Assay Detail
Binding
CHEMBL1786290
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Inhibition of Toxoplasma gondii recombinant N-terminal hexahistidine tagged CDPK1 expressed in Escherichia coli using syntide-2 as substrate after 90 mins by luminescence based scintillation counter
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Toxoplasma gondii |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Calmodulin-domain protein kinase 1 (CHEMBL1781862) ↗| Type | SINGLE PROTEIN |
| Organism | Toxoplasma gondii |
Publication
Discovery of Potent and Selective Inhibitors of Calcium-Dependent Protein Kinase 1 (CDPK1) from C. parvum and T. gondii.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 7.10 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1785012 | — | — | 1 | 8.40 |
| CHEMBL1785021 | — | — | 1 | 8.30 |
| CHEMBL1241489 | — | — | 1 | 8.30 |
| CHEMBL1785018 | — | — | 1 | 8.30 |
| CHEMBL1785020 | — | — | 1 | 8.22 |
| CHEMBL1785017 | — | — | 1 | 8.05 |
| CHEMBL1782086 | — | — | 1 | 8.05 |
| CHEMBL1785015 | — | — | 1 | 7.89 |
| CHEMBL1785014 | — | — | 1 | 7.85 |
| CHEMBL1231371 | — | — | 1 | 7.82 |
| CHEMBL1231372 | — | — | 1 | 7.82 |
| CHEMBL1785024 | — | — | 1 | 7.77 |
| CHEMBL1784975 | — | — | 1 | 7.75 |
| CHEMBL1785016 | — | — | 1 | 7.72 |
| CHEMBL1785011 | — | — | 1 | 7.70 |
| CHEMBL1242754 | — | — | 1 | 7.62 |
| CHEMBL573578 | — | — | 1 | 7.51 |
| CHEMBL1784969 | — | — | 1 | 7.44 |
| CHEMBL1242290 | — | — | 1 | 7.43 |
| CHEMBL1242847 | — | — | 1 | 7.40 |
| CHEMBL1785023 | — | — | 1 | 7.35 |
| CHEMBL1785013 | — | — | 1 | 7.32 |
| CHEMBL1784965 | — | — | 1 | 7.28 |
| CHEMBL1784972 | — | — | 1 | 7.27 |
| CHEMBL1785054 | — | — | 1 | 7.25 |
| CHEMBL1784964 | — | — | 1 | 7.23 |
| CHEMBL1784966 | — | — | 1 | 7.04 |
| CHEMBL1784971 | — | — | 1 | 7.03 |
| CHEMBL1784968 | — | — | 1 | 7.00 |
| CHEMBL1784974 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1785012 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1785021 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1785018 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1241489 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1785020 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1785017 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1782086 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1785015 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1785014 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1231371 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1231372 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1785024 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1784975 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1785016 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1785011 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1242754 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL573578 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1784969 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1242290 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1242847 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1785023 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1785013 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1784965 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1784972 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1785054 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1784964 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1784966 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL1784971 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL1784968 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1784974 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1231370 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1241588 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1784967 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1784970 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1785026 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1785019 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1242660 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL1784959 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL1784973 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1785022 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1784963 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1784960 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL1785053 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1241946 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL264406 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1784962 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1784961 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1785052 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1785025 | — | IC50 | > | 3000.0 | nM | - |