Assay Detail
Binding
CHEMBL5731353
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Luminescent Kinase Assay: Inhibition of TgCDPK1 and CpCDPK1 was determined using a luminescent kinase assay which measures ATP depletion in the presence of the Syntide 2 peptide substrate (KinaseGlo). For description of the methods and assays, see WO 2011/094628, incorporated by reference herein. Similar to TgCDPK1, exogenous calcium was necessary for CpCDPK1 to possess maximum catalytic activity (data not shown). Notably, both kinases were tested at the same ATP concentration which allows direct comparison of inhibitor potencies due to these enzymes possessing similar Kms for this cofactor.
309
Total Activities
103
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Calmodulin-domain protein kinase 1 (CHEMBL1781862) ↗| Type | SINGLE PROTEIN |
| Organism | Toxoplasma gondii |
Publication
5-aminopyrazole-4-carboxamide inhibitors of CDPK1 from T. gondii and C. parvum
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 103 | 7.71 | 8.70 |
| kon | 103 | - | - |
| k_off | 103 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3108998 | — | — | 3 | 8.70 |
| CHEMBL3109011 | — | — | 3 | 8.70 |
| CHEMBL3770409 | — | — | 3 | 8.70 |
| CHEMBL3108912 | — | — | 3 | 8.70 |
| CHEMBL2030552 | — | — | 3 | 8.52 |
| CHEMBL2078876 | — | — | 3 | 8.52 |
| CHEMBL5997598 | — | — | 3 | 8.52 |
| CHEMBL3771104 | — | — | 3 | 8.40 |
| CHEMBL3108991 | — | — | 3 | 8.40 |
| CHEMBL3108913 | — | — | 3 | 8.40 |
| CHEMBL3108996 | — | — | 3 | 8.30 |
| CHEMBL3770923 | — | — | 3 | 8.30 |
| CHEMBL3770076 | — | — | 3 | 8.30 |
| CHEMBL5875870 | — | — | 3 | 8.30 |
| CHEMBL3769990 | — | — | 3 | 8.24 |
| CHEMBL3108986 | — | — | 3 | 8.22 |
| CHEMBL5915240 | — | — | 3 | 8.22 |
| CHEMBL3771018 | — | — | 3 | 8.22 |
| CHEMBL3770802 | — | — | 3 | 8.22 |
| CHEMBL3771134 | — | — | 3 | 8.22 |
| CHEMBL3770676 | — | — | 3 | 8.22 |
| CHEMBL3109010 | — | — | 3 | 8.22 |
| CHEMBL3108988 | — | — | 3 | 8.15 |
| CHEMBL3108997 | — | — | 3 | 8.15 |
| CHEMBL3108999 | — | — | 3 | 8.15 |
| CHEMBL3770980 | — | — | 3 | 8.15 |
| CHEMBL3769459 | — | — | 3 | 8.15 |
| CHEMBL5891569 | — | — | 3 | 8.15 |
| CHEMBL1231371 | — | — | 3 | 8.10 |
| CHEMBL3108985 | — | — | 3 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3770409 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3108912 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3109011 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3108998 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2030552 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5997598 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2078876 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3108913 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3771104 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3108991 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5875870 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3108996 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3770076 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3770923 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3769990 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3771018 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3109010 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5915240 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3770676 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3770802 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3108986 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3771134 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3108988 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3770980 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3108999 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3108997 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5891569 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3769459 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1231371 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3769918 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3108985 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3108987 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3770885 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5934987 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL6018550 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3769798 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3973192 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5922123 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3109009 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3108992 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3108916 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3770760 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3108990 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL6047879 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3771242 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3771306 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL6011159 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3769685 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6007813 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5973238 | — | IC50 | = | 12.0 | nM | 7.92 |