Assay Detail
Binding
CHEMBL4817793
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Inhibition of recombinant Plasmodium falciparum N-terminal His6-tagged GGPPS expressed in Escherichia coli expression system assessed as reduction in pyrophosphate release using GPP as substrate incubated for 30 mins followed by substrate addition by PPiLight detection reagent based luminescence assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 5.68 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4867168 | — | — | 1 | 6.30 |
| CHEMBL4847712 | — | — | 1 | 6.10 |
| CHEMBL532155 | — | — | 1 | 6.09 |
| CHEMBL4876627 | — | — | 1 | 6.03 |
| CHEMBL4870802 | — | — | 1 | 6.02 |
| CHEMBL4865424 | — | — | 1 | 6.02 |
| CHEMBL4855233 | — | — | 1 | 5.99 |
| CHEMBL4851589 | — | — | 1 | 5.98 |
| CHEMBL4849401 | — | — | 1 | 5.98 |
| CHEMBL4863548 | — | — | 1 | 5.88 |
| CHEMBL4874597 | — | — | 1 | 5.87 |
| CHEMBL4852931 | — | — | 1 | 5.85 |
| CHEMBL4856601 | — | — | 1 | 5.79 |
| CHEMBL4871401 | — | — | 1 | 5.75 |
| CHEMBL4858832 | — | — | 1 | 5.75 |
| CHEMBL4857440 | — | — | 1 | 5.74 |
| CHEMBL4872683 | — | — | 1 | 5.71 |
| CHEMBL4856911 | — | — | 1 | 5.69 |
| CHEMBL4863651 | — | — | 1 | 5.67 |
| CHEMBL4866665 | — | — | 1 | 5.62 |
| CHEMBL4879178 | — | — | 1 | 5.61 |
| CHEMBL4866275 | — | — | 1 | 5.55 |
| CHEMBL4847850 | — | — | 1 | 5.51 |
| CHEMBL4846803 | — | — | 1 | 5.50 |
| CHEMBL4863081 | — | — | 1 | 5.42 |
| CHEMBL4848497 | — | — | 1 | 5.22 |
| CHEMBL4854080 | — | — | 1 | 5.22 |
| CHEMBL4861274 | — | — | 1 | 5.22 |
| CHEMBL4861481 | — | — | 1 | 5.09 |
| CHEMBL4857559 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4867168 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4847712 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL532155 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4876627 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4870802 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4865424 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4855233 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL4851589 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4849401 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL4863548 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL4874597 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL4852931 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL4856601 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL4871401 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4858832 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4857440 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL4872683 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL4856911 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL4863651 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL4866665 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL4879178 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL4866275 | — | IC50 | = | 2790.0 | nM | 5.55 |
| CHEMBL4847850 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4846803 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL4863081 | — | IC50 | = | 3790.0 | nM | 5.42 |
| CHEMBL4848497 | — | IC50 | = | 6060.0 | nM | 5.22 |
| CHEMBL4854080 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL4861274 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4861481 | — | IC50 | = | 8120.0 | nM | 5.09 |
| CHEMBL4857559 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4847938 | — | IC50 | = | 12990.0 | nM | 4.89 |
| CHEMBL4848892 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4861469 | — | IC50 | > | 10000.0 | nM | - |