Assay Detail
Binding
CHEMBL4706923
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Inhibition of CHK1 in human HT-29 cells assessed as abrogation of etoposide-induced G2 checkpoint arrest by ELISA
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.45 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4753307 | — | — | 1 | 7.92 |
| CHEMBL4742233 | — | — | 1 | 7.89 |
| CHEMBL4789854 | — | — | 1 | 7.68 |
| CHEMBL4169078 | SRA-737 | 1.0 | 1 | 7.52 |
| CHEMBL4790962 | — | — | 1 | 7.22 |
| CHEMBL4784718 | — | — | 1 | 7.14 |
| CHEMBL4792322 | — | — | 1 | 7.00 |
| CHEMBL4740741 | — | — | 1 | 7.00 |
| CHEMBL4741023 | — | — | 1 | 6.92 |
| CHEMBL4784549 | — | — | 1 | 6.89 |
| CHEMBL4754960 | — | — | 1 | 6.80 |
| CHEMBL4793954 | — | — | 1 | 6.75 |
| CHEMBL4797851 | — | — | 1 | 6.62 |
| CHEMBL4752718 | — | — | 1 | 6.55 |
| CHEMBL4782664 | — | — | 1 | 6.51 |
| CHEMBL4745794 | — | — | 1 | 6.41 |
| CHEMBL4789820 | — | — | 1 | 6.40 |
| CHEMBL4797888 | — | — | 1 | 6.36 |
| CHEMBL4791739 | — | — | 1 | 6.36 |
| CHEMBL4755864 | — | — | 1 | 6.30 |
| CHEMBL4742116 | — | — | 1 | 6.22 |
| CHEMBL4778934 | — | — | 1 | 6.22 |
| CHEMBL4796773 | — | — | 1 | 6.20 |
| CHEMBL4740662 | — | — | 1 | 6.10 |
| CHEMBL1928692 | — | — | 1 | 6.08 |
| CHEMBL4782716 | — | — | 1 | 6.07 |
| CHEMBL4761664 | — | — | 1 | 6.05 |
| CHEMBL4740334 | — | — | 1 | 6.00 |
| CHEMBL4799304 | — | — | 1 | 5.96 |
| CHEMBL4798119 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4753307 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4742233 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4789854 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4169078 | SRA-737 | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4790962 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4784718 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4792322 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4740741 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4741023 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4784549 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4754960 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL4793954 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4797851 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4752718 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4782664 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4745794 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4789820 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4791739 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4797888 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4755864 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4742116 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4778934 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4796773 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4740662 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1928692 | — | IC50 | = | 825.0 | nM | 6.08 |
| CHEMBL4782716 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4761664 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4740334 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4799304 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4798119 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4751342 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4752942 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4756720 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4743137 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4760882 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4750202 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4745956 | — | IC50 | > | 10000.0 | nM | - |