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Assay Detail

CHEMBL698635

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

Functional
Effective concentration required to increase the oxidation of lactate in cellular assay using Human Skin Fibroblasts
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 1 — Organism
Curated By Intermediate

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Secondary amides of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.
Aicher TD, Anderson RC, Gao J, Shetty SS, Coppola GM, Stanton JL, Knorr DC, Sperbeck DM, Brand LJ, Vinluan CC, Kaplan EL, Dragland CJ, Tomaselli HC, Islam A, Lozito RJ, Liu X, Maniara WM, Fillers WS, DelGrande D, Walter RE, Mann WR.
J Med Chem (2000) 43 : 236 -249
PubMed 10649979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.80 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316388 1 7.24
CHEMBL309697 1 6.80
CHEMBL304292 1 6.60
CHEMBL419846 1 6.33
CHEMBL79457 1 5.95
CHEMBL93045 1 5.27
CHEMBL313843 1 4.89
CHEMBL309318 1 4.60
CHEMBL311859 1 4.54
CHEMBL306823 SODIUM DICHLOROACETATE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316388 EC50 = 57.0 nM 7.24
CHEMBL309697 EC50 = 159.0 nM 6.80
CHEMBL304292 EC50 = 250.0 nM 6.60
CHEMBL419846 EC50 = 473.0 nM 6.33
CHEMBL79457 EC50 = 1120.0 nM 5.95
CHEMBL93045 EC50 = 5400.0 nM 5.27
CHEMBL313843 EC50 = 13000.0 nM 4.89
CHEMBL309318 EC50 = 25200.0 nM 4.60
CHEMBL311859 EC50 = 29000.0 nM 4.54
CHEMBL306823 SODIUM DICHLOROACETATE EC50 = 130000.0 nM -