Assay Detail
Binding
CHEMBL923939
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Inhibition of Chk1
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 55 | 7.51 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245802 | — | — | 1 | 9.30 |
| CHEMBL398750 | — | — | 1 | 9.10 |
| CHEMBL396372 | — | — | 1 | 9.00 |
| CHEMBL397313 | — | — | 1 | 8.70 |
| CHEMBL247222 | — | — | 1 | 8.70 |
| CHEMBL247026 | — | — | 1 | 8.70 |
| CHEMBL247590 | — | — | 1 | 8.70 |
| CHEMBL247396 | — | — | 1 | 8.70 |
| CHEMBL245796 | — | — | 1 | 8.70 |
| CHEMBL400893 | — | — | 1 | 8.52 |
| CHEMBL245401 | — | — | 1 | 8.52 |
| CHEMBL247588 | — | — | 1 | 8.52 |
| CHEMBL400689 | — | — | 1 | 8.52 |
| CHEMBL399254 | — | — | 1 | 8.40 |
| CHEMBL247201 | — | — | 1 | 8.40 |
| CHEMBL248396 | — | — | 1 | 8.30 |
| CHEMBL401326 | — | — | 1 | 8.22 |
| CHEMBL399532 | — | — | 1 | 8.22 |
| CHEMBL395894 | — | — | 1 | 8.15 |
| CHEMBL247394 | — | — | 1 | 8.05 |
| CHEMBL247193 | — | — | 1 | 8.00 |
| CHEMBL245605 | — | — | 1 | 7.96 |
| CHEMBL248667 | — | — | 1 | 7.85 |
| CHEMBL440959 | — | — | 1 | 7.82 |
| CHEMBL247028 | — | — | 1 | 7.80 |
| CHEMBL445410 | — | — | 1 | 7.77 |
| CHEMBL248395 | — | — | 1 | 7.72 |
| CHEMBL248668 | — | — | 1 | 7.70 |
| CHEMBL247237 | — | — | 1 | 7.60 |
| CHEMBL401274 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245802 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL398750 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL396372 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL397313 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL247222 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL247026 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL247590 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL247396 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL245796 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL400893 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL245401 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL247588 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL400689 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL247201 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL399254 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL248396 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL401326 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL399532 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL395894 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL247394 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL247193 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL245605 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL248667 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL440959 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL247028 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL445410 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL248395 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL248668 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL247237 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL401274 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL247199 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL247200 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL398913 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL247611 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL397132 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL398728 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL400688 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL399255 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL247027 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL247427 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL247426 | — | IC50 | = | 779.0 | nM | 6.11 |
| CHEMBL247652 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL398912 | — | IC50 | = | 1288.0 | nM | 5.89 |
| CHEMBL248225 | — | IC50 | = | 1374.0 | nM | 5.86 |
| CHEMBL399253 | — | IC50 | = | 1743.0 | nM | 5.76 |
| CHEMBL401075 | — | IC50 | = | 3003.0 | nM | 5.52 |
| CHEMBL248394 | — | IC50 | = | 3709.0 | nM | 5.43 |
| CHEMBL245604 | — | IC50 | = | 4579.0 | nM | 5.34 |
| CHEMBL246620 | — | IC50 | = | 5140.0 | nM | 5.29 |
| CHEMBL245603 | — | IC50 | = | 6223.0 | nM | 5.21 |