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Assay Detail

CHEMBL4355755

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

Binding
Inhibition of OGA in rat PC12 cells assessed as OGlcNAcylated protein level incubated for 24 hrs by ELISA
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein O-GlcNAcase (CHEMBL3351213)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.
Selnick HG, Hess JF, Tang C, Liu K, Schachter JB, Ballard JE, Marcus J, Klein DJ, Wang X, Pearson M, Savage MJ, Kaul R, Li TS, Vocadlo DJ, Zhou Y, Zhu Y, Mu C, Wang Y, Wei Z, Bai C, Duffy JL, McEachern EJ.
J Med Chem (2019) 62 : 10062 -10097
PubMed 31487175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 7.00 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4443587 1 8.77
CHEMBL4444446 1 7.97
CHEMBL1213603 1 7.87
CHEMBL4545886 1 7.55
CHEMBL4113501 1 7.51
CHEMBL4516713 1 7.48
CHEMBL4108795 1 7.46
CHEMBL4483089 1 7.43
CHEMBL4561925 1 7.38
CHEMBL4111094 1 7.28
CHEMBL3897809 1 7.24
CHEMBL4586062 1 6.92
CHEMBL3681909 1 6.82
CHEMBL3686728 1 6.78
CHEMBL4543991 1 6.75
CHEMBL4473252 1 6.75
CHEMBL4454814 1 6.65
CHEMBL4112447 1 6.51
CHEMBL4476839 1 6.48
CHEMBL4110365 1 6.45
CHEMBL4107048 1 6.44
CHEMBL4448352 1 6.35
CHEMBL4583010 1 6.35
CHEMBL4456515 1 6.29
CHEMBL4513613 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4443587 EC50 = 1.71 nM 8.77
CHEMBL4444446 EC50 = 10.6 nM 7.97
CHEMBL1213603 EC50 = 13.5 nM 7.87
CHEMBL4545886 EC50 = 28.0 nM 7.55
CHEMBL4113501 EC50 = 31.2 nM 7.51
CHEMBL4516713 EC50 = 33.1 nM 7.48
CHEMBL4108795 EC50 = 34.4 nM 7.46
CHEMBL4483089 EC50 = 36.7 nM 7.43
CHEMBL4561925 EC50 = 41.4 nM 7.38
CHEMBL4111094 EC50 = 52.7 nM 7.28
CHEMBL3897809 EC50 = 58.2 nM 7.24
CHEMBL4586062 EC50 = 119.0 nM 6.92
CHEMBL3681909 EC50 = 152.0 nM 6.82
CHEMBL3686728 EC50 = 165.0 nM 6.78
CHEMBL4543991 EC50 = 176.0 nM 6.75
CHEMBL4473252 EC50 = 177.0 nM 6.75
CHEMBL4454814 EC50 = 224.0 nM 6.65
CHEMBL4112447 EC50 = 307.0 nM 6.51
CHEMBL4476839 EC50 = 328.0 nM 6.48
CHEMBL4110365 EC50 = 358.0 nM 6.45
CHEMBL4107048 EC50 = 364.0 nM 6.44
CHEMBL4448352 EC50 = 443.0 nM 6.35
CHEMBL4583010 EC50 = 445.0 nM 6.35
CHEMBL4456515 EC50 = 509.0 nM 6.29
CHEMBL4513613 EC50 = 2400.0 nM 5.62