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Assay Detail

CHEMBL4670705

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

Binding
Inhibition of recombinant human LDHA using sodium pyruvate as substrate preincubated for 5 mins followed by diaphorase/resazurin addition and measured after 20 mins by fluorescence based assay
89
Total Activities
89
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

Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.
Rai G,Urban DJ,Mott BT,Hu X,Yang SM,Benavides GA,Johnson MS,Squadrito GL,Brimacombe KR,Lee TD,Cheff DM,Zhu H,Henderson MJ,Pohida K,Sulikowski GA,Dranow DM,Kabir M,Shah P,Padilha E,Tao D,Fang Y,Christov PP,Kim K,Jana S,Muttil P,Anderson T,Kunda NK,Hathaway HJ,Kusewitt DF,Oshima N,Cherukuri M,Davies DR,Norenberg JP,Sklar LA,Moore WJ,Dang CV,Stott GM,Neckers L,Flint AJ,Darley-Usmar VM,Simeonov A,Waterson AG,Jadhav A,Hall MD,Maloney DJ
J Med Chem (2020) 63 : 10984 -11011
PubMed 32902275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 89 7.32 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4792513 1 9.00
CHEMBL4786682 1 8.52
CHEMBL4797357 1 8.30
CHEMBL4752940 1 8.22
CHEMBL4749903 1 8.15
CHEMBL4759378 1 8.15
CHEMBL4747300 1 8.15
CHEMBL4783945 1 8.10
CHEMBL4790159 1 8.10
CHEMBL4759499 1 8.10
CHEMBL4786717 1 8.05
CHEMBL4760911 1 8.05
CHEMBL4783252 1 8.05
CHEMBL4794789 1 8.05
CHEMBL4777867 1 8.05
CHEMBL4751495 1 8.00
CHEMBL4787940 1 7.96
CHEMBL4752751 1 7.96
CHEMBL4740977 1 7.92
CHEMBL4783367 1 7.89
CHEMBL4763489 1 7.85
CHEMBL4762989 1 7.85
CHEMBL4754755 1 7.82
CHEMBL4758290 1 7.82
CHEMBL4746658 1 7.82
CHEMBL4751355 1 7.82
CHEMBL4784731 1 7.80
CHEMBL4784520 1 7.77
CHEMBL4761628 1 7.68
CHEMBL4782843 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4792513 IC50 = 1.0 nM 9.00
CHEMBL4786682 IC50 = 3.0 nM 8.52
CHEMBL4797357 IC50 = 5.0 nM 8.30
CHEMBL4752940 IC50 = 6.0 nM 8.22
CHEMBL4749903 IC50 = 7.0 nM 8.15
CHEMBL4759378 IC50 = 7.0 nM 8.15
CHEMBL4747300 IC50 = 7.0 nM 8.15
CHEMBL4783945 IC50 = 8.0 nM 8.10
CHEMBL4790159 IC50 = 8.0 nM 8.10
CHEMBL4759499 IC50 = 8.0 nM 8.10
CHEMBL4783252 IC50 = 9.0 nM 8.05
CHEMBL4777867 IC50 = 9.0 nM 8.05
CHEMBL4794789 IC50 = 9.0 nM 8.05
CHEMBL4760911 IC50 = 9.0 nM 8.05
CHEMBL4786717 IC50 = 9.0 nM 8.05
CHEMBL4751495 IC50 = 10.0 nM 8.00
CHEMBL4787940 IC50 = 11.0 nM 7.96
CHEMBL4752751 IC50 = 11.0 nM 7.96
CHEMBL4740977 IC50 = 12.0 nM 7.92
CHEMBL4783367 IC50 = 13.0 nM 7.89
CHEMBL4763489 IC50 = 14.0 nM 7.85
CHEMBL4762989 IC50 = 14.0 nM 7.85
CHEMBL4751355 IC50 = 15.0 nM 7.82
CHEMBL4746658 IC50 = 15.0 nM 7.82
CHEMBL4754755 IC50 = 15.0 nM 7.82
CHEMBL4758290 IC50 = 15.0 nM 7.82
CHEMBL4784731 IC50 = 16.0 nM 7.80
CHEMBL4784520 IC50 = 17.0 nM 7.77
CHEMBL4761628 IC50 = 21.0 nM 7.68
CHEMBL4782843 IC50 = 22.0 nM 7.66
CHEMBL4786033 IC50 = 23.0 nM 7.64
CHEMBL4741188 IC50 = 23.0 nM 7.64
CHEMBL4786241 IC50 = 23.0 nM 7.64
CHEMBL4785391 IC50 = 24.0 nM 7.62
CHEMBL4081890 IC50 = 24.0 nM 7.62
CHEMBL4788048 IC50 = 24.0 nM 7.62
CHEMBL4752866 IC50 = 24.0 nM 7.62
CHEMBL4746456 IC50 = 25.0 nM 7.60
CHEMBL4758227 IC50 = 25.0 nM 7.60
CHEMBL4742726 IC50 = 31.0 nM 7.51
CHEMBL4791940 IC50 = 32.0 nM 7.50
CHEMBL4762895 IC50 = 33.0 nM 7.48
CHEMBL4756608 IC50 = 33.0 nM 7.48
CHEMBL4777976 IC50 = 33.0 nM 7.48
CHEMBL4755095 IC50 = 36.0 nM 7.44
CHEMBL4761804 IC50 = 36.0 nM 7.44
CHEMBL4754861 IC50 = 36.0 nM 7.44
CHEMBL4786346 IC50 = 39.0 nM 7.41
CHEMBL4753379 IC50 = 40.0 nM 7.40
CHEMBL4763797 IC50 = 43.0 nM 7.37