Assay Detail
Binding
CHEMBL4029552
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Inhibition of kinase tracer-236 binding to GST-tagged CDK19/CyclinC (unknown origin) after 60 mins by TR-FRET assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-C/Cyclin-dependent kinase 19 (CHEMBL3883323) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.98 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4061525 | — | — | 1 | 9.44 |
| CHEMBL4083552 | — | — | 1 | 9.26 |
| CHEMBL4086487 | — | — | 1 | 9.24 |
| CHEMBL4070408 | — | — | 1 | 9.11 |
| CHEMBL4060856 | — | — | 1 | 9.01 |
| CHEMBL4066819 | — | — | 1 | 9.00 |
| CHEMBL4076395 | — | — | 1 | 9.00 |
| CHEMBL4074204 | — | — | 1 | 8.96 |
| CHEMBL4071040 | — | — | 1 | 8.89 |
| CHEMBL4082469 | — | — | 1 | 8.89 |
| CHEMBL4062244 | — | — | 1 | 8.89 |
| CHEMBL4077627 | — | — | 1 | 8.72 |
| CHEMBL4090775 | — | — | 1 | 8.62 |
| CHEMBL4091345 | — | — | 1 | 8.57 |
| CHEMBL4069854 | — | — | 1 | 8.55 |
| CHEMBL4060714 | — | — | 1 | 8.18 |
| CHEMBL4072372 | — | — | 1 | 8.04 |
| CHEMBL4088931 | — | — | 1 | 8.03 |
| CHEMBL4059564 | — | — | 1 | 7.92 |
| CHEMBL4065027 | — | — | 1 | 7.82 |
| CHEMBL4063358 | — | — | 1 | 7.72 |
| CHEMBL4063680 | — | — | 1 | 7.68 |
| CHEMBL4062262 | — | — | 1 | 7.66 |
| CHEMBL4061783 | — | — | 1 | 7.60 |
| CHEMBL4082699 | — | — | 1 | 7.34 |
| CHEMBL4092709 | — | — | 1 | 7.19 |
| CHEMBL4069269 | — | — | 1 | 7.15 |
| CHEMBL4084957 | — | — | 1 | 7.03 |
| CHEMBL4097047 | — | — | 1 | 6.96 |
| CHEMBL4083979 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4061525 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL4083552 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL4086487 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL4070408 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL4060856 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL4066819 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL4076395 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4074204 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4062244 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4082469 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4071040 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4077627 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4090775 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4091345 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4069854 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4060714 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4072372 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4088931 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4059564 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4065027 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4063358 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4063680 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4062262 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4061783 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4082699 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4092709 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4069269 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4084957 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4097047 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4083979 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4060582 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4102907 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4073611 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4100438 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4090315 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4091219 | — | IC50 | - | — | - |