Assay Detail
Binding
CHEMBL962375
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Inhibition of His6x-tagged Plasmodium falciparum Pfmrk expressed in Escherichia coli by microtiter plate scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.73 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL139856 | — | — | 1 | 5.89 |
| CHEMBL446640 | — | — | 1 | 5.09 |
| CHEMBL470424 | — | — | 1 | 5.05 |
| CHEMBL187682 | — | — | 1 | 5.00 |
| CHEMBL506696 | — | — | 1 | 4.92 |
| CHEMBL187926 | — | — | 1 | 4.77 |
| CHEMBL471252 | — | — | 1 | 4.75 |
| CHEMBL385631 | — | — | 1 | 4.72 |
| CHEMBL450678 | — | — | 1 | 4.70 |
| CHEMBL16947 | WR-190433 | — | 1 | 4.66 |
| CHEMBL511497 | — | — | 1 | 4.47 |
| CHEMBL509932 | — | — | 1 | 4.42 |
| CHEMBL218330 | — | — | 1 | 4.30 |
| CHEMBL471667 | — | — | 1 | 4.21 |
| CHEMBL221432 | — | — | 1 | 4.00 |
| CHEMBL471253 | — | — | 1 | - |
| CHEMBL471254 | — | — | 1 | - |
| CHEMBL221741 | — | — | 1 | - |
| CHEMBL468255 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL139856 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL446640 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL470424 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL187682 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL506696 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL187926 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL471252 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL385631 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL450678 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL16947 | WR-190433 | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL511497 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL509932 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL218330 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL471667 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL221432 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL471253 | — | IC50 | = | 268000.0 | nM | - |
| CHEMBL471254 | — | IC50 | > | 256000.0 | nM | - |
| CHEMBL221741 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL468255 | — | IC50 | > | 100000.0 | nM | - |