Assay Detail
Binding
CHEMBL4340985
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His tagged human recombinant PIM1 using PIM tide (ARKRRRHPSGPPTA) as substrate incubated for 1 hr by fluorescence based assay
41
Total Activities
41
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 of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.46 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1952142 | — | — | 1 | 9.00 |
| CHEMBL4555990 | — | — | 1 | 8.40 |
| CHEMBL4440880 | — | — | 1 | 8.22 |
| CHEMBL4556293 | — | — | 1 | 8.15 |
| CHEMBL4460019 | — | — | 1 | 8.15 |
| CHEMBL4468395 | — | — | 1 | 8.15 |
| CHEMBL4564783 | — | — | 1 | 8.00 |
| CHEMBL4483071 | — | — | 1 | 7.92 |
| CHEMBL4517926 | — | — | 1 | 7.92 |
| CHEMBL4584365 | — | — | 1 | 7.92 |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | 7.89 |
| CHEMBL4446938 | — | — | 1 | 7.89 |
| CHEMBL4577938 | — | — | 1 | 7.85 |
| CHEMBL4543342 | — | — | 1 | 7.85 |
| CHEMBL4567516 | — | — | 1 | 7.80 |
| CHEMBL4467003 | — | — | 1 | 7.77 |
| CHEMBL4526558 | — | — | 1 | 7.75 |
| CHEMBL4562507 | — | — | 1 | 7.70 |
| CHEMBL4576509 | — | — | 1 | 7.68 |
| CHEMBL4461326 | — | — | 1 | 7.60 |
| CHEMBL4521827 | — | — | 1 | 7.58 |
| CHEMBL4457634 | — | — | 1 | 7.52 |
| CHEMBL4527736 | — | — | 1 | 7.52 |
| CHEMBL4513415 | — | — | 1 | 7.52 |
| CHEMBL4547383 | — | — | 1 | 7.50 |
| CHEMBL4573369 | — | — | 1 | 7.44 |
| CHEMBL4521605 | — | — | 1 | 7.42 |
| CHEMBL4449598 | — | — | 1 | 7.34 |
| CHEMBL4526234 | — | — | 1 | 7.04 |
| CHEMBL4561045 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1952142 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4555990 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4440880 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4556293 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4460019 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4468395 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4564783 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4483071 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4517926 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4584365 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4446938 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1952329 | SGI-1776 | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4577938 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4543342 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4567516 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4467003 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4526558 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4562507 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4576509 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4461326 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4521827 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4527736 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4513415 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4457634 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4547383 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4573369 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4521605 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4449598 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4526234 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4561045 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4455041 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL4461970 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4438392 | — | IC50 | = | 425.0 | nM | 6.37 |
| CHEMBL4443603 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL4451847 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4463624 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4590812 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4471892 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4589127 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4454795 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4587006 | — | IC50 | > | 10000.0 | nM | - |