Assay Detail
Binding
CHEMBL4478464
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Inhibition of full length recombinant Pim-1 (unknown origin) assessed as reduction in phosphorylation of biotinylated-BAD peptide at Serine 112 residue preincubated for 30 mins followed by substrate addition for 1 hr by HTRF assay
26
Total Activities
26
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 Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.94 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3979182 | — | — | 1 | 10.00 |
| CHEMBL3902148 | — | — | 1 | 10.00 |
| CHEMBL3896195 | — | — | 1 | 9.70 |
| CHEMBL3950704 | — | — | 1 | 9.70 |
| CHEMBL3979678 | — | — | 1 | 9.52 |
| CHEMBL4587596 | — | — | 1 | 9.52 |
| CHEMBL3896124 | — | — | 1 | 9.40 |
| CHEMBL3932879 | — | — | 1 | 9.30 |
| CHEMBL4541192 | — | — | 1 | 9.22 |
| CHEMBL3974543 | — | — | 1 | 9.15 |
| CHEMBL4587256 | — | — | 1 | 9.15 |
| CHEMBL3959725 | — | — | 1 | 9.10 |
| CHEMBL4572195 | — | — | 1 | 9.05 |
| CHEMBL3927716 | — | — | 1 | 9.05 |
| CHEMBL3940411 | — | — | 1 | 8.92 |
| CHEMBL4589855 | — | — | 1 | 8.82 |
| CHEMBL3918714 | — | — | 1 | 8.80 |
| CHEMBL4527131 | — | — | 1 | 8.60 |
| CHEMBL3907325 | — | — | 1 | 8.59 |
| CHEMBL4522524 | — | — | 1 | 8.51 |
| CHEMBL4530924 | — | — | 1 | 8.35 |
| CHEMBL4514782 | — | — | 1 | 8.19 |
| CHEMBL4546373 | — | — | 1 | 8.19 |
| CHEMBL3913500 | — | — | 1 | 8.18 |
| CHEMBL4559238 | — | — | 1 | 8.14 |
| CHEMBL3949896 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3979182 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3902148 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3896195 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3950704 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3979678 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4587596 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3896124 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3932879 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4541192 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3974543 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4587256 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3959725 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4572195 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3927716 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3940411 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4589855 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3918714 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4527131 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3907325 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4522524 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4530924 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4514782 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4546373 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3913500 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4559238 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3949896 | — | IC50 | = | 44.0 | nM | 7.36 |