Assay Detail
Binding
CHEMBL2033650
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Inhibition of human Pim-1 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate preincubated for 15 mins prior substrate addition measured after 45 mins by fluorescence assay
14
Total Activities
14
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
Implications of promiscuous Pim-1 kinase fragment inhibitor hydrophobic interactions for fragment-based drug design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.08 | 9.33 |
| Ki | 1 | 7.96 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2032375 | — | — | 1 | 9.33 |
| CHEMBL2032368 | — | — | 1 | 7.96 |
| CHEMBL183906 | — | — | 1 | 7.62 |
| CHEMBL441913 | — | — | 1 | 7.30 |
| CHEMBL493937 | — | — | 1 | 7.24 |
| CHEMBL2032369 | — | — | 1 | 7.04 |
| CHEMBL406652 | — | — | 1 | 6.26 |
| CHEMBL2032370 | — | — | 1 | 5.22 |
| CHEMBL1738915 | — | — | 1 | 5.22 |
| CHEMBL1738916 | — | — | 1 | 5.05 |
| CHEMBL2032371 | — | — | 1 | 5.00 |
| CHEMBL2032372 | — | — | 1 | 4.77 |
| CHEMBL2032373 | — | — | 1 | 4.55 |
| CHEMBL2032374 | — | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2032375 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL2032368 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL183906 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL441913 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL493937 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2032369 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL406652 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2032370 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1738915 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1738916 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL2032371 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2032372 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2032373 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL2032374 | — | IC50 | = | 37000.0 | nM | 4.43 |