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Assay Detail

CHEMBL5340494

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

Binding
Inhibition of C-terminal 6His-tagged human recombinant SCoR2 AKR1A1 expressed in Escherichia coli BL21-CodonPlus competent cells using DL-glyceraldehyde as substrate
4
Total Activities
4
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

Aldo-keto reductase family 1 member A1 (CHEMBL2246)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a Selective SCoR2 Inhibitor That Protects Against Acute Kidney Injury.
Zhou HL, Hausladen A, Anand P, Rajavel M, Stomberski CT, Zhang R, Premont RT, Greenlee WJ, van den Akker F, Stamler JS.
J Med Chem (2023) 66 : 5657 -5668
PubMed 37027003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.74 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269455 IMIRESTAT 2.0 1 7.35
CHEMBL436 TOLRESTAT 4.0 1 7.19
CHEMBL56337 EPALRESTAT 4.0 1 6.49
CHEMBL266497 SORBINIL 3.0 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269455 IMIRESTAT IC50 = 45.0 nM 7.35
CHEMBL436 TOLRESTAT IC50 = 65.0 nM 7.19
CHEMBL56337 EPALRESTAT IC50 = 325.0 nM 6.49
CHEMBL266497 SORBINIL IC50 = 1200.0 nM 5.92