Assay Detail
Binding
CHEMBL888355
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Inhibition of Chk1
49
Total Activities
49
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
Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 8.42 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL248012 | — | — | 1 | 10.00 |
| CHEMBL247646 | — | — | 1 | 10.00 |
| CHEMBL247825 | — | — | 1 | 9.70 |
| CHEMBL248036 | — | — | 1 | 9.70 |
| CHEMBL248199 | — | — | 1 | 9.40 |
| CHEMBL245601 | — | — | 1 | 9.22 |
| CHEMBL400740 | — | — | 1 | 9.22 |
| CHEMBL248002 | — | — | 1 | 9.15 |
| CHEMBL247826 | — | — | 1 | 9.15 |
| CHEMBL248190 | — | — | 1 | 9.10 |
| CHEMBL248198 | — | — | 1 | 9.10 |
| CHEMBL245600 | — | — | 1 | 9.10 |
| CHEMBL247649 | — | — | 1 | 9.10 |
| CHEMBL248008 | — | — | 1 | 9.00 |
| CHEMBL400286 | — | — | 1 | 9.00 |
| CHEMBL245796 | — | — | 1 | 8.80 |
| CHEMBL245602 | — | — | 1 | 8.70 |
| CHEMBL398465 | — | — | 1 | 8.70 |
| CHEMBL246842 | — | — | 1 | 8.70 |
| CHEMBL391989 | — | — | 1 | 8.70 |
| CHEMBL247827 | — | — | 1 | 8.70 |
| CHEMBL248007 | — | — | 1 | 8.70 |
| CHEMBL429294 | — | — | 1 | 8.70 |
| CHEMBL400790 | — | — | 1 | 8.52 |
| CHEMBL247459 | — | — | 1 | 8.40 |
| CHEMBL248212 | — | — | 1 | 8.30 |
| CHEMBL247824 | — | — | 1 | 8.30 |
| CHEMBL248200 | — | — | 1 | 8.30 |
| CHEMBL248011 | — | — | 1 | 8.30 |
| CHEMBL247460 | — | — | 1 | 8.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL248012 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL247646 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL248036 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL247825 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL248199 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL245601 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL400740 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL248002 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL247826 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL248190 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL248198 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL245600 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL247649 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL248008 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL400286 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL245796 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL245602 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL398465 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL246842 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL391989 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL247827 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL248007 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL429294 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL400790 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL247459 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL247824 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL248200 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL248011 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL248212 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL247460 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL400665 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL247821 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL248001 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL398852 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL391596 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL398851 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL246845 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL248040 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL248010 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL248038 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL248000 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL248005 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL248214 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL399573 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL247018 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL248193 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL401005 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL401408 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL248194 | — | IC50 | < | 0.1 | nM | - |