Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4370193

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

Binding
Inhibition recombinant human N-terminal 6His-tagged GLO1 (2 to 184 residues) expressed in Escherichia coli using MG as substrate preincubated for 15 to 20 mins followed by substrate addition and measured every 1 min for 8 mins
60
Total Activities
60
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

Lactoylglutathione lyase (CHEMBL2424)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Metal-Binding Pharmacophore Library Yields the Discovery of a Glyoxalase 1 Inhibitor.
Perez C, Barkley-Levenson AM, Dick BL, Glatt PF, Martinez Y, Siegel D, Momper JD, Palmer AA, Cohen SM.
J Med Chem (2019) 62 : 1609 -1625
PubMed 30628789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 5.46 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4559294 1 6.43
CHEMBL4516514 1 6.34
CHEMBL4543065 1 6.32
CHEMBL4539074 1 6.30
CHEMBL4457949 1 6.27
CHEMBL4571524 1 6.23
CHEMBL4573731 1 6.19
CHEMBL4466017 1 6.14
CHEMBL4532036 1 6.10
CHEMBL4514413 1 6.10
CHEMBL4580349 1 5.98
CHEMBL4467660 1 5.92
CHEMBL4575972 1 5.92
CHEMBL3981698 1 5.89
CHEMBL4454726 1 5.88
CHEMBL3392484 1 5.44
CHEMBL4582242 1 5.41
CHEMBL4440697 1 5.41
CHEMBL4444789 1 5.38
CHEMBL4582717 1 5.34
CHEMBL257234 1 5.31
CHEMBL4547694 1 5.26
CHEMBL4571585 1 5.24
CHEMBL4468491 1 5.21
CHEMBL4465108 1 5.21
CHEMBL4530675 1 5.18
CHEMBL4471411 1 5.18
CHEMBL3948213 1 5.16
CHEMBL3392552 1 5.16
CHEMBL3966573 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4559294 IC50 = 370.0 nM 6.43
CHEMBL4516514 IC50 = 460.0 nM 6.34
CHEMBL4543065 IC50 = 480.0 nM 6.32
CHEMBL4539074 IC50 = 500.0 nM 6.30
CHEMBL4457949 IC50 = 540.0 nM 6.27
CHEMBL4571524 IC50 = 590.0 nM 6.23
CHEMBL4573731 IC50 = 640.0 nM 6.19
CHEMBL4466017 IC50 = 720.0 nM 6.14
CHEMBL4532036 IC50 = 790.0 nM 6.10
CHEMBL4514413 IC50 = 790.0 nM 6.10
CHEMBL4580349 IC50 = 1040.0 nM 5.98
CHEMBL4467660 IC50 = 1210.0 nM 5.92
CHEMBL4575972 IC50 = 1190.0 nM 5.92
CHEMBL3981698 IC50 = 1300.0 nM 5.89
CHEMBL4454726 IC50 = 1320.0 nM 5.88
CHEMBL3392484 IC50 = 3600.0 nM 5.44
CHEMBL4582242 IC50 = 3900.0 nM 5.41
CHEMBL4440697 IC50 = 3900.0 nM 5.41
CHEMBL4444789 IC50 = 4200.0 nM 5.38
CHEMBL4582717 IC50 = 4600.0 nM 5.34
CHEMBL257234 IC50 = 4900.0 nM 5.31
CHEMBL4547694 IC50 = 5500.0 nM 5.26
CHEMBL4571585 IC50 = 5700.0 nM 5.24
CHEMBL4468491 IC50 = 6100.0 nM 5.21
CHEMBL4465108 IC50 = 6200.0 nM 5.21
CHEMBL4530675 IC50 = 6600.0 nM 5.18
CHEMBL4471411 IC50 = 6600.0 nM 5.18
CHEMBL3948213 IC50 = 6900.0 nM 5.16
CHEMBL3392552 IC50 = 7000.0 nM 5.16
CHEMBL3966573 IC50 = 7300.0 nM 5.14
CHEMBL397804 IC50 = 7500.0 nM 5.12
CHEMBL4562864 IC50 = 7600.0 nM 5.12
CHEMBL257286 IC50 = 8500.0 nM 5.07
CHEMBL4586764 IC50 = 8700.0 nM 5.06
CHEMBL3941648 IC50 = 11200.0 nM 4.95
CHEMBL4448798 IC50 = 11200.0 nM 4.95
CHEMBL3633431 IC50 = 11500.0 nM 4.94
CHEMBL4569197 IC50 = 11900.0 nM 4.92
CHEMBL4551803 IC50 = 13900.0 nM 4.86
CHEMBL1321754 IC50 = 14500.0 nM 4.84
CHEMBL4593835 IC50 = 15400.0 nM 4.81
CHEMBL1235568 IC50 = 18500.0 nM 4.73
CHEMBL1095743 IC50 = 43000.0 nM 4.37
CHEMBL3956684 IC50 > 20000.0 nM -
CHEMBL4561485 IC50 > 200000.0 nM -
CHEMBL4468867 IC50 > 200000.0 nM -
CHEMBL4442283 IC50 > 200000.0 nM -
CHEMBL4443754 IC50 > 100000.0 nM -
CHEMBL4474760 IC50 > 100000.0 nM -
CHEMBL1866173 IC50 > 200000.0 nM -