Assay Detail
Binding
CHEMBL4370147
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Inhibition of PIM1/PIM2/PIM3 in human KMS-12-BM cells assessed as reduction in BAD phosphorylation after 110 mins by flow cytometric analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KMS-12-BM |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 7.15 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4450494 | — | — | 1 | 8.10 |
| CHEMBL3950704 | — | — | 1 | 7.96 |
| CHEMBL4568404 | — | — | 1 | 7.92 |
| CHEMBL4471849 | — | — | 1 | 7.72 |
| CHEMBL4436404 | — | — | 1 | 7.68 |
| CHEMBL3958862 | — | — | 1 | 7.62 |
| CHEMBL4461181 | — | — | 1 | 7.62 |
| CHEMBL4441708 | — | — | 1 | 7.51 |
| CHEMBL3919725 | — | — | 1 | 7.46 |
| CHEMBL4456165 | — | — | 1 | 7.44 |
| CHEMBL4476513 | — | — | 1 | 7.42 |
| CHEMBL3940091 | — | — | 1 | 7.38 |
| CHEMBL4563904 | — | — | 1 | 7.34 |
| CHEMBL4468122 | — | — | 1 | 7.32 |
| CHEMBL4591512 | — | — | 1 | 7.26 |
| CHEMBL4470271 | — | — | 1 | 7.24 |
| CHEMBL3979678 | — | — | 1 | 7.23 |
| CHEMBL4464030 | — | — | 1 | 7.08 |
| CHEMBL4513589 | — | — | 1 | 7.00 |
| CHEMBL4472803 | — | — | 1 | 6.90 |
| CHEMBL4436502 | — | — | 1 | 6.71 |
| CHEMBL4443684 | — | — | 1 | 6.65 |
| CHEMBL4556760 | — | — | 1 | 6.47 |
| CHEMBL4463004 | — | — | 1 | 6.33 |
| CHEMBL4445845 | — | — | 1 | 6.15 |
| CHEMBL4573829 | — | — | 1 | 5.91 |
| CHEMBL4446411 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4450494 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3950704 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4568404 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4471849 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4436404 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3958862 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4461181 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4441708 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3919725 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4456165 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4476513 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3940091 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4563904 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4468122 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4591512 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4470271 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3979678 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4464030 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4513589 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4472803 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4436502 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL4443684 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL4556760 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL4463004 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL4445845 | — | IC50 | = | 707.0 | nM | 6.15 |
| CHEMBL4573829 | — | IC50 | = | 1239.0 | nM | 5.91 |
| CHEMBL4446411 | — | IC50 | = | 1805.0 | nM | 5.74 |