Assay Detail
Binding
CHEMBL3750239
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PIM1 kinase (unknown origin) using NH2-AGAGRSRHSSYPAGT-OH as substrate by kinase-Glo assay
14
Total Activities
14
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
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.30 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3652000 | — | — | 1 | 8.30 |
| CHEMBL3105022 | — | — | 1 | - |
| CHEMBL3651946 | — | — | 1 | - |
| CHEMBL3746909 | — | — | 1 | - |
| CHEMBL3651953 | — | — | 1 | - |
| CHEMBL3747545 | — | — | 1 | - |
| CHEMBL3651966 | LGH-447 | 1.0 | 1 | - |
| CHEMBL3747207 | — | — | 1 | - |
| CHEMBL3676258 | — | — | 1 | - |
| CHEMBL3676290 | — | — | 1 | - |
| CHEMBL3676284 | — | — | 1 | - |
| CHEMBL3676300 | — | — | 1 | - |
| CHEMBL3746984 | — | — | 1 | - |
| CHEMBL3651993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3652000 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3105022 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3651946 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3746909 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3651953 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3747545 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3651966 | LGH-447 | Ki | < | 1.0 | nM | - |
| CHEMBL3747207 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3676258 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3676290 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3676284 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3676300 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3746984 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3651993 | — | Ki | < | 1.0 | nM | - |