Assay Detail
Binding
CHEMBL3750380
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PIM2 kinase (unknown origin) using Biotin-AGAGRSRHSSYPAGT-OH as substrate after 2 hrs by alphascreen assay
3
Total Activities
3
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-2 (CHEMBL4523) ↗| 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 | 3 | 8.92 | 10.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3651966 | LGH-447 | 1.0 | 1 | 10.74 |
| CHEMBL2048872 | — | — | 1 | 9.80 |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3651966 | LGH-447 | Ki | = | 0.018 | nM | 10.74 |
| CHEMBL2048872 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL1952329 | SGI-1776 | Ki | = | 610.0 | nM | 6.21 |