Assay Detail
Binding
CHEMBL666233
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Inhibitory concentration tested against enzyme dihydroorotate dehydrogenase in rat
70
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Dihydroorotate dehydrogenase (quinone), mitochondrial (CHEMBL2383) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, structure-activity relationships, and pharmacokinetic properties of dihydroorotate dehydrogenase inhibitors: 2-cyano-3-cyclopropyl-3-hydroxy-N-[3'-methyl-4'-(trifluoromethyl)phenyl ] propenamide and related compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 70 | 6.55 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL356115 | — | — | 1 | 8.52 |
| CHEMBL344913 | — | — | 1 | 8.30 |
| CHEMBL141248 | — | — | 1 | 8.30 |
| CHEMBL960 | LEFLUNOMIDE | 4.0 | 1 | 8.05 |
| CHEMBL139937 | — | — | 1 | 7.96 |
| CHEMBL343081 | — | — | 1 | 7.96 |
| CHEMBL973 | TERIFLUNOMIDE | 4.0 | 1 | 7.89 |
| CHEMBL143816 | — | — | 1 | 7.89 |
| CHEMBL142218 | LAFLUNIMUS | 2.0 | 1 | 7.85 |
| CHEMBL358621 | — | — | 1 | 7.80 |
| CHEMBL140558 | — | — | 1 | 7.77 |
| CHEMBL141774 | — | — | 1 | 7.75 |
| CHEMBL344556 | — | — | 1 | 7.68 |
| CHEMBL141732 | — | — | 1 | 7.68 |
| CHEMBL141047 | — | — | 1 | 7.64 |
| CHEMBL358411 | — | — | 1 | 7.55 |
| CHEMBL143116 | — | — | 1 | 7.48 |
| CHEMBL143237 | — | — | 1 | 7.43 |
| CHEMBL357459 | — | — | 1 | 7.40 |
| CHEMBL2111978 | — | — | 1 | 7.40 |
| CHEMBL142074 | — | — | 1 | 7.30 |
| CHEMBL141195 | — | — | 1 | 7.28 |
| CHEMBL143518 | — | — | 1 | 7.20 |
| CHEMBL143319 | — | — | 1 | 7.17 |
| CHEMBL143052 | — | — | 1 | 7.12 |
| CHEMBL142214 | — | — | 1 | 7.10 |
| CHEMBL141104 | — | — | 1 | 7.10 |
| CHEMBL344613 | — | — | 1 | 6.97 |
| CHEMBL139647 | — | — | 1 | 6.86 |
| CHEMBL143460 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL356115 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL344913 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL141248 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL960 | LEFLUNOMIDE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL139937 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL343081 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL973 | TERIFLUNOMIDE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL143816 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL142218 | LAFLUNIMUS | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL358621 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL140558 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL141774 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL344556 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL141732 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL141047 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL358411 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL143116 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL143237 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL357459 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2111978 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL142074 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL141195 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL143518 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL143319 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL143052 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL142214 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL141104 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL344613 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL139647 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL143460 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL139954 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL334922 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL141040 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL141086 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL337130 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL141126 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL141015 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL140115 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL344996 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL143196 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL141074 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL142705 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL357498 | — | IC50 | = | 832.0 | nM | 6.08 |
| CHEMBL139818 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL141472 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL142996 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL344405 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL141237 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL139611 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL141041 | — | IC50 | = | 2000.0 | nM | 5.70 |