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Assay Detail

CHEMBL3374593

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

Binding
Inhibition of MDH2 (unknown origin) pre-incubated for 1 hr followed by malate and NAD+ addition
9
Total Activities
9
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

Synthesis and structure-activity relationship study of chemical probes as hypoxia induced factor-1α/malate dehydrogenase 2 inhibitors.
Naik R, Won M, Ban HS, Bhattarai D, Xu X, Eo Y, Hong YS, Singh S, Choi Y, Ahn HC, Lee K.
J Med Chem (2014) 57 : 9522 -9538
PubMed 25356789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.15 5.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3359147 1 5.26
CHEMBL427092 1 5.20
CHEMBL3359141 1 5.15
CHEMBL3359145 1 4.99
CHEMBL3359142 1 -
CHEMBL3359143 1 -
CHEMBL3359144 1 -
CHEMBL3359146 1 -
CHEMBL3359148 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3359147 IC50 = 5500.0 nM 5.26
CHEMBL427092 IC50 = 6300.0 nM 5.20
CHEMBL3359141 IC50 = 7100.0 nM 5.15
CHEMBL3359145 IC50 = 10200.0 nM 4.99
CHEMBL3359142 IC50 > 20000.0 nM -
CHEMBL3359143 IC50 > 20000.0 nM -
CHEMBL3359144 IC50 > 20000.0 nM -
CHEMBL3359146 IC50 > 20000.0 nM -
CHEMBL3359148 IC50 > 20000.0 nM -