Assay Detail
Binding
CHEMBL2354115
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Inhibition of Cryptosporidium parvum N-terminal His6-tagged IMPDH-mediated NADH production expressed in Escherichia coli BL21(DE3) preincubated for 5 mins prior to substrate addition by fluorescence assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cryptosporidium parvum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Inosine-5'-monophosphate dehydrogenase (CHEMBL6145) ↗| Type | SINGLE PROTEIN |
| Organism | Cryptosporidium parvum |
Publication
Optimization of benzoxazole-based inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.80 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2348794 | — | — | 1 | 9.30 |
| CHEMBL2348627 | — | — | 1 | 9.22 |
| CHEMBL2348796 | — | — | 1 | 8.92 |
| CHEMBL2348803 | — | — | 1 | 8.85 |
| CHEMBL2348793 | — | — | 1 | 8.70 |
| CHEMBL2348798 | — | — | 1 | 8.64 |
| CHEMBL2348804 | — | — | 1 | 8.57 |
| CHEMBL2348816 | — | — | 1 | 8.52 |
| CHEMBL2348823 | — | — | 1 | 8.21 |
| CHEMBL2348628 | — | — | 1 | 8.15 |
| CHEMBL2348797 | — | — | 1 | 8.05 |
| CHEMBL2348818 | — | — | 1 | 8.05 |
| CHEMBL2348795 | — | — | 1 | 7.85 |
| CHEMBL2348806 | — | — | 1 | 7.77 |
| CHEMBL2348811 | — | — | 1 | 7.72 |
| CHEMBL2348815 | — | — | 1 | 7.70 |
| CHEMBL2348635 | — | — | 1 | 7.65 |
| CHEMBL2348821 | — | — | 1 | 7.62 |
| CHEMBL2348807 | — | — | 1 | 7.58 |
| CHEMBL2348819 | — | — | 1 | 7.57 |
| CHEMBL2348805 | — | — | 1 | 7.55 |
| CHEMBL2348814 | — | — | 1 | 7.55 |
| CHEMBL2348813 | — | — | 1 | 7.40 |
| CHEMBL1500466 | — | — | 1 | 7.36 |
| CHEMBL2348799 | — | — | 1 | 7.30 |
| CHEMBL2348636 | — | — | 1 | 7.22 |
| CHEMBL2348812 | — | — | 1 | 6.98 |
| CHEMBL2348633 | — | — | 1 | 6.92 |
| CHEMBL2348801 | — | — | 1 | 6.82 |
| CHEMBL2348802 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2348794 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2348627 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2348796 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2348803 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2348793 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2348798 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2348804 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL2348816 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2348823 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL2348628 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2348797 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2348818 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2348795 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2348806 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2348811 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2348815 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2348635 | — | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL2348821 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2348807 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2348819 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2348805 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2348814 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2348813 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1500466 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2348799 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2348636 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2348812 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL2348633 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2348801 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2348802 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2348629 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2348822 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2348800 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348634 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348808 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348809 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348632 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348631 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348630 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348817 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348626 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348820 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1367075 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2348810 | — | IC50 | > | 5000.0 | nM | - |