Assay Detail
Binding
CHEMBL4431786
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Toxoplasma gondii CDPK1 using Biotin-C6-PLARTLSVAGLPGKK as substrate after 90 mins in presence of ATP by luciferase reporter gene assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Toxoplasma gondii |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Calmodulin-domain protein kinase 1 (CHEMBL1781862) ↗| Type | SINGLE PROTEIN |
| Organism | Toxoplasma gondii |
Publication
Development of an Orally Available and Central Nervous System (CNS) Penetrant Toxoplasma gondii Calcium-Dependent Protein Kinase 1 (TgCDPK1) Inhibitor with Minimal Human Ether-a-go-go-Related Gene (hERG) Activity for the Treatment of Toxoplasmosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.43 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4591429 | — | — | 1 | 9.10 |
| CHEMBL4553699 | — | — | 1 | 9.05 |
| CHEMBL4571877 | — | — | 1 | 9.00 |
| CHEMBL4455656 | — | — | 1 | 8.96 |
| CHEMBL4558168 | — | — | 1 | 8.92 |
| CHEMBL4471923 | — | — | 1 | 8.89 |
| CHEMBL4543259 | — | — | 1 | 8.82 |
| CHEMBL4517731 | — | — | 1 | 8.80 |
| CHEMBL4476674 | — | — | 1 | 8.74 |
| CHEMBL4556402 | — | — | 1 | 8.74 |
| CHEMBL4536241 | — | — | 1 | 8.70 |
| CHEMBL4573817 | — | — | 1 | 8.70 |
| CHEMBL4537636 | — | — | 1 | 8.70 |
| CHEMBL4439120 | — | — | 1 | 8.68 |
| CHEMBL4450160 | — | — | 1 | 8.66 |
| CHEMBL4572244 | — | — | 1 | 8.62 |
| CHEMBL4444685 | — | — | 1 | 8.60 |
| CHEMBL2078876 | — | — | 1 | 8.54 |
| CHEMBL4587540 | — | — | 1 | 8.49 |
| CHEMBL4445333 | — | — | 1 | 8.48 |
| CHEMBL4572930 | — | — | 1 | 8.40 |
| CHEMBL4582694 | — | — | 1 | 8.40 |
| CHEMBL4443394 | — | — | 1 | 8.35 |
| CHEMBL4461001 | — | — | 1 | 8.25 |
| CHEMBL4558606 | — | — | 1 | 8.22 |
| CHEMBL4576165 | — | — | 1 | 8.21 |
| CHEMBL4435505 | — | — | 1 | 8.00 |
| CHEMBL4445679 | — | — | 1 | 8.00 |
| CHEMBL2078877 | — | — | 1 | 7.96 |
| CHEMBL4469755 | — | — | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4591429 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4553699 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4571877 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4455656 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4558168 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4471923 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4543259 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4517731 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4476674 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4556402 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4536241 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4573817 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4537636 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4439120 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4450160 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4572244 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4444685 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2078876 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4587540 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4445333 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4572930 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4582694 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4443394 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4461001 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4558606 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4576165 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4435505 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4445679 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2078877 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4469755 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4440560 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4593860 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4464073 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4584646 | — | IC50 | = | 94.0 | nM | 7.03 |