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Assay Detail

CHEMBL4431229

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

Binding
Inhibition of human recombinant carboxy-terminal His-tagged LDHB by UV endpoint assay
36
Total Activities
36
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

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 36 6.72 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065858 1 8.30
CHEMBL4436150 1 7.52
CHEMBL4467769 1 7.46
CHEMBL4576717 1 7.46
CHEMBL4536094 1 7.34
CHEMBL4520899 1 7.31
CHEMBL4444963 1 7.30
CHEMBL4453059 1 7.26
CHEMBL4521960 1 7.24
CHEMBL4475593 1 7.22
CHEMBL4543949 1 7.16
CHEMBL4450897 1 7.12
CHEMBL4435570 1 7.11
CHEMBL4543194 1 7.10
CHEMBL4557701 1 6.85
CHEMBL4589484 1 6.85
CHEMBL4534918 1 6.85
CHEMBL4545064 1 6.80
CHEMBL4583899 1 6.75
CHEMBL4555982 1 6.72
CHEMBL4578904 1 6.70
CHEMBL4437061 1 6.68
CHEMBL4474069 1 6.60
CHEMBL4444202 1 6.57
CHEMBL4468333 1 6.41
CHEMBL4445937 1 6.32
CHEMBL4574842 1 6.18
CHEMBL4530052 1 6.13
CHEMBL4575930 1 6.11
CHEMBL4591832 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065858 IC50 = 5.0 nM 8.30
CHEMBL4436150 IC50 = 30.0 nM 7.52
CHEMBL4576717 IC50 = 35.0 nM 7.46
CHEMBL4467769 IC50 = 35.0 nM 7.46
CHEMBL4536094 IC50 = 46.0 nM 7.34
CHEMBL4520899 IC50 = 49.0 nM 7.31
CHEMBL4444963 IC50 = 50.0 nM 7.30
CHEMBL4453059 IC50 = 55.0 nM 7.26
CHEMBL4521960 IC50 = 57.0 nM 7.24
CHEMBL4475593 IC50 = 60.0 nM 7.22
CHEMBL4543949 IC50 = 70.0 nM 7.16
CHEMBL4450897 IC50 = 75.0 nM 7.12
CHEMBL4435570 IC50 = 77.0 nM 7.11
CHEMBL4543194 IC50 = 80.0 nM 7.10
CHEMBL4534918 IC50 = 140.0 nM 6.85
CHEMBL4557701 IC50 = 140.0 nM 6.85
CHEMBL4589484 IC50 = 140.0 nM 6.85
CHEMBL4545064 IC50 = 160.0 nM 6.80
CHEMBL4583899 IC50 = 180.0 nM 6.75
CHEMBL4555982 IC50 = 190.0 nM 6.72
CHEMBL4578904 IC50 = 200.0 nM 6.70
CHEMBL4437061 IC50 = 210.0 nM 6.68
CHEMBL4474069 IC50 = 250.0 nM 6.60
CHEMBL4444202 IC50 = 270.0 nM 6.57
CHEMBL4468333 IC50 = 390.0 nM 6.41
CHEMBL4445937 IC50 = 480.0 nM 6.32
CHEMBL4574842 IC50 = 660.0 nM 6.18
CHEMBL4530052 IC50 = 740.0 nM 6.13
CHEMBL4575930 IC50 = 780.0 nM 6.11
CHEMBL4591832 IC50 = 800.0 nM 6.10
CHEMBL4529408 IC50 = 1100.0 nM 5.96
CHEMBL4522422 IC50 = 1800.0 nM 5.75
CHEMBL4566884 IC50 = 2200.0 nM 5.66
CHEMBL4468343 IC50 = 2300.0 nM 5.64
CHEMBL3358863 IC50 = 18000.0 nM 4.75
CHEMBL4458771 IC50 > 10000.0 nM -