Assay Detail
Binding
CHEMBL5044068
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant DHODH expressed in Escherichia coli BL21 (DE3) using dihydroorotate as substrate and CoQ6 as co-substrate incubated for 10 mins by DCIP based multimode microplate reader analysis
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dihydroorotate dehydrogenase (quinone), mitochondrial (CHEMBL1966) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Orally Available Retinoic Acid Receptor-Related Orphan Receptor γ-t/Dihydroorotate Dehydrogenase Dual Inhibitors for the Treatment of Refractory Inflammatory Bowel Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 5.76 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085951 | — | — | 1 | 6.80 |
| CHEMBL5086318 | — | — | 1 | 6.76 |
| CHEMBL973 | TERIFLUNOMIDE | 4.0 | 1 | 6.64 |
| CHEMBL5093830 | — | — | 1 | 6.53 |
| CHEMBL5092142 | — | — | 1 | 6.44 |
| CHEMBL5075214 | — | — | 1 | 6.37 |
| CHEMBL5080135 | — | — | 1 | 6.24 |
| CHEMBL5086624 | — | — | 1 | 6.23 |
| CHEMBL5074809 | — | — | 1 | 6.14 |
| CHEMBL5082345 | — | — | 1 | 6.10 |
| CHEMBL5087043 | — | — | 1 | 5.99 |
| CHEMBL5080090 | — | — | 1 | 5.98 |
| CHEMBL5075048 | — | — | 1 | 5.94 |
| CHEMBL5075372 | — | — | 1 | 5.85 |
| CHEMBL5091053 | — | — | 1 | 5.67 |
| CHEMBL5075277 | — | — | 1 | 5.63 |
| CHEMBL5079972 | — | — | 1 | 5.57 |
| CHEMBL5089276 | — | — | 1 | 5.34 |
| CHEMBL5070273 | — | — | 1 | 5.33 |
| CHEMBL5071971 | — | — | 1 | 5.22 |
| CHEMBL5087158 | — | — | 1 | 5.12 |
| CHEMBL5076141 | — | — | 1 | 5.07 |
| CHEMBL5082516 | — | — | 1 | 5.03 |
| CHEMBL5084708 | — | — | 1 | 4.95 |
| CHEMBL5075241 | — | — | 1 | 4.92 |
| CHEMBL5079686 | — | — | 1 | 4.86 |
| CHEMBL5079868 | — | — | 1 | 4.69 |
| CHEMBL5082633 | — | — | 1 | - |
| CHEMBL5079945 | — | — | 1 | - |
| CHEMBL5091280 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085951 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL5086318 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL973 | TERIFLUNOMIDE | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL5093830 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL5092142 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL5075214 | — | IC50 | = | 432.0 | nM | 6.37 |
| CHEMBL5080135 | — | IC50 | = | 573.0 | nM | 6.24 |
| CHEMBL5086624 | — | IC50 | = | 588.0 | nM | 6.23 |
| CHEMBL5074809 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL5082345 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL5087043 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5080090 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL5075048 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL5075372 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL5091053 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL5075277 | — | IC50 | = | 2350.0 | nM | 5.63 |
| CHEMBL5079972 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL5089276 | — | IC50 | = | 4520.0 | nM | 5.34 |
| CHEMBL5070273 | — | IC50 | = | 4680.0 | nM | 5.33 |
| CHEMBL5071971 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL5087158 | — | IC50 | = | 7550.0 | nM | 5.12 |
| CHEMBL5076141 | — | IC50 | = | 8430.0 | nM | 5.07 |
| CHEMBL5082516 | — | IC50 | = | 9320.0 | nM | 5.03 |
| CHEMBL5084708 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL5075241 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL5079686 | — | IC50 | = | 13900.0 | nM | 4.86 |
| CHEMBL5079868 | — | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL5087808 | — | IC50 | - | — | - | |
| CHEMBL3609408 | — | IC50 | - | — | - | |
| CHEMBL62136 | T091317 | IC50 | - | — | - | |
| CHEMBL5091602 | — | IC50 | - | — | - | |
| CHEMBL5074291 | — | IC50 | - | — | - | |
| CHEMBL5091987 | — | IC50 | - | — | - | |
| CHEMBL5083524 | — | IC50 | - | — | - | |
| CHEMBL5072854 | — | IC50 | - | — | - | |
| CHEMBL5085812 | — | IC50 | - | — | - | |
| CHEMBL5079969 | — | IC50 | - | — | - | |
| CHEMBL5080847 | — | IC50 | - | — | - | |
| CHEMBL5089480 | — | IC50 | - | — | - | |
| CHEMBL5079282 | — | IC50 | - | — | - | |
| CHEMBL5091280 | — | IC50 | - | — | - | |
| CHEMBL5079945 | — | IC50 | - | — | - | |
| CHEMBL5082633 | — | IC50 | - | — | - |