Assay Detail
Binding
CHEMBL994190
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Inhibition of Pim1
10
Total Activities
10
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
Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.87 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL523823 | — | — | 1 | 8.60 |
| CHEMBL509801 | — | — | 1 | 7.91 |
| CHEMBL492223 | — | — | 1 | 7.82 |
| CHEMBL468280 | — | — | 1 | 7.66 |
| CHEMBL491405 | — | — | 1 | 7.44 |
| CHEMBL489784 | — | — | 1 | 6.57 |
| CHEMBL500183 | — | — | 1 | 5.93 |
| CHEMBL489783 | — | — | 1 | 5.90 |
| CHEMBL454241 | — | — | 1 | 5.57 |
| CHEMBL522266 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL523823 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL509801 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL492223 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL468280 | — | Ki | = | 21.8 | nM | 7.66 |
| CHEMBL491405 | — | Ki | = | 36.5 | nM | 7.44 |
| CHEMBL489784 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL500183 | — | Ki | = | 1162.0 | nM | 5.93 |
| CHEMBL489783 | — | Ki | = | 1271.0 | nM | 5.90 |
| CHEMBL454241 | — | Ki | = | 2698.0 | nM | 5.57 |
| CHEMBL522266 | — | Ki | = | 4894.0 | nM | 5.31 |