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Assay Detail

CHEMBL5578801

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

Binding
Inhibition of GST-tagged human recombinant OGA using fuoresceinmono-beta-o-N-acetylglucosarnine as substrate incubated for 60 mins under dark condition by microplate reader based analysis
62
Total Activities
62
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

Protein O-GlcNAcase (CHEMBL5921)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4-(Arylethynyl)piperidine Derivatives as Potent Nonsaccharide <i>O</i>-GlcNAcase Inhibitors for the Treatment of Alzheimer's Disease.
Cheng Z, Shang N, Wang X, Kang Y, Zhou J, Lan J, Hu J, Peng Y, Xu B.
J Med Chem (2024) 67 : 14292 -14312
PubMed 39109492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 7.72 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5591488 1 9.47
CHEMBL5591695 1 9.37
CHEMBL5593700 1 9.14
CHEMBL5594475 1 9.07
CHEMBL5591879 1 8.81
CHEMBL5592778 1 8.76
CHEMBL5594221 1 8.74
CHEMBL5592978 1 8.67
CHEMBL5590780 1 8.52
CHEMBL5593511 1 8.49
CHEMBL5579695 1 8.46
CHEMBL5592385 1 8.44
CHEMBL5591089 1 8.43
CHEMBL5591704 1 8.36
CHEMBL5591551 1 8.33
CHEMBL5591513 1 8.31
CHEMBL5583946 1 8.26
CHEMBL5591099 1 8.10
CHEMBL5591460 1 8.06
CHEMBL5595991 1 8.06
CHEMBL5591200 1 8.05
CHEMBL5584048 1 8.05
CHEMBL5590193 1 8.02
CHEMBL5591950 1 7.99
CHEMBL5594139 1 7.97
CHEMBL5592023 1 7.92
CHEMBL5592284 1 7.80
CHEMBL5595937 1 7.79
CHEMBL5592814 1 7.71
CHEMBL5593028 1 7.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5591488 IC50 = 0.34 nM 9.47
CHEMBL5591695 IC50 = 0.43 nM 9.37
CHEMBL5593700 IC50 = 0.72 nM 9.14
CHEMBL5594475 IC50 = 0.85 nM 9.07
CHEMBL5591879 IC50 = 1.54 nM 8.81
CHEMBL5592778 IC50 = 1.73 nM 8.76
CHEMBL5594221 IC50 = 1.82 nM 8.74
CHEMBL5592978 IC50 = 2.13 nM 8.67
CHEMBL5590780 IC50 = 3.04 nM 8.52
CHEMBL5593511 IC50 = 3.25 nM 8.49
CHEMBL5579695 IC50 = 3.49 nM 8.46
CHEMBL5592385 IC50 = 3.61 nM 8.44
CHEMBL5591089 IC50 = 3.75 nM 8.43
CHEMBL5591704 IC50 = 4.36 nM 8.36
CHEMBL5591551 IC50 = 4.63 nM 8.33
CHEMBL5591513 IC50 = 4.93 nM 8.31
CHEMBL5583946 IC50 = 5.44 nM 8.26
CHEMBL5591099 IC50 = 7.99 nM 8.10
CHEMBL5591460 IC50 = 8.73 nM 8.06
CHEMBL5595991 IC50 = 8.76 nM 8.06
CHEMBL5591200 IC50 = 8.86 nM 8.05
CHEMBL5584048 IC50 = 8.88 nM 8.05
CHEMBL5590193 IC50 = 9.53 nM 8.02
CHEMBL5591950 IC50 = 10.27 nM 7.99
CHEMBL5594139 IC50 = 10.77 nM 7.97
CHEMBL5592023 IC50 = 12.16 nM 7.92
CHEMBL5592284 IC50 = 15.74 nM 7.80
CHEMBL5595937 IC50 = 16.04 nM 7.79
CHEMBL5592814 IC50 = 19.41 nM 7.71
CHEMBL5593028 IC50 = 22.52 nM 7.65
CHEMBL5591919 IC50 = 23.61 nM 7.63
CHEMBL5592529 IC50 = 23.89 nM 7.62
CHEMBL5593505 IC50 = 25.05 nM 7.60
CHEMBL5590863 IC50 = 25.88 nM 7.59
CHEMBL5595069 IC50 = 29.11 nM 7.54
CHEMBL5590741 IC50 = 32.34 nM 7.49
CHEMBL5591556 IC50 = 33.04 nM 7.48
CHEMBL5584000 IC50 = 33.76 nM 7.47
CHEMBL5594381 IC50 = 41.98 nM 7.38
CHEMBL5594264 IC50 = 42.68 nM 7.37
CHEMBL5590996 IC50 = 42.29 nM 7.37
CHEMBL5593786 IC50 = 43.29 nM 7.36
CHEMBL5591471 IC50 = 49.15 nM 7.31
CHEMBL5591664 IC50 = 51.41 nM 7.29
CHEMBL5583610 IC50 = 51.98 nM 7.28
CHEMBL5596027 IC50 = 53.63 nM 7.27
CHEMBL5583633 IC50 = 56.85 nM 7.25
CHEMBL5594901 IC50 = 57.38 nM 7.24
CHEMBL5593996 IC50 = 58.41 nM 7.23
CHEMBL5592062 IC50 = 62.52 nM 7.20