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Assay Detail

CHEMBL5142000

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

Binding
Binding affinity to His fused human DHODH expressed in Escherichia coli by surface plasmon resonance assay
2
Total Activities
2
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

<i>N</i>-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.
Cisar JS, Pietsch C, DeRatt LG, Jacoby E, Kazmi F, Keohane C, Legenski K, Matico R, Shaffer P, Simonnet Y, Tanner A, Wang CY, Wang W, Attar R, Edwards JP, Kuduk SD.
J Med Chem (2022) 65 : 11241 -11256
PubMed 35925768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.72 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5193821 1 8.96
CHEMBL5193591 1 8.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5193821 Kd = 1.1 nM 8.96
CHEMBL5193591 Kd = 3.3 nM 8.48