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Assay Detail

CHEMBL2212266

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

Binding
Inhibition of human recombinant GLO1 expressed in Escherichia coli BL21 assessed as decrease in reduced glutathione level after 1 hr by Ellman's method
18
Total Activities
18
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

Design and evaluation of azaindole-substituted N-hydroxypyridones as glyoxalase I inhibitors.
Chiba T, Ohwada J, Sakamoto H, Kobayashi T, Fukami TA, Irie M, Miura T, Ohara K, Koyano H.
Bioorg Med Chem Lett (2012) 22 : 7486 -7489
PubMed 23122816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.34 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203964 1 7.96
CHEMBL2203978 1 7.85
CHEMBL2203976 1 7.40
CHEMBL2203975 1 6.60
CHEMBL2203963 1 6.58
CHEMBL2203974 1 6.55
CHEMBL2203966 1 6.52
CHEMBL2203965 1 6.52
CHEMBL2203977 1 6.32
CHEMBL2203967 1 6.29
CHEMBL218644 1 5.92
CHEMBL1624076 1 5.92
CHEMBL2203968 1 5.82
CHEMBL2203970 1 5.09
CHEMBL2203971 1 5.08
CHEMBL2203969 1 5.08
CHEMBL2203973 1 -
CHEMBL2203972 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203964 IC50 = 11.0 nM 7.96
CHEMBL2203978 IC50 = 14.0 nM 7.85
CHEMBL2203976 IC50 = 40.0 nM 7.40
CHEMBL2203975 IC50 = 250.0 nM 6.60
CHEMBL2203963 IC50 = 260.0 nM 6.58
CHEMBL2203974 IC50 = 280.0 nM 6.55
CHEMBL2203966 IC50 = 300.0 nM 6.52
CHEMBL2203965 IC50 = 300.0 nM 6.52
CHEMBL2203977 IC50 = 480.0 nM 6.32
CHEMBL2203967 IC50 = 510.0 nM 6.29
CHEMBL218644 IC50 = 1200.0 nM 5.92
CHEMBL1624076 IC50 = 1190.0 nM 5.92
CHEMBL2203968 IC50 = 1520.0 nM 5.82
CHEMBL2203970 IC50 = 8130.0 nM 5.09
CHEMBL2203971 IC50 = 8400.0 nM 5.08
CHEMBL2203969 IC50 = 8280.0 nM 5.08
CHEMBL2203973 IC50 > 10000.0 nM -
CHEMBL2203972 IC50 > 10000.0 nM -