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Assay Detail

CHEMBL4032334

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Binding
Inhibition of LDH in human A673 cells assessed as reduction in lactate production preincubated for 2 hrs measured after 30 mins by high throughput fluorescence assay
ChEMBL ↗
49
Total Activities
49
Compounds Tested
2
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 (CHEMBL4105929) ↗
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
Inhibition 28 - -
IC50 21 5.10 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081890 — — 1 6.29
CHEMBL4100845 — — 1 6.01
CHEMBL4065858 — — 1 5.84
CHEMBL4082867 — — 1 5.72
CHEMBL4059985 — — 1 5.47
CHEMBL4101800 — — 1 5.36
CHEMBL4075666 — — 1 5.03
CHEMBL4080497 — — 1 5.00
CHEMBL3335794 — — 1 4.84
CHEMBL4090677 — — 1 4.83
CHEMBL4066429 — — 1 4.78
CHEMBL4076027 — — 1 4.70
CHEMBL4090794 — — 1 4.60
CHEMBL4063125 — — 1 4.57
CHEMBL4076958 — — 1 4.57
CHEMBL4099443 — — 1 4.52
CHEMBL4069796 — — 1 4.51
CHEMBL4092360 — — 1 -
CHEMBL4084774 — — 1 -
CHEMBL4076973 — — 1 -
CHEMBL4096677 — — 1 -
CHEMBL4103659 — — 1 -
CHEMBL4077876 — — 1 -
CHEMBL4095904 — — 1 -
CHEMBL4069450 — — 1 -
CHEMBL4076264 — — 1 -
CHEMBL1479261 — — 1 -
CHEMBL2442491 — — 1 -
CHEMBL4097383 — — 1 -
CHEMBL4073369 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081890 — IC50 = 517.0 nM 6.29
CHEMBL4100845 — IC50 = 983.0 nM 6.01
CHEMBL4065858 — IC50 = 1440.0 nM 5.84
CHEMBL4082867 — IC50 = 1920.0 nM 5.72
CHEMBL4059985 — IC50 = 3370.0 nM 5.47
CHEMBL4101800 — IC50 = 4350.0 nM 5.36
CHEMBL4075666 — IC50 = 9450.0 nM 5.03
CHEMBL4080497 — IC50 = 9880.0 nM 5.00
CHEMBL3335794 — IC50 = 14500.0 nM 4.84
CHEMBL4090677 — IC50 = 14700.0 nM 4.83
CHEMBL4066429 — IC50 = 16500.0 nM 4.78
CHEMBL4076027 — IC50 = 19900.0 nM 4.70
CHEMBL4090794 — IC50 = 25200.0 nM 4.60
CHEMBL4063125 — IC50 = 26800.0 nM 4.57
CHEMBL4076958 — IC50 = 26800.0 nM 4.57
CHEMBL4099443 — IC50 = 30000.0 nM 4.52
CHEMBL4069796 — IC50 = 30800.0 nM 4.51
CHEMBL4079370 — Inhibition - % -
CHEMBL4072598 — Inhibition - % -
CHEMBL4072608 — Inhibition - % -
CHEMBL4076353 — Inhibition - % -
CHEMBL4071941 — Inhibition - % -
CHEMBL4060749 — Inhibition - % -
CHEMBL4092553 — Inhibition - % -
CHEMBL4076159 — Inhibition - % -
CHEMBL4059700 — Inhibition - % -
CHEMBL4081640 — Inhibition - % -
CHEMBL4073737 — Inhibition - % -
CHEMBL2059811 — IC50 > 57000.0 nM -
CHEMBL4080650 — Inhibition - % -
CHEMBL4077586 — Inhibition - % -
CHEMBL4066686 — Inhibition - % -
CHEMBL4062653 — Inhibition - % -
CHEMBL4059909 — Inhibition - % -
CHEMBL4070504 — Inhibition - % -
CHEMBL4094023 — Inhibition - % -
CHEMBL4073369 — Inhibition - % -
CHEMBL4097383 — Inhibition - % -
CHEMBL2442491 — Inhibition - % -
CHEMBL1479261 — Inhibition - % -
CHEMBL4076264 — Inhibition - % -
CHEMBL4069450 — Inhibition - % -
CHEMBL4095904 — Inhibition - % -
CHEMBL4077876 — Inhibition - % -
CHEMBL4103659 — Inhibition - % -
CHEMBL4096677 — Inhibition - % -
CHEMBL4076973 — IC50 > 57000.0 nM -
CHEMBL4084774 — IC50 > 57000.0 nM -
CHEMBL4092360 — IC50 > 57000.0 nM -