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Assay Detail

CHEMBL5149904

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

Binding
Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis
24
Total Activities
24
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-like protein (CHEMBL3638349)
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 24 6.51 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5193156 1 7.14
CHEMBL5202172 1 7.14
CHEMBL5204178 1 6.98
CHEMBL5174554 1 6.82
CHEMBL5195495 1 6.80
CHEMBL5190683 1 6.76
CHEMBL5202004 1 6.76
CHEMBL5181839 1 6.70
CHEMBL5197396 1 6.66
CHEMBL5207620 1 6.62
CHEMBL5194983 1 6.53
CHEMBL5181626 1 6.53
CHEMBL5186970 1 6.47
CHEMBL201747 1 6.46
CHEMBL5178150 1 6.45
CHEMBL5174441 1 6.45
CHEMBL5188828 1 6.38
CHEMBL5187305 1 6.29
CHEMBL5205052 1 5.90
CHEMBL5198938 1 5.72
CHEMBL5175865 1 5.15
CHEMBL5182535 1 -
CHEMBL5185768 1 -
CHEMBL275066 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5193156 IC50 = 73.0 nM 7.14
CHEMBL5202172 IC50 = 72.0 nM 7.14
CHEMBL5204178 IC50 = 104.0 nM 6.98
CHEMBL5174554 IC50 = 152.0 nM 6.82
CHEMBL5195495 IC50 = 157.0 nM 6.80
CHEMBL5190683 IC50 = 173.0 nM 6.76
CHEMBL5202004 IC50 = 172.0 nM 6.76
CHEMBL5181839 IC50 = 202.0 nM 6.70
CHEMBL5197396 IC50 = 219.0 nM 6.66
CHEMBL5207620 IC50 = 239.0 nM 6.62
CHEMBL5194983 IC50 = 297.0 nM 6.53
CHEMBL5181626 IC50 = 298.0 nM 6.53
CHEMBL5186970 IC50 = 342.0 nM 6.47
CHEMBL201747 IC50 = 351.0 nM 6.46
CHEMBL5178150 IC50 = 359.0 nM 6.45
CHEMBL5174441 IC50 = 353.0 nM 6.45
CHEMBL5188828 IC50 = 414.0 nM 6.38
CHEMBL5187305 IC50 = 514.0 nM 6.29
CHEMBL5205052 IC50 = 1249.0 nM 5.90
CHEMBL5198938 IC50 = 1900.0 nM 5.72
CHEMBL5175865 IC50 = 7028.0 nM 5.15
CHEMBL5182535 IC50 - -
CHEMBL5185768 IC50 - -
CHEMBL275066 IC50 - -