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Assay Detail

CHEMBL4827634

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

Binding
Inhibition of recombinant human LDHA expressed in BL21 gold (DE3) using sodium pyruvate as substrate preincubated for 10 mins followed by sodium pyruvate and NADPH addition
8
Total Activities
8
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

L-lactate dehydrogenase A chain (CHEMBL4835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual Glycolate Oxidase/Lactate Dehydrogenase A Inhibitors for Primary Hyperoxaluria.
Ding J, Gumpena R, Boily MO, Caron A, Chong O, Cox JH, Dumais V, Gaudreault S, Graff AH, King A, Knight J, Oballa R, Surendradoss J, Tang T, Wu J, Lowther WT, Powell DA.
ACS Med Chem Lett (2021) 12 : 1116 -1123
PubMed 34267881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.96 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4850573 1 10.15
CHEMBL4855986 1 10.00
CHEMBL4861379 1 9.52
CHEMBL4847068 1 9.52
CHEMBL4873879 1 9.40
CHEMBL4864519 1 9.30
CHEMBL4081890 1 7.50
CHEMBL2059811 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4850573 IC50 = 0.07 nM 10.15
CHEMBL4855986 IC50 = 0.1 nM 10.00
CHEMBL4861379 IC50 = 0.3 nM 9.52
CHEMBL4847068 IC50 = 0.3 nM 9.52
CHEMBL4873879 IC50 = 0.4 nM 9.40
CHEMBL4864519 IC50 = 0.5 nM 9.30
CHEMBL4081890 IC50 = 32.0 nM 7.50
CHEMBL2059811 IC50 = 500.0 nM 6.30