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Assay Detail

CHEMBL5512154

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

Binding
Inhibition of sQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader
ChEMBL ↗
56
Total Activities
56
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

X-ray Structure-Guided Discovery of a Potent Benzimidazole Glutaminyl Cyclase Inhibitor That Shows Activity in a Parkinson's Disease Mouse Model.
Mou J, Ning XL, Wang XY, Hou SY, Meng FB, Zhou C, Wu JW, Li C, Jia T, Wu X, Wu Y, Chen Y, Li GB.
J Med Chem (2024) 67 : 8730 -8756
PubMed 38817193 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 6.15 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4462495 — — 1 10.28
CHEMBL5559845 — — 1 8.35
CHEMBL5193156 — — 1 7.92
CHEMBL5527908 — — 1 7.92
CHEMBL5518036 — — 1 7.60
CHEMBL5560683 — — 1 7.47
CHEMBL5560391 — — 1 7.46
CHEMBL3659477 VAROGLUTAMSTAT 2.0 1 7.44
CHEMBL5555409 — — 1 7.33
CHEMBL5566962 — — 1 7.31
CHEMBL5561959 — — 1 7.29
CHEMBL5561339 — — 1 7.29
CHEMBL5560058 — — 1 7.28
CHEMBL5564558 — — 1 7.23
CHEMBL5537088 — — 1 6.92
CHEMBL201747 — — 1 6.66
CHEMBL5568265 — — 1 6.54
CHEMBL5556470 — — 1 6.47
CHEMBL5561191 — — 1 6.44
CHEMBL5531968 — — 1 6.42
CHEMBL5555768 — — 1 6.41
CHEMBL5559543 — — 1 6.39
CHEMBL5564379 — — 1 6.28
CHEMBL5560570 — — 1 6.28
CHEMBL5556007 — — 1 6.12
CHEMBL5517915 — — 1 6.11
CHEMBL5523426 — — 1 6.07
CHEMBL5559912 — — 1 5.93
CHEMBL5565896 — — 1 5.72
CHEMBL5559655 — — 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4462495 — IC50 = 0.053 nM 10.28
CHEMBL5559845 — IC50 = 4.5 nM 8.35
CHEMBL5527908 — IC50 = 12.0 nM 7.92
CHEMBL5193156 — IC50 = 12.0 nM 7.92
CHEMBL5518036 — IC50 = 25.0 nM 7.60
CHEMBL5560683 — IC50 = 33.9 nM 7.47
CHEMBL5560391 — IC50 = 35.0 nM 7.46
CHEMBL3659477 VAROGLUTAMSTAT IC50 = 36.0 nM 7.44
CHEMBL5555409 — IC50 = 47.0 nM 7.33
CHEMBL5566962 — IC50 = 49.0 nM 7.31
CHEMBL5561959 — IC50 = 51.0 nM 7.29
CHEMBL5561339 — IC50 = 51.0 nM 7.29
CHEMBL5560058 — IC50 = 53.0 nM 7.28
CHEMBL5564558 — IC50 = 59.0 nM 7.23
CHEMBL5537088 — IC50 = 120.0 nM 6.92
CHEMBL201747 — IC50 = 220.0 nM 6.66
CHEMBL5568265 — IC50 = 290.0 nM 6.54
CHEMBL5556470 — IC50 = 340.0 nM 6.47
CHEMBL5561191 — IC50 = 360.0 nM 6.44
CHEMBL5531968 — IC50 = 380.0 nM 6.42
CHEMBL5555768 — IC50 = 390.0 nM 6.41
CHEMBL5559543 — IC50 = 410.0 nM 6.39
CHEMBL5564379 — IC50 = 530.0 nM 6.28
CHEMBL5560570 — IC50 = 520.0 nM 6.28
CHEMBL5556007 — IC50 = 760.0 nM 6.12
CHEMBL5517915 — IC50 = 770.0 nM 6.11
CHEMBL5523426 — IC50 = 850.0 nM 6.07
CHEMBL5559912 — IC50 = 1180.0 nM 5.93
CHEMBL5565896 — IC50 = 1900.0 nM 5.72
CHEMBL5559655 — IC50 = 1920.0 nM 5.72
CHEMBL5556737 — IC50 = 2210.0 nM 5.66
CHEMBL5559993 — IC50 = 2200.0 nM 5.66
CHEMBL5542283 — IC50 = 2240.0 nM 5.65
CHEMBL5532102 — IC50 = 2250.0 nM 5.65
CHEMBL5568222 — IC50 = 2430.0 nM 5.61
CHEMBL5555505 — IC50 = 2490.0 nM 5.60
CHEMBL5557682 — IC50 = 2600.0 nM 5.58
CHEMBL5558976 — IC50 = 2870.0 nM 5.54
CHEMBL5566006 — IC50 = 3870.0 nM 5.41
CHEMBL5532405 — IC50 = 3940.0 nM 5.41
CHEMBL5564421 — IC50 = 4040.0 nM 5.39
CHEMBL5567679 — IC50 = 4220.0 nM 5.38
CHEMBL5568345 — IC50 = 4980.0 nM 5.30
CHEMBL5565074 — IC50 = 7030.0 nM 5.15
CHEMBL5568447 — IC50 = 15440.0 nM 4.81
CHEMBL5560506 — IC50 = 17700.0 nM 4.75
CHEMBL5561371 — IC50 = 21840.0 nM 4.66
CHEMBL5557644 — IC50 = 22930.0 nM 4.64
CHEMBL5557925 — IC50 = 32330.0 nM 4.49
CHEMBL5556534 — IC50 = 33000.0 nM 4.48