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Assay Detail

CHEMBL2444356

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

Binding
Inhibition of human recombinant N-terminal His6-tagged AKR1B1 expressed in Escherichia coli by fluorescence assay in presence of NADPH
19
Total Activities
19
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 B1 (CHEMBL1900)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of 2-phenyliminochromene derivatives as inhibitors for aldo-keto reductase (AKR) 1B10.
Endo S, Hu D, Suyama M, Matsunaga T, Sugimoto K, Matsuya Y, El-Kabbani O, Kuwata K, Hara A, Kitade Y, Toyooka N.
Bioorg Med Chem (2013) 21 : 6378 -6384
PubMed 24071447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.68 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2440411 1 8.17
CHEMBL1172665 1 7.96
CHEMBL2440426 1 7.92
CHEMBL2440423 1 7.72
CHEMBL2440427 1 7.70
CHEMBL2440415 1 7.70
CHEMBL2440422 1 7.62
CHEMBL2440417 1 7.62
CHEMBL2440425 1 7.60
CHEMBL2440424 1 7.58
CHEMBL2440414 1 7.57
CHEMBL2440412 1 7.55
CHEMBL2440413 1 7.55
CHEMBL2440416 1 7.54
CHEMBL2440428 1 7.47
CHEMBL2440421 1 -
CHEMBL2440418 1 -
CHEMBL2440419 1 -
CHEMBL2440420 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2440411 IC50 = 6.7 nM 8.17
CHEMBL1172665 IC50 = 11.0 nM 7.96
CHEMBL2440426 IC50 = 12.0 nM 7.92
CHEMBL2440423 IC50 = 19.0 nM 7.72
CHEMBL2440427 IC50 = 20.0 nM 7.70
CHEMBL2440415 IC50 = 20.0 nM 7.70
CHEMBL2440422 IC50 = 24.0 nM 7.62
CHEMBL2440417 IC50 = 24.0 nM 7.62
CHEMBL2440425 IC50 = 25.0 nM 7.60
CHEMBL2440424 IC50 = 26.0 nM 7.58
CHEMBL2440414 IC50 = 27.0 nM 7.57
CHEMBL2440412 IC50 = 28.0 nM 7.55
CHEMBL2440413 IC50 = 28.0 nM 7.55
CHEMBL2440416 IC50 = 29.0 nM 7.54
CHEMBL2440428 IC50 = 34.0 nM 7.47
CHEMBL2440421 IC50 > 10000.0 nM -
CHEMBL2440418 IC50 > 10000.0 nM -
CHEMBL2440419 IC50 > 10000.0 nM -
CHEMBL2440420 IC50 > 10000.0 nM -