Assay Detail
Binding
CHEMBL5117326
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Pim-1 (unknown origin) measured by ADP-Glo kinase assay
10
Total Activities
10
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 |
Target
Serine/threonine-protein kinase pim-1 (CHEMBL2147) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and bioactivity evaluation of macrocyclic benzo[b]pyrido[4,3-e][1,4]oxazine derivatives as novel Pim-1 kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.64 | 7.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5199618 | — | — | 1 | 7.45 |
| CHEMBL5205827 | — | — | 1 | 7.24 |
| CHEMBL5204548 | — | — | 1 | 7.09 |
| CHEMBL5177750 | — | — | 1 | 6.86 |
| CHEMBL5197665 | — | — | 1 | 6.75 |
| CHEMBL5189982 | — | — | 1 | 6.57 |
| CHEMBL5197400 | — | — | 1 | 6.36 |
| CHEMBL5181648 | — | — | 1 | 6.33 |
| CHEMBL5204474 | — | — | 1 | 6.05 |
| CHEMBL5187722 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5199618 | — | IC50 | = | 35.13 | nM | 7.45 |
| CHEMBL5205827 | — | IC50 | = | 57.34 | nM | 7.24 |
| CHEMBL5204548 | — | IC50 | = | 81.49 | nM | 7.09 |
| CHEMBL5177750 | — | IC50 | = | 139.6 | nM | 6.86 |
| CHEMBL5197665 | — | IC50 | = | 175.9 | nM | 6.75 |
| CHEMBL5189982 | — | IC50 | = | 269.6 | nM | 6.57 |
| CHEMBL5197400 | — | IC50 | = | 433.7 | nM | 6.36 |
| CHEMBL5181648 | — | IC50 | = | 467.5 | nM | 6.33 |
| CHEMBL5204474 | — | IC50 | = | 880.6 | nM | 6.05 |
| CHEMBL5187722 | — | IC50 | = | 2185.0 | nM | 5.66 |