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Assay Detail

CHEMBL669211

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition measurement of orotate formation from radiolabeled dihydroorotate, using partially purified DHODase isolated from human liver.
ChEMBL ↗
54
Total Activities
54
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 (CHEMBL1966) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Immunosuppressive structure-activity relationships of Brequinar and related cinchoninic acid derivatives
Batt DG, Copeland RA, Dowling RL, Gardner TL, Jones EA, Orwat MJ, Pinto DJ, Pitts WJ, Magolda RL, Jaffee BD
Bioorg Med Chem Lett (1995) 5 : 1549 -1554
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 7.28 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39448 — — 1 8.77
CHEMBL288708 — — 1 8.10
CHEMBL38692 — — 1 8.08
CHEMBL39162 — — 1 8.00
CHEMBL290910 — — 1 8.00
CHEMBL43639 — — 1 7.96
CHEMBL38434 BREQUINAR 2.0 1 7.92
CHEMBL40093 — — 1 7.89
CHEMBL39472 — — 1 7.89
CHEMBL289470 — — 1 7.77
CHEMBL38986 — — 1 7.70
CHEMBL38421 — — 1 7.62
CHEMBL40846 — — 1 7.60
CHEMBL39396 — — 1 7.55
CHEMBL38614 — — 1 7.54
CHEMBL36047 — — 1 7.52
CHEMBL38242 — — 1 7.42
CHEMBL416057 — — 1 7.40
CHEMBL41719 — — 1 7.40
CHEMBL39971 — — 1 7.32
CHEMBL38978 — — 1 7.30
CHEMBL41799 — — 1 7.25
CHEMBL36981 — — 1 7.22
CHEMBL290674 — — 1 7.20
CHEMBL38639 — — 1 6.85
CHEMBL40182 — — 1 6.82
CHEMBL39151 — — 1 6.70
CHEMBL289071 — — 1 6.68
CHEMBL38669 — — 1 6.68
CHEMBL39188 — — 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39448 — Ki = 1.7 nM 8.77
CHEMBL288708 — Ki = 8.0 nM 8.10
CHEMBL38692 — Ki = 8.4 nM 8.08
CHEMBL39162 — Ki = 10.0 nM 8.00
CHEMBL290910 — Ki = 10.0 nM 8.00
CHEMBL43639 — Ki = 11.0 nM 7.96
CHEMBL38434 BREQUINAR Ki = 12.0 nM 7.92
CHEMBL40093 — Ki = 13.0 nM 7.89
CHEMBL39472 — Ki = 13.0 nM 7.89
CHEMBL289470 — Ki = 17.0 nM 7.77
CHEMBL38986 — Ki = 20.0 nM 7.70
CHEMBL38421 — Ki = 24.0 nM 7.62
CHEMBL40846 — Ki = 25.0 nM 7.60
CHEMBL39396 — Ki = 28.0 nM 7.55
CHEMBL38614 — Ki = 29.0 nM 7.54
CHEMBL36047 — Ki = 30.0 nM 7.52
CHEMBL38242 — Ki = 38.0 nM 7.42
CHEMBL416057 — Ki = 40.0 nM 7.40
CHEMBL41719 — Ki = 40.0 nM 7.40
CHEMBL39971 — Ki = 48.0 nM 7.32
CHEMBL38978 — Ki = 50.0 nM 7.30
CHEMBL41799 — Ki = 56.0 nM 7.25
CHEMBL36981 — Ki = 60.0 nM 7.22
CHEMBL290674 — Ki = 63.0 nM 7.20
CHEMBL38639 — Ki = 140.0 nM 6.85
CHEMBL40182 — Ki = 150.0 nM 6.82
CHEMBL39151 — Ki = 200.0 nM 6.70
CHEMBL289071 — Ki = 210.0 nM 6.68
CHEMBL38669 — Ki = 210.0 nM 6.68
CHEMBL39188 — Ki = 210.0 nM 6.68
CHEMBL40220 — Ki = 220.0 nM 6.66
CHEMBL38476 — Ki = 230.0 nM 6.64
CHEMBL433445 — Ki = 270.0 nM 6.57
CHEMBL289555 — Ki = 300.0 nM 6.52
CHEMBL288381 — Ki = 390.0 nM 6.41
CHEMBL38440 — Ki = 400.0 nM 6.40
CHEMBL39325 — Ki = 420.0 nM 6.38
CHEMBL289854 — Ki = 500.0 nM 6.30
CHEMBL288137 — Ki > 500.0 nM -
CHEMBL39397 — Ki > 500.0 nM -
CHEMBL38997 — Ki > 500.0 nM -
CHEMBL38953 — Ki > 500.0 nM -
CHEMBL288852 — Ki > 500.0 nM -
CHEMBL291268 — Ki > 500.0 nM -
CHEMBL440660 — Ki > 500.0 nM -
CHEMBL38620 — Ki > 500.0 nM -
CHEMBL43638 — Ki > 500.0 nM -
CHEMBL39191 — Ki > 500.0 nM -
CHEMBL39167 — Ki > 500.0 nM -
CHEMBL43521 — Ki > 500.0 nM -