Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5141994

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

Binding
Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assay
29
Total Activities
29
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
IC50 29 8.31 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5180161 1 9.70
CHEMBL5193821 1 9.52
CHEMBL5171223 1 9.52
CHEMBL5187184 1 9.30
CHEMBL5186161 1 9.25
CHEMBL5198030 1 9.22
CHEMBL5206111 1 9.10
CHEMBL5209113 1 8.96
CHEMBL5193591 1 8.96
CHEMBL5077508 1 8.92
CHEMBL5197263 1 8.72
CHEMBL5176109 1 8.64
CHEMBL5205042 1 8.62
CHEMBL5207423 1 8.62
CHEMBL5197809 1 8.55
CHEMBL5193091 1 8.33
CHEMBL5178023 1 8.28
CHEMBL5170313 1 8.24
CHEMBL5181951 1 8.21
CHEMBL5201357 1 8.00
CHEMBL5197655 1 7.96
CHEMBL5184263 1 7.85
CHEMBL5209156 1 7.80
CHEMBL5193667 1 7.66
CHEMBL5175690 1 7.64
CHEMBL5189556 1 7.50
CHEMBL5201472 1 6.52
CHEMBL5199042 1 5.85
CHEMBL5191554 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5180161 IC50 = 0.2 nM 9.70
CHEMBL5193821 IC50 = 0.3 nM 9.52
CHEMBL5171223 IC50 = 0.3 nM 9.52
CHEMBL5187184 IC50 = 0.5 nM 9.30
CHEMBL5186161 IC50 = 0.56 nM 9.25
CHEMBL5198030 IC50 = 0.6 nM 9.22
CHEMBL5206111 IC50 = 0.8 nM 9.10
CHEMBL5209113 IC50 = 1.1 nM 8.96
CHEMBL5193591 IC50 = 1.1 nM 8.96
CHEMBL5077508 IC50 = 1.2 nM 8.92
CHEMBL5197263 IC50 = 1.9 nM 8.72
CHEMBL5176109 IC50 = 2.3 nM 8.64
CHEMBL5205042 IC50 = 2.4 nM 8.62
CHEMBL5207423 IC50 = 2.4 nM 8.62
CHEMBL5197809 IC50 = 2.8 nM 8.55
CHEMBL5193091 IC50 = 4.7 nM 8.33
CHEMBL5178023 IC50 = 5.2 nM 8.28
CHEMBL5170313 IC50 = 5.7 nM 8.24
CHEMBL5181951 IC50 = 6.1 nM 8.21
CHEMBL5201357 IC50 = 10.0 nM 8.00
CHEMBL5197655 IC50 = 11.0 nM 7.96
CHEMBL5184263 IC50 = 14.0 nM 7.85
CHEMBL5209156 IC50 = 16.0 nM 7.80
CHEMBL5193667 IC50 = 22.0 nM 7.66
CHEMBL5175690 IC50 = 23.0 nM 7.64
CHEMBL5189556 IC50 = 32.0 nM 7.50
CHEMBL5201472 IC50 = 302.0 nM 6.52
CHEMBL5199042 IC50 = 1400.0 nM 5.85
CHEMBL5191554 IC50 = 3600.0 nM 5.44