Assay Detail
Binding
CHEMBL955982
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Inhibition of human recombinant Pim1 expressed in insect cells by HTRF
12
Total Activities
12
Compounds Tested
2
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
Indolyl-pyrrolone as a new scaffold for Pim1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.52 | 5.68 |
| IC50 | 5 | 6.14 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.00 |
| CHEMBL268769 | — | — | 1 | 6.82 |
| CHEMBL478510 | — | — | 1 | 5.68 |
| CHEMBL476454 | — | — | 1 | 5.68 |
| CHEMBL478324 | — | — | 1 | 5.66 |
| CHEMBL476452 | — | — | 1 | 5.40 |
| CHEMBL478323 | — | — | 1 | 5.38 |
| CHEMBL476025 | — | — | 1 | 5.35 |
| CHEMBL515778 | — | — | 1 | 4.80 |
| CHEMBL515495 | — | — | 1 | - |
| CHEMBL478141 | — | — | 1 | - |
| CHEMBL500812 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL268769 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL478510 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL476454 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL478324 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL476452 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL478323 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL476025 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL515778 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL515495 | — | Ki | - | — | - | |
| CHEMBL478141 | — | Ki | - | — | - | |
| CHEMBL500812 | — | Ki | - | — | - |