Assay Detail
Binding
CHEMBL4370145
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant PIM1 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay
27
Total Activities
27
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 ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 9.71 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4513589 | — | — | 1 | 10.70 |
| CHEMBL4450494 | — | — | 1 | 10.52 |
| CHEMBL4471849 | — | — | 1 | 10.52 |
| CHEMBL4568404 | — | — | 1 | 10.30 |
| CHEMBL4436404 | — | — | 1 | 10.22 |
| CHEMBL3940091 | — | — | 1 | 10.15 |
| CHEMBL4446411 | — | — | 1 | 10.10 |
| CHEMBL4441708 | — | — | 1 | 10.05 |
| CHEMBL3958862 | — | — | 1 | 10.00 |
| CHEMBL4468122 | — | — | 1 | 9.96 |
| CHEMBL4464030 | — | — | 1 | 9.92 |
| CHEMBL4591512 | — | — | 1 | 9.89 |
| CHEMBL4470271 | — | — | 1 | 9.85 |
| CHEMBL4472803 | — | — | 1 | 9.80 |
| CHEMBL3919725 | — | — | 1 | 9.77 |
| CHEMBL3950704 | — | — | 1 | 9.70 |
| CHEMBL4436502 | — | — | 1 | 9.68 |
| CHEMBL4456165 | — | — | 1 | 9.54 |
| CHEMBL3979678 | — | — | 1 | 9.47 |
| CHEMBL4563904 | — | — | 1 | 9.46 |
| CHEMBL4461181 | — | — | 1 | 9.44 |
| CHEMBL4476513 | — | — | 1 | 9.26 |
| CHEMBL4445845 | — | — | 1 | 9.25 |
| CHEMBL4463004 | — | — | 1 | 9.19 |
| CHEMBL4443684 | — | — | 1 | 8.92 |
| CHEMBL4556760 | — | — | 1 | 8.74 |
| CHEMBL4573829 | — | — | 1 | 7.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4513589 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL4450494 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4471849 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4568404 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL4436404 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3940091 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL4446411 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL4441708 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3958862 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4468122 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4464030 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL4591512 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4470271 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL4472803 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3919725 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3950704 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4436502 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL4456165 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL3979678 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4563904 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL4461181 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL4476513 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL4445845 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL4463004 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL4443684 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4556760 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4573829 | — | IC50 | = | 20.3 | nM | 7.69 |