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Assay Detail

CHEMBL3784463

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Binding
Inhibition of human recombinant glutaminyl cyclase expressed in Escherichia coli using H-Gln-Gln-H substrate measured for 15 mins by spectrophotometry
12
Total Activities
12
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

Glutaminyl-peptide cyclotransferase (CHEMBL4508)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitory effect of flavonoids on human glutaminyl cyclase.
Li M, Dong Y, Yu X, Zou Y, Zheng Y, Bu X, Quan J, He Z, Wu H.
Bioorg Med Chem (2016) 24 : 2280 -2286
PubMed 27061673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.70 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201747 1 5.28
CHEMBL3780265 1 4.85
CHEMBL3780826 1 4.82
CHEMBL3781389 1 4.82
CHEMBL3781227 1 4.79
CHEMBL3781737 1 4.78
CHEMBL3781605 1 4.71
CHEMBL3780173 1 4.58
CHEMBL3780401 1 4.55
CHEMBL59589 1 4.46
CHEMBL3780601 1 4.43
CHEMBL294878 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201747 IC50 = 5300.0 nM 5.28
CHEMBL3780265 IC50 = 14200.0 nM 4.85
CHEMBL3780826 IC50 = 15300.0 nM 4.82
CHEMBL3781389 IC50 = 15000.0 nM 4.82
CHEMBL3781227 IC50 = 16100.0 nM 4.79
CHEMBL3781737 IC50 = 16800.0 nM 4.78
CHEMBL3781605 IC50 = 19300.0 nM 4.71
CHEMBL3780173 IC50 = 26000.0 nM 4.58
CHEMBL3780401 IC50 = 27900.0 nM 4.55
CHEMBL59589 IC50 = 34600.0 nM 4.46
CHEMBL3780601 IC50 = 37200.0 nM 4.43
CHEMBL294878 IC50 = 45200.0 nM 4.34