Assay Detail
Binding
CHEMBL3812017
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Inhibition of human full-length Pim1 expressed in Escherichia coli assessed as phosphorylation of biotinylated BAD peptide at Ser-112 preincubated for 30 mins followed by substrate addition measured after 1 hr by HTRF assay
18
Total Activities
18
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
Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 9.29 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3810121 | — | — | 1 | 10.22 |
| CHEMBL3808669 | — | — | 1 | 10.15 |
| CHEMBL3810095 | — | — | 1 | 10.00 |
| CHEMBL3808662 | — | — | 1 | 10.00 |
| CHEMBL3809565 | — | — | 1 | 9.52 |
| CHEMBL3809691 | — | — | 1 | 9.52 |
| CHEMBL3808887 | — | — | 1 | 9.52 |
| CHEMBL3808942 | — | — | 1 | 9.40 |
| CHEMBL3809940 | — | — | 1 | 9.40 |
| CHEMBL3809377 | — | — | 1 | 9.30 |
| CHEMBL3809986 | — | — | 1 | 9.22 |
| CHEMBL3809127 | — | — | 1 | 9.00 |
| CHEMBL3809044 | — | — | 1 | 9.00 |
| CHEMBL3809463 | — | — | 1 | 9.00 |
| CHEMBL3808445 | — | — | 1 | 8.70 |
| CHEMBL3810085 | — | — | 1 | 8.52 |
| CHEMBL3809623 | — | — | 1 | 8.52 |
| CHEMBL3808459 | — | — | 1 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3810121 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3808669 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3810095 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3808662 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3809565 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3809691 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3808887 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3808942 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3809940 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3809377 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3809986 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3809127 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3809044 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3809463 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3808445 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3810085 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3809623 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3808459 | — | IC50 | = | 5.0 | nM | 8.30 |