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Assay Detail

CHEMBL2384178

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

Binding
Inhibition of human recombinant carboxy-terminal his-tagged LDHB (1 to 333) expressed in insect cells using pyruvate as substrate after 10 mins by UV endpoint analysis
22
Total Activities
22
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 B chain (CHEMBL4940)
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 22 4.86 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2382403 1 5.64
CHEMBL2382404 1 5.62
CHEMBL2382401 1 5.52
CHEMBL2382402 1 5.43
CHEMBL2382405 1 5.11
CHEMBL2382337 1 4.96
CHEMBL15976 OXAMATE 1 4.47
CHEMBL2382400 1 4.37
CHEMBL210497 1 4.25
CHEMBL2382397 1 4.03
CHEMBL2382389 1 4.01
CHEMBL2382338 1 -
CHEMBL2382339 1 -
CHEMBL2382390 1 -
CHEMBL2382391 1 -
CHEMBL2382392 1 -
CHEMBL2382393 1 -
CHEMBL2382394 1 -
CHEMBL2382395 1 -
CHEMBL2382396 1 -
CHEMBL2382398 1 -
CHEMBL2382399 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2382403 IC50 = 2300.0 nM 5.64
CHEMBL2382404 IC50 = 2400.0 nM 5.62
CHEMBL2382401 IC50 = 3000.0 nM 5.52
CHEMBL2382402 IC50 = 3700.0 nM 5.43
CHEMBL2382405 IC50 = 7700.0 nM 5.11
CHEMBL2382337 IC50 = 11100.0 nM 4.96
CHEMBL15976 OXAMATE IC50 = 33800.0 nM 4.47
CHEMBL2382400 IC50 = 42800.0 nM 4.37
CHEMBL210497 IC50 = 56400.0 nM 4.25
CHEMBL2382397 IC50 = 93000.0 nM 4.03
CHEMBL2382389 IC50 = 98000.0 nM 4.01
CHEMBL2382338 IC50 > 100000.0 nM -
CHEMBL2382339 IC50 > 100000.0 nM -
CHEMBL2382390 IC50 - -
CHEMBL2382391 IC50 - -
CHEMBL2382392 IC50 - -
CHEMBL2382393 IC50 > 100000.0 nM -
CHEMBL2382394 IC50 > 100000.0 nM -
CHEMBL2382395 IC50 - -
CHEMBL2382396 IC50 > 100000.0 nM -
CHEMBL2382398 IC50 > 100000.0 nM -
CHEMBL2382399 IC50 > 100000.0 nM -