | — | — | 1 | 6.82 |
| CHEMBL2158515 | — | — | 1 | 6.82 |
| CHEMBL2158521 | — | — | 1 | 6.70 |
| CHEMBL2158587 | — | — | 1 | 6.70 |
| CHEMBL2158513 | — | — | 1 | 6.60 |
| CHEMBL2158512 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158531 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2158527 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1822525 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2158525 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2158526 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2158529 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2158518 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2158519 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2158530 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2158516 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2158528 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2158511 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1934334 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2158586 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2158515 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2158521 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2158587 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2158513 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2158512 | — | IC50 | = | 500.0 | nM | 6.30 |