Assay Detail
Binding
CHEMBL4416170
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Plasmodium falciparum full length N-terminal His-tagged PKG expressed in Escherichia coli RosettaTM 2(DE3) pLysS cells using FAM-GRTGRRNSI-NH2 as substrate preincubated for 30 mins followed by ATP addition and measured after 30 mins by microfluidic mobility shift assay
57
Total Activities
57
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 |
Target
cGMP-dependent protein kinase (CHEMBL2169724) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum |
Publication
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against <i>Plasmodium falciparum</i> Malaria Parasites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 57 | 8.16 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4531058 | — | — | 1 | 9.22 |
| CHEMBL4459320 | — | — | 1 | 8.89 |
| CHEMBL4469667 | — | — | 1 | 8.77 |
| CHEMBL4532321 | — | — | 1 | 8.77 |
| CHEMBL4449947 | — | — | 1 | 8.77 |
| CHEMBL4451783 | — | — | 1 | 8.77 |
| CHEMBL4461276 | — | — | 1 | 8.77 |
| CHEMBL4288103 | — | — | 1 | 8.70 |
| CHEMBL4455587 | — | — | 1 | 8.70 |
| CHEMBL4286841 | — | — | 1 | 8.70 |
| CHEMBL4593717 | — | — | 1 | 8.64 |
| CHEMBL4572858 | — | — | 1 | 8.52 |
| CHEMBL4585607 | — | — | 1 | 8.48 |
| CHEMBL4531226 | — | — | 1 | 8.44 |
| CHEMBL4444451 | — | — | 1 | 8.44 |
| CHEMBL4566588 | — | — | 1 | 8.42 |
| CHEMBL4546641 | — | — | 1 | 8.37 |
| CHEMBL4591417 | — | — | 1 | 8.36 |
| CHEMBL4459919 | — | — | 1 | 8.32 |
| CHEMBL4446015 | — | — | 1 | 8.30 |
| CHEMBL4446024 | — | — | 1 | 8.25 |
| CHEMBL4473609 | — | — | 1 | 8.00 |
| CHEMBL4585479 | — | — | 1 | 7.99 |
| CHEMBL4572065 | — | — | 1 | 7.93 |
| CHEMBL4461850 | — | — | 1 | 7.90 |
| CHEMBL4462111 | — | — | 1 | 7.79 |
| CHEMBL4567664 | — | — | 1 | 7.47 |
| CHEMBL4572752 | — | — | 1 | 7.35 |
| CHEMBL4548154 | — | — | 1 | 7.28 |
| CHEMBL4516715 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4531058 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4459320 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4532321 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4449947 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4451783 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4461276 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4469667 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4288103 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4455587 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4286841 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4593717 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4572858 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4585607 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4444451 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4531226 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4566588 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4546641 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4591417 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4459919 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4446015 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4446024 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4473609 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4585479 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL4572065 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4461850 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL4462111 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL4567664 | — | IC50 | = | 33.9 | nM | 7.47 |
| CHEMBL4572752 | — | IC50 | = | 44.7 | nM | 7.35 |
| CHEMBL4548154 | — | IC50 | = | 52.5 | nM | 7.28 |
| CHEMBL4516715 | — | IC50 | = | 89.1 | nM | 7.05 |
| CHEMBL4444869 | — | IC50 | = | 1259.0 | nM | 5.90 |
| CHEMBL4551036 | — | IC50 | = | 1862.0 | nM | 5.73 |
| CHEMBL4586918 | — | IC50 | - | — | - | |
| CHEMBL4436765 | — | IC50 | - | — | - | |
| CHEMBL4586441 | — | IC50 | - | — | - | |
| CHEMBL4534387 | — | IC50 | - | — | - | |
| CHEMBL4454838 | — | IC50 | - | — | - | |
| CHEMBL4565096 | — | IC50 | - | — | - | |
| CHEMBL4439775 | — | IC50 | - | — | - | |
| CHEMBL4441206 | — | IC50 | - | — | - | |
| CHEMBL4566303 | — | IC50 | - | — | - | |
| CHEMBL4461043 | — | IC50 | - | — | - | |
| CHEMBL4453994 | — | IC50 | - | — | - | |
| CHEMBL4437350 | — | IC50 | - | — | - | |
| CHEMBL4536120 | — | IC50 | - | — | - | |
| CHEMBL4471859 | — | IC50 | - | — | - | |
| CHEMBL4465850 | — | IC50 | - | — | - | |
| CHEMBL4552534 | — | IC50 | - | — | - | |
| CHEMBL4530907 | — | IC50 | - | — | - | |
| CHEMBL4448543 | — | IC50 | - | — | - |