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Assay Detail

CHEMBL4032328

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

Binding
Stabilization of LDHA in human A673 cell lysate preincubated for 20 mins followed by incubation at 70 degreeC for 10 mins by cellular thermal shift assay
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

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ.
J Med Chem (2017) 60 : 9184 -9204
PubMed 29120638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.05 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4059985 1 7.16
CHEMBL4081890 1 6.77
CHEMBL4100845 1 6.60
CHEMBL4065858 1 5.90
CHEMBL2059811 1 5.80
CHEMBL4080497 1 5.59
CHEMBL4076973 1 5.45
CHEMBL3335794 1 5.09
CHEMBL1479261 1 -
CHEMBL4101800 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4059985 EC50 = 70.0 nM 7.16
CHEMBL4081890 EC50 = 170.0 nM 6.77
CHEMBL4100845 EC50 = 250.0 nM 6.60
CHEMBL4065858 EC50 = 1260.0 nM 5.90
CHEMBL2059811 EC50 = 1600.0 nM 5.80
CHEMBL4080497 EC50 = 2560.0 nM 5.59
CHEMBL4076973 EC50 = 3530.0 nM 5.45
CHEMBL3335794 EC50 = 8180.0 nM 5.09
CHEMBL1479261 EC50 > 100000.0 nM -
CHEMBL4101800 EC50 > 100000.0 nM -