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Assay Detail

CHEMBL4431230

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

Binding
Inhibition of LDHA in human MiPaca2 cells assessed as inhibition of lactate production
10
Total Activities
10
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

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.
Purkey HE, Robarge K, Chen J, Chen Z, Corson LB, Ding CZ, DiPasquale AG, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Gao Z, Ge H, Hitz A, Ho Q, Labadie SS, Lai KW, Liu W, Liu Y, Li C, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sideris S, Ultsch M, Wei B, Yen I, Yue Q, Zhang H, Zhou A.
ACS Med Chem Lett (2016) 7 : 896 -901
PubMed 27774125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.42 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4520899 1 6.17
CHEMBL4065858 1 6.17
CHEMBL4450897 1 5.54
CHEMBL4534918 1 5.41
CHEMBL4543949 1 5.29
CHEMBL4475593 1 5.21
CHEMBL4557701 1 5.00
CHEMBL4583899 1 4.60
CHEMBL4543194 1 -
CHEMBL4536094 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4520899 IC50 = 670.0 nM 6.17
CHEMBL4065858 IC50 = 670.0 nM 6.17
CHEMBL4450897 IC50 = 2900.0 nM 5.54
CHEMBL4534918 IC50 = 3900.0 nM 5.41
CHEMBL4543949 IC50 = 5100.0 nM 5.29
CHEMBL4475593 IC50 = 6100.0 nM 5.21
CHEMBL4557701 IC50 = 9900.0 nM 5.00
CHEMBL4583899 IC50 = 25000.0 nM 4.60
CHEMBL4543194 IC50 > 50000.0 nM -
CHEMBL4536094 IC50 > 50000.0 nM -