Assay Detail
Binding
CHEMBL960124
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Pim1 after 15 mins by scintillation counting-based competition assay in presence of 100 uM [gamma33P]ATP
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase pim-1 (CHEMBL2147) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.11 | 7.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.61 |
| CHEMBL494762 | — | — | 1 | 6.92 |
| CHEMBL493937 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL494762 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL493937 | — | IC50 | = | 161.0 | nM | 6.79 |