Assay Detail
Functional
CHEMBL4370179
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antitumor activity against human KMS-12-BM cells xenografted in po dosed SCID-beige mouse assessed as tumor growth inhibition administered once daily for 14 days and measured twice per week
3
Total Activities
1
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KMS-12-BM |
| Confidence | 1 — Organism |
| 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 |
|---|---|---|---|
| TGI | 1 | - | - |
| ED50 | 1 | - | - |
| EC50 | 1 | 7.82 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4568404 | — | — | 3 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4568404 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4568404 | — | TGI | - | — | - | |
| CHEMBL4568404 | — | ED50 | = | 12.0 | mg.kg-1 | - |