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Assay Detail

CHEMBL5149905

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

Binding
Inhibition of recombinant human QC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis
69
Total Activities
69
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

2-Amino-1,3,4-thiadiazoles as Glutaminyl Cyclases Inhibitors Increase Phagocytosis through Modification of CD47-SIRPα Checkpoint.
Park E, Song KH, Kim D, Lee M, Van Manh N, Kim H, Hong KB, Lee J, Song JY, Kang S.
ACS Med Chem Lett (2022) 13 : 1459 -1467
PubMed 36105338 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 69 6.46 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5193156 1 7.92
CHEMBL5190683 1 7.77
CHEMBL5181839 1 7.75
CHEMBL5202172 1 7.70
CHEMBL201747 1 7.54
CHEMBL5195495 1 7.24
CHEMBL5197396 1 7.01
CHEMBL5207620 1 7.00
CHEMBL5194983 1 6.97
CHEMBL5202004 1 6.96
CHEMBL5178150 1 6.93
CHEMBL5204178 1 6.81
CHEMBL5186970 1 6.80
CHEMBL5198938 1 6.77
CHEMBL5174441 1 6.72
CHEMBL5174554 1 6.70
CHEMBL5175865 1 6.70
CHEMBL5188828 1 6.30
CHEMBL5205052 1 6.30
CHEMBL5187305 1 6.22
CHEMBL5194144 1 5.82
CHEMBL5196820 1 5.80
CHEMBL5186424 1 5.75
CHEMBL5183220 1 5.68
CHEMBL5181626 1 5.66
CHEMBL5169588 1 5.60
CHEMBL5172975 1 5.47
CHEMBL5196169 1 5.44
CHEMBL5194882 1 5.42
CHEMBL5196273 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5193156 IC50 = 12.0 nM 7.92
CHEMBL5190683 IC50 = 17.0 nM 7.77
CHEMBL5181839 IC50 = 18.0 nM 7.75
CHEMBL5202172 IC50 = 20.0 nM 7.70
CHEMBL201747 IC50 = 29.0 nM 7.54
CHEMBL5195495 IC50 = 57.0 nM 7.24
CHEMBL5197396 IC50 = 98.0 nM 7.01
CHEMBL5207620 IC50 = 100.0 nM 7.00
CHEMBL5194983 IC50 = 108.0 nM 6.97
CHEMBL5202004 IC50 = 111.0 nM 6.96
CHEMBL5178150 IC50 = 118.0 nM 6.93
CHEMBL5204178 IC50 = 154.0 nM 6.81
CHEMBL5186970 IC50 = 160.0 nM 6.80
CHEMBL5198938 IC50 = 170.0 nM 6.77
CHEMBL5174441 IC50 = 190.0 nM 6.72
CHEMBL5174554 IC50 = 199.0 nM 6.70
CHEMBL5175865 IC50 = 200.0 nM 6.70
CHEMBL5188828 IC50 = 500.0 nM 6.30
CHEMBL5205052 IC50 = 500.0 nM 6.30
CHEMBL5187305 IC50 = 600.0 nM 6.22
CHEMBL5194144 IC50 = 1500.0 nM 5.82
CHEMBL5196820 IC50 = 1600.0 nM 5.80
CHEMBL5186424 IC50 = 1800.0 nM 5.75
CHEMBL5183220 IC50 = 2090.0 nM 5.68
CHEMBL5181626 IC50 = 2180.0 nM 5.66
CHEMBL5169588 IC50 = 2500.0 nM 5.60
CHEMBL5172975 IC50 = 3400.0 nM 5.47
CHEMBL5196169 IC50 = 3600.0 nM 5.44
CHEMBL5194882 IC50 = 3800.0 nM 5.42
CHEMBL5196273 IC50 = 4200.0 nM 5.38
CHEMBL5201318 IC50 = 4600.0 nM 5.34
CHEMBL280998 CATECHOL IC50 = 5000.0 nM 5.30
CHEMBL81398 IC50 = 353000.0 nM -
CHEMBL5173734 IC50 - -
CHEMBL52209 IC50 = 772000.0 nM -
CHEMBL70927 DEFERIPRONE IC50 - -
CHEMBL1235568 IC50 - -
CHEMBL1649594 IC50 - -
CHEMBL5194795 IC50 - -
CHEMBL1650621 IC50 - -
CHEMBL1650620 IC50 - -
CHEMBL61236 IC50 - -
CHEMBL310555 OXYQUINOLINE IC50 = 208000.0 nM -
CHEMBL1368601 IC50 = 203000.0 nM -
CHEMBL99932 8-AMINOQUINOLINE IC50 - -
CHEMBL79857 IC50 = 232000.0 nM -
CHEMBL275066 IC50 - -
CHEMBL5185768 IC50 = 144000.0 nM -
CHEMBL5182535 IC50 - -
CHEMBL574699 BARBITURIC ACID IC50 - -