Assay Detail
Binding
CHEMBL960121
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Pim2
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase pim-2 (CHEMBL4523) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.79 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL510884 | — | — | 1 | 8.00 |
| CHEMBL494354 | — | — | 1 | 7.92 |
| CHEMBL523534 | — | — | 1 | 7.77 |
| CHEMBL494355 | — | — | 1 | 7.72 |
| CHEMBL454281 | — | — | 1 | 7.66 |
| CHEMBL455255 | — | — | 1 | 7.60 |
| CHEMBL495030 | — | — | 1 | 7.57 |
| CHEMBL493937 | — | — | 1 | 7.40 |
| CHEMBL492581 | — | — | 1 | 7.30 |
| CHEMBL493559 | — | — | 1 | 7.03 |
| CHEMBL455227 | — | — | 1 | 6.85 |
| CHEMBL492354 | — | — | 1 | 6.82 |
| CHEMBL523841 | — | — | 1 | 6.80 |
| CHEMBL522822 | — | — | 1 | 6.70 |
| CHEMBL492580 | — | — | 1 | 6.58 |
| CHEMBL494501 | — | — | 1 | 6.51 |
| CHEMBL522340 | — | — | 1 | 6.43 |
| CHEMBL449471 | — | — | 1 | 6.32 |
| CHEMBL523520 | — | — | 1 | 6.06 |
| CHEMBL493560 | — | — | 1 | 5.99 |
| CHEMBL493536 | — | — | 1 | 5.92 |
| CHEMBL506100 | — | — | 1 | 5.85 |
| CHEMBL492753 | — | — | 1 | 5.77 |
| CHEMBL473468 | — | — | 1 | 5.66 |
| CHEMBL493754 | — | — | 1 | 5.48 |
| CHEMBL493138 | — | — | 1 | - |
| CHEMBL521831 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL510884 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL494354 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL523534 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL494355 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL454281 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL455255 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL495030 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL493937 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL492581 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL493559 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL455227 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL492354 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL523841 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL522822 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL492580 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL494501 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL522340 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL449471 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL523520 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL493560 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL493536 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL506100 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL492753 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL473468 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL493754 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL493138 | — | IC50 | > | 8000.0 | nM | - |
| CHEMBL521831 | — | IC50 | > | 8000.0 | nM | - |