Assay Detail
Binding
CHEMBL1825979
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NPM/ALK phosphorylation in human KARPAS299 cells by ELISA
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KARPAS-299 |
| 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
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 | 9 | 7.07 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1822527 | — | — | 1 | 7.30 |
| CHEMBL1822525 | — | — | 1 | 7.22 |
| CHEMBL1822523 | — | — | 1 | 7.16 |
| CHEMBL1822521 | — | — | 1 | 7.10 |
| CHEMBL1822526 | — | — | 1 | 7.10 |
| CHEMBL1822522 | — | — | 1 | 7.07 |
| CHEMBL1822519 | — | — | 1 | 7.00 |
| CHEMBL1822520 | — | — | 1 | 7.00 |
| CHEMBL1822524 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1822527 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1822525 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1822523 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1822521 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1822526 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1822522 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1822519 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1822520 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1822524 | — | IC50 | = | 200.0 | nM | 6.70 |