Assay Detail
Binding
CHEMBL3750370
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PIM kinase in luciferase expressing human KMS11 cells assessed as inhibition of phosphorylation of S6RP after 1 hr by electrochemiluminescence assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KMS11 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 |
|---|---|---|---|
| EC50 | 5 | 6.59 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3105022 | — | — | 1 | 7.52 |
| CHEMBL3651966 | LGH-447 | 1.0 | 1 | 6.75 |
| CHEMBL3676300 | — | — | 1 | 6.50 |
| CHEMBL3651993 | — | — | 1 | 6.15 |
| CHEMBL3651946 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3105022 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3651966 | LGH-447 | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3676300 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3651993 | — | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3651946 | — | EC50 | = | 910.0 | nM | 6.04 |