Assay Detail
Binding
CHEMBL960122
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Inhibition of Pim1 in presence of 1 uM ATP
6
Total Activities
6
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 | 6 | 7.41 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.12 |
| CHEMBL494354 | — | — | 1 | 7.89 |
| CHEMBL454281 | — | — | 1 | 7.48 |
| CHEMBL492581 | — | — | 1 | 7.30 |
| CHEMBL493937 | — | — | 1 | 7.24 |
| CHEMBL449471 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL494354 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL454281 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL492581 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL493937 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL449471 | — | IC50 | = | 370.0 | nM | 6.43 |