Assay Detail
Binding
CHEMBL4394697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged CHK1 (M1 to T476 residues) expressed in baculovirus infected insect cells using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay
40
Total Activities
40
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 Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 40 | 7.95 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4577258 | — | — | 1 | 9.40 |
| CHEMBL4448921 | — | — | 1 | 9.40 |
| CHEMBL4444269 | — | — | 1 | 9.30 |
| CHEMBL3544911 | PREXASERTIB | 2.0 | 1 | 9.25 |
| CHEMBL4451583 | — | — | 1 | 9.05 |
| CHEMBL4470089 | — | — | 1 | 8.89 |
| CHEMBL4473680 | — | — | 1 | 8.85 |
| CHEMBL4455460 | — | — | 1 | 8.74 |
| CHEMBL4466510 | — | — | 1 | 8.71 |
| CHEMBL4562902 | — | — | 1 | 8.61 |
| CHEMBL4587139 | — | — | 1 | 8.59 |
| CHEMBL4443253 | — | — | 1 | 8.59 |
| CHEMBL4570849 | — | — | 1 | 8.44 |
| CHEMBL4562325 | — | — | 1 | 8.43 |
| CHEMBL4466434 | — | — | 1 | 8.35 |
| CHEMBL4482947 | — | — | 1 | 8.33 |
| CHEMBL4580169 | — | — | 1 | 8.33 |
| CHEMBL4554563 | — | — | 1 | 8.19 |
| CHEMBL4457287 | — | — | 1 | 8.08 |
| CHEMBL4542788 | — | — | 1 | 8.06 |
| CHEMBL4517983 | — | — | 1 | 8.05 |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | 7.98 |
| CHEMBL4456833 | — | — | 1 | 7.96 |
| CHEMBL4537352 | — | — | 1 | 7.90 |
| CHEMBL4467504 | — | — | 1 | 7.84 |
| CHEMBL4550791 | — | — | 1 | 7.82 |
| CHEMBL4571899 | — | — | 1 | 7.80 |
| CHEMBL4446662 | — | — | 1 | 7.71 |
| CHEMBL4542480 | — | — | 1 | 7.67 |
| CHEMBL4439792 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4577258 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4448921 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4444269 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3544911 | PREXASERTIB | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL4451583 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL4470089 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4473680 | — | IC50 | = | 1.43 | nM | 8.85 |
| CHEMBL4455460 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4466510 | — | IC50 | = | 1.96 | nM | 8.71 |
| CHEMBL4562902 | — | IC50 | = | 2.43 | nM | 8.61 |
| CHEMBL4443253 | — | IC50 | = | 2.58 | nM | 8.59 |
| CHEMBL4587139 | — | IC50 | = | 2.56 | nM | 8.59 |
| CHEMBL4570849 | — | IC50 | = | 3.62 | nM | 8.44 |
| CHEMBL4562325 | — | IC50 | = | 3.75 | nM | 8.43 |
| CHEMBL4466434 | — | IC50 | = | 4.49 | nM | 8.35 |
| CHEMBL4482947 | — | IC50 | = | 4.72 | nM | 8.33 |
| CHEMBL4580169 | — | IC50 | = | 4.72 | nM | 8.33 |
| CHEMBL4554563 | — | IC50 | = | 6.44 | nM | 8.19 |
| CHEMBL4457287 | — | IC50 | = | 8.34 | nM | 8.08 |
| CHEMBL4542788 | — | IC50 | = | 8.76 | nM | 8.06 |
| CHEMBL4517983 | — | IC50 | = | 8.88 | nM | 8.05 |
| CHEMBL3039517 | RABUSERTIB | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL4456833 | — | IC50 | = | 10.95 | nM | 7.96 |
| CHEMBL4537352 | — | IC50 | = | 12.71 | nM | 7.90 |
| CHEMBL4467504 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL4550791 | — | IC50 | = | 15.14 | nM | 7.82 |
| CHEMBL4571899 | — | IC50 | = | 15.92 | nM | 7.80 |
| CHEMBL4446662 | — | IC50 | = | 19.43 | nM | 7.71 |
| CHEMBL4542480 | — | IC50 | = | 21.19 | nM | 7.67 |
| CHEMBL4444613 | — | IC50 | = | 26.33 | nM | 7.58 |
| CHEMBL4439792 | — | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL4473363 | — | IC50 | = | 29.02 | nM | 7.54 |
| CHEMBL4587158 | — | IC50 | = | 59.49 | nM | 7.23 |
| CHEMBL4453338 | — | IC50 | = | 58.94 | nM | 7.23 |
| CHEMBL4472226 | — | IC50 | = | 99.58 | nM | 7.00 |
| CHEMBL4554892 | — | IC50 | = | 365.25 | nM | 6.44 |
| CHEMBL4465516 | — | IC50 | = | 517.35 | nM | 6.29 |
| CHEMBL4467745 | — | IC50 | = | 1406.0 | nM | 5.85 |
| CHEMBL4538448 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL4442379 | — | IC50 | = | 6053.5 | nM | 5.22 |