Assay Detail
Binding
CHEMBL4340983
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal 6-His tagged human recombinant PIM3 using PIM tide (ARKRRRHPSGPPTA) as substrate incubated for 1 hr by fluorescence based assay
32
Total Activities
32
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-3 (CHEMBL5407) ↗| 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 | 32 | 7.23 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1952142 | — | — | 1 | 9.10 |
| CHEMBL4457634 | — | — | 1 | 9.00 |
| CHEMBL4555990 | — | — | 1 | 8.22 |
| CHEMBL4483071 | — | — | 1 | 8.22 |
| CHEMBL4564783 | — | — | 1 | 8.15 |
| CHEMBL4526558 | — | — | 1 | 7.92 |
| CHEMBL4527736 | — | — | 1 | 7.85 |
| CHEMBL4577938 | — | — | 1 | 7.77 |
| CHEMBL4460019 | — | — | 1 | 7.58 |
| CHEMBL4468395 | — | — | 1 | 7.40 |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | 7.30 |
| CHEMBL4576509 | — | — | 1 | 7.26 |
| CHEMBL4446938 | — | — | 1 | 7.24 |
| CHEMBL4440880 | — | — | 1 | 7.24 |
| CHEMBL4517926 | — | — | 1 | 7.22 |
| CHEMBL4556293 | — | — | 1 | 7.16 |
| CHEMBL4567516 | — | — | 1 | 7.12 |
| CHEMBL4521605 | — | — | 1 | 7.10 |
| CHEMBL4543342 | — | — | 1 | 7.09 |
| CHEMBL4584365 | — | — | 1 | 7.02 |
| CHEMBL4573369 | — | — | 1 | 6.88 |
| CHEMBL4467003 | — | — | 1 | 6.85 |
| CHEMBL4521827 | — | — | 1 | 6.62 |
| CHEMBL4561045 | — | — | 1 | 6.59 |
| CHEMBL4562507 | — | — | 1 | 6.55 |
| CHEMBL4547383 | — | — | 1 | 6.52 |
| CHEMBL4461326 | — | — | 1 | 6.45 |
| CHEMBL4513415 | — | — | 1 | 6.40 |
| CHEMBL4449598 | — | — | 1 | 5.81 |
| CHEMBL4526234 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1952142 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4457634 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4555990 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4483071 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4564783 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4526558 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4527736 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4577938 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4460019 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4468395 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1952329 | SGI-1776 | IC50 | = | 50.5 | nM | 7.30 |
| CHEMBL4576509 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4446938 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4440880 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4517926 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4556293 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4567516 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4521605 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4543342 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4584365 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4573369 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4467003 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4521827 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4561045 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL4562507 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL4547383 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4461326 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL4513415 | — | IC50 | = | 402.0 | nM | 6.40 |
| CHEMBL4449598 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4526234 | — | IC50 | = | 4080.0 | nM | 5.39 |
| CHEMBL4455041 | — | IC50 | - | — | - | |
| CHEMBL4461970 | — | IC50 | > | 10000.0 | nM | - |