Assay Detail
Functional
CHEMBL4394717
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Z138 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Z-138 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.04 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448921 | — | — | 1 | 7.92 |
| CHEMBL3544911 | PREXASERTIB | 2.0 | 1 | 7.48 |
| CHEMBL4470089 | — | — | 1 | 7.37 |
| CHEMBL4444269 | — | — | 1 | 7.33 |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | 6.43 |
| CHEMBL4456833 | — | — | 1 | 6.38 |
| CHEMBL4562902 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448921 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3544911 | PREXASERTIB | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4470089 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4444269 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3039517 | RABUSERTIB | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4456833 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL4562902 | — | IC50 | = | 413.0 | nM | 6.38 |