Assay Detail
Binding
CHEMBL4478466
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Inhibition of pan Pim in human KMS-12-BM cells assessed as reduction in phosphorylation of biotinylated-BAD peptide at Serine 112 residue after 110 mins by flow cytometry
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KMS-12-BM |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase PIM (CHEMBL3559682) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.70 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3950704 | — | — | 1 | 7.96 |
| CHEMBL4541192 | — | — | 1 | 7.66 |
| CHEMBL4587596 | — | — | 1 | 7.64 |
| CHEMBL3902148 | — | — | 1 | 7.58 |
| CHEMBL3979182 | — | — | 1 | 7.54 |
| CHEMBL3974543 | — | — | 1 | 7.52 |
| CHEMBL3979678 | — | — | 1 | 7.51 |
| CHEMBL3940411 | — | — | 1 | 7.36 |
| CHEMBL3918714 | — | — | 1 | 7.19 |
| CHEMBL3896124 | — | — | 1 | 7.11 |
| CHEMBL4572195 | — | — | 1 | 7.06 |
| CHEMBL3959725 | — | — | 1 | 6.96 |
| CHEMBL4587256 | — | — | 1 | 6.90 |
| CHEMBL3927716 | — | — | 1 | 6.84 |
| CHEMBL3896195 | — | — | 1 | 6.83 |
| CHEMBL4589855 | — | — | 1 | 6.78 |
| CHEMBL3932879 | — | — | 1 | 6.39 |
| CHEMBL4546373 | — | — | 1 | 5.94 |
| CHEMBL4527131 | — | — | 1 | 5.86 |
| CHEMBL4530924 | — | — | 1 | 5.79 |
| CHEMBL3907325 | — | — | 1 | 5.79 |
| CHEMBL4514782 | — | — | 1 | 5.54 |
| CHEMBL3913500 | — | — | 1 | 5.34 |
| CHEMBL3949896 | — | — | 1 | 5.24 |
| CHEMBL4559238 | — | — | 1 | 5.22 |
| CHEMBL4522524 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3950704 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4541192 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4587596 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3902148 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3979182 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3974543 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3979678 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3940411 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3918714 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3896124 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4572195 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3959725 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4587256 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL3927716 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL3896195 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL4589855 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL3932879 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL4546373 | — | IC50 | = | 1142.0 | nM | 5.94 |
| CHEMBL4527131 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL4530924 | — | IC50 | = | 1642.0 | nM | 5.79 |
| CHEMBL3907325 | — | IC50 | = | 1635.0 | nM | 5.79 |
| CHEMBL4514782 | — | IC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL3913500 | — | IC50 | = | 4560.0 | nM | 5.34 |
| CHEMBL3949896 | — | IC50 | = | 5760.0 | nM | 5.24 |
| CHEMBL4559238 | — | IC50 | = | 5960.0 | nM | 5.22 |
| CHEMBL4522524 | — | IC50 | > | 2000.0 | nM | - |