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Assay Detail

CHEMBL2384180

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

Binding
Binding affinity to human recombinant carboxy-terminal avi-tagged LDHA (1 to 331) expressed in Escherichia coli by surface plasmon resonance analysis presence of NADH
21
Total Activities
21
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

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
Kd 21 5.19 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2382401 1 5.66
CHEMBL2382403 1 5.54
CHEMBL2382404 1 5.52
CHEMBL2382402 1 5.29
CHEMBL2382337 1 5.21
CHEMBL2382405 1 5.05
CHEMBL2382400 1 4.81
CHEMBL210497 1 4.42
CHEMBL2382338 1 -
CHEMBL2382339 1 -
CHEMBL2382389 1 -
CHEMBL2382390 1 -
CHEMBL2382391 1 -
CHEMBL2382392 1 -
CHEMBL2382393 1 -
CHEMBL2382394 1 -
CHEMBL2382395 1 -
CHEMBL2382396 1 -
CHEMBL2382397 1 -
CHEMBL2382398 1 -
CHEMBL2382399 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2382401 Kd = 2200.0 nM 5.66
CHEMBL2382403 Kd = 2900.0 nM 5.54
CHEMBL2382404 Kd = 3000.0 nM 5.52
CHEMBL2382402 Kd = 5100.0 nM 5.29
CHEMBL2382337 Kd = 6100.0 nM 5.21
CHEMBL2382405 Kd = 8900.0 nM 5.05
CHEMBL2382400 Kd = 15400.0 nM 4.81
CHEMBL210497 Kd = 38400.0 nM 4.42
CHEMBL2382338 Kd = 532000.0 nM -
CHEMBL2382339 Kd = 570000.0 nM -
CHEMBL2382389 Kd = 552000.0 nM -
CHEMBL2382390 Kd = 1011000.0 nM -
CHEMBL2382391 Kd = 1105000.0 nM -
CHEMBL2382392 Kd = 1215000.0 nM -
CHEMBL2382393 Kd = 386000.0 nM -
CHEMBL2382394 Kd = 462000.0 nM -
CHEMBL2382395 Kd = 1055000.0 nM -
CHEMBL2382396 Kd = 314000.0 nM -
CHEMBL2382397 Kd = 466000.0 nM -
CHEMBL2382398 Kd = 640000.0 nM -
CHEMBL2382399 Kd = 552000.0 nM -