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Assay Detail

CHEMBL2384176

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

Binding
Inhibition of human recombinant carboxy-terminal his-tagged MDH-2 (20 to 338) expressed in Escherichia coli using oxaloacetic acid as substrate after 10 mins by UV endpoint analysis
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

Malate dehydrogenase, mitochondrial (CHEMBL5917)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase.
Dragovich PS, Fauber BP, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Malek S, Pan B, Peterson D, Pitts K, Purkey HE, Sideris S, Ultsch M, VanderPorten E, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X.
Bioorg Med Chem Lett (2013) 23 : 3186 -3194
PubMed 23628333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.07 5.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242020 1 5.07
CHEMBL2382337 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242020 IC50 = 8480.0 nM 5.07
CHEMBL2382337 IC50 > 10000.0 nM -