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Assay Detail

CHEMBL4355754

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Binding
Inhibition of recombinant human OGA
ChEMBL ↗
48
Total Activities
48
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 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
Ki 48 7.61 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4443587 — — 1 9.44
CHEMBL1213603 — — 1 9.39
CHEMBL4444446 — — 1 9.28
CHEMBL4108795 — — 1 9.26
CHEMBL4113501 — — 1 8.62
CHEMBL3681909 — — 1 8.55
CHEMBL4112447 — — 1 8.52
CHEMBL4545886 — — 1 8.48
CHEMBL4561925 — — 1 8.28
CHEMBL4483089 — — 1 8.26
CHEMBL4456515 — — 1 8.25
CHEMBL4111094 — — 1 8.10
CHEMBL4473252 — — 1 8.05
CHEMBL4516713 — — 1 8.03
CHEMBL4110365 — — 1 7.96
CHEMBL3686728 — — 1 7.89
CHEMBL4586062 — — 1 7.85
CHEMBL4583010 — — 1 7.85
CHEMBL4543991 — — 1 7.70
CHEMBL3897809 — — 1 7.64
CHEMBL4453820 — — 1 7.58
CHEMBL4113968 — — 1 7.55
CHEMBL4448352 — — 1 7.54
CHEMBL4476839 — — 1 7.46
CHEMBL4576476 — — 1 7.39
CHEMBL4107048 — — 1 7.36
CHEMBL4454814 — — 1 7.30
CHEMBL4465511 — — 1 7.30
CHEMBL4436228 — — 1 7.24
CHEMBL4110677 — — 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4443587 — Ki = 0.36 nM 9.44
CHEMBL1213603 — Ki = 0.41 nM 9.39
CHEMBL4444446 — Ki = 0.53 nM 9.28
CHEMBL4108795 — Ki = 0.55 nM 9.26
CHEMBL4113501 — Ki = 2.4 nM 8.62
CHEMBL3681909 — Ki = 2.8 nM 8.55
CHEMBL4112447 — Ki = 3.0 nM 8.52
CHEMBL4545886 — Ki = 3.3 nM 8.48
CHEMBL4561925 — Ki = 5.3 nM 8.28
CHEMBL4483089 — Ki = 5.5 nM 8.26
CHEMBL4456515 — Ki = 5.6 nM 8.25
CHEMBL4111094 — Ki = 7.9 nM 8.10
CHEMBL4473252 — Ki = 9.0 nM 8.05
CHEMBL4516713 — Ki = 9.4 nM 8.03
CHEMBL4110365 — Ki = 11.0 nM 7.96
CHEMBL3686728 — Ki = 13.0 nM 7.89
CHEMBL4586062 — Ki = 14.0 nM 7.85
CHEMBL4583010 — Ki = 14.0 nM 7.85
CHEMBL4543991 — Ki = 20.0 nM 7.70
CHEMBL3897809 — Ki = 23.0 nM 7.64
CHEMBL4453820 — Ki = 26.0 nM 7.58
CHEMBL4113968 — Ki = 28.0 nM 7.55
CHEMBL4448352 — Ki = 29.0 nM 7.54
CHEMBL4476839 — Ki = 35.0 nM 7.46
CHEMBL4576476 — Ki = 41.0 nM 7.39
CHEMBL4107048 — Ki = 44.0 nM 7.36
CHEMBL4454814 — Ki = 50.0 nM 7.30
CHEMBL4465511 — Ki = 50.0 nM 7.30
CHEMBL4436228 — Ki = 58.0 nM 7.24
CHEMBL4110677 — Ki = 69.0 nM 7.16
CHEMBL4541985 — Ki = 72.0 nM 7.14
CHEMBL4440249 — Ki = 74.0 nM 7.13
CHEMBL4449194 — Ki = 180.0 nM 6.75
CHEMBL4570378 — Ki = 190.0 nM 6.72
CHEMBL4470857 — Ki = 200.0 nM 6.70
CHEMBL4519186 — Ki = 270.0 nM 6.57
CHEMBL4513613 — Ki = 760.0 nM 6.12
CHEMBL4454942 — Ki = 960.0 nM 6.02
CHEMBL4465024 — Ki = 1200.0 nM 5.92
CHEMBL4446308 — Ki = 1700.0 nM 5.77
CHEMBL4530018 — Ki = 1800.0 nM 5.75
CHEMBL4577980 — Ki > 3000.0 nM -
CHEMBL3686726 — Ki > 3000.0 nM -
CHEMBL4520749 — Ki > 3000.0 nM -
CHEMBL4546366 — Ki > 3000.0 nM -
CHEMBL4554360 — Ki > 3000.0 nM -
CHEMBL4578331 — Ki > 3000.0 nM -
CHEMBL4552866 — Ki > 3000.0 nM -