Protein Information

General Information of the Protein

Protein ID	PT01962
Protein Name	Protein O-GlcNAcase
Secondarily Protein Name	Beta-N-acetylglucosaminidase Beta-N-acetylhexosaminidase Beta-hexosaminidase Meningioma-expressed antigen 5 N-acetyl-beta-D-glucosaminidase N-acetyl-beta-glucosaminidase Nuclear cytoplasmic O-GlcNAcase and acetyltransferase
Gene Name	OGA
Secondarily Gene Name	HEXC KIAA0679 MEA5 MGEA5
Sequence	MVQKESQATLEERESELSSNPAASAGASLEPPAAPAPGEDNPAGAGGAAVAGAAGGARRFLCGVVEGFYGRPWVMEQRKELFRRLQKWELNTYLYAPKDDYKHRMFWREMYSVEEAEQLMTLISAAREYEIEFIYAISPGLDITFSNPKEVSTLKRKLDQVSQFGCRSFALLFDDIDHNMCAADKEVFSSFAHAQVSITNEIYQYLGEPETFLFCPTEYCGTFCYPNVSQSPYLRTVGEKLLPGIEVLWTGPKVVSKEIPVESIEEVSKIIKRAPVIWDNIHANDYDQKRLFLGPYKGRSTELIPRLKGVLTNPNCEFEANYVAIHTLATWYKSNMNGVRKDVVMTDSEDSTVSIQIKLENEGSDEDIETDVLYSPQMALKLALTEWLQEFGVPHQYSSRQVAHSGAKASVVDGTPLVAAPSLNATTVVTTVYQEPIMSQGAALSGEPTTLTKEEEKKQPDEEPMDMVVEKQEETDHKNDNQILSEIVEAKMAEELKPMDTDKESIAESKSPEMSMQEDCISDIAPMQTDEQTNKEQFVPGPNEKPLYTAEPVTLEDLQLLADLFYLPYEHGPKGAQMLREFQWLRANSSVVSVNCKGKDSEKIEEWRSRAAKFEEMCGLVMGMFTRLSNCANRTILYDMYSYVWDIKSIMSMVKSFVQWLGCRSHSSAQFLIGDQEPWAFRGGLAGEFQRLLPIDGANDLFFQPPPLTPTSKVYTIRPYFPKDEASVYKICREMYDDGVGLPFQSQPDLIGDKLVGGLLSLSLDYCFVLEDEDGICGYALGTVDVTPFIKKCKISWIPFMQEKYTKPNGDKELSEAEKIMLSFHEEQEVLPETFLANFPSLIKMDIHKKVTDPSVAKSMMACLLSSLKANGSRGAFCEVRPDDKRILEFYSKLGCFEIAKMEGFPKDVVILGRSL Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme
Function	Cleaves GlcNAc but not GalNAc from O-glycosylated proteins. Can use p-nitrophenyl-beta-GlcNAc and 4-methylumbelliferone-GlcNAc as substrates but not p-nitrophenyl-beta-GalNAc or p-nitrophenyl-alpha-GlcNAc (in vitro) (PubMed:11148210). Does not bind acetyl-CoA and does not have histone acetyltransferase activity (PubMed:24088714). Show/Hide
Uniprot ID	Primary ID: O60502 Secondarily ID: B7WPB9 D3DR79 E9PGF9 O75166 Q86WV0 Q8IV98 Q9BVA5 Q9HAR0 Show/Hide
Ensembl ID	ENSG00000198408
HGNC ID	HGNC:7056
Subcellular Location	Nucleus

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000006 , HEK293

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0444119 Compound Info	4-(4-methylpiperidin-1-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine Show/Hide	C16H21N5	1
1	IC50 = 18 nM Bioactivity Info	TI LI LO TS
CP0444117 Compound Info	4-(4-methylpiperidin-1-yl)-N-(2-phenylethyl)pyrimidin-2-amine Show/Hide	C18H24N4	1
1	IC50 = 24 nM Bioactivity Info	TI LI LO TS
CP0495620 Compound Info	4-(4-methylpiperidin-1-yl)-N-(2-pyridin-3-ylethyl)pyrimidin-2-amine Show/Hide	C17H23N5	1
1	IC50 = 31 nM Bioactivity Info	TI LI LO TS
CP0549571 Compound Info	N-[1-(4-methylpiperazin-1-yl)propan-2-yl]-4-(4-methylpiperidin-1-yl)pyrimidin-2-amine Show/Hide	C18H32N6	1
1	IC50 = 41 nM Bioactivity Info	TI LI LO TS
CP0573035 Compound Info	N-[5-[[2-(4,6-dimethylpyridin-2-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	1
1	IC50 = 46 nM Bioactivity Info	TI LI LO TS
CP0495621 Compound Info	N-[(1-methylimidazol-4-yl)methyl]-4-(4-methylpiperidin-1-yl)pyrimidin-2-amine Show/Hide	C15H22N6	1
1	IC50 = 46 nM Bioactivity Info	TI LI LO TS
CP0553231 Compound Info	N-[5-[[2-(2-methoxy-6-methylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5O2S	1
1	IC50 = 56 nM Bioactivity Info	TI LI LO TS
CP0225389 Compound Info	N-[5-[[2-(2,5-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	1
1	IC50 = 77.62 nM Bioactivity Info	TI LI LO TS
CP0471574 Compound Info	N-[5-[[2-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	2
1	IC50 = 141 nM Bioactivity Info	TI LI LO TS
2	IC50 = 141.25 nM Bioactivity Info	TI LI LO TS
CP0160370 Compound Info	N-[5-[[2-[2-methyl-5-(trifluoromethyl)pyridin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H24F3N5OS	1
1	IC50 = 147.91 nM Bioactivity Info	TI LI LO TS
CP0519318 Compound Info	N-[5-[[2-(2,6-dimethylpyrimidin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C19H26N6OS	2
1	IC50 = 169.82 nM Bioactivity Info	TI LI LO TS
2	IC50 = 170 nM Bioactivity Info	TI LI LO TS
CP0532966 Compound Info	N-[5-[[2-(2,6-dimethylpyridin-4-yl)-6-azaspiro[3.4]octan-6-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H26N4OS	1
1	IC50 = 182 nM Bioactivity Info	TI LI LO TS
CP0330307 Compound Info	N-[5-[[2-(3,5-dimethylpyridin-2-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	1
1	IC50 = 208.93 nM Bioactivity Info	TI LI LO TS
CP0533294 Compound Info	N-[5-[[8-(2,6-dimethylpyridin-4-yl)-2-azaspiro[4.4]nonan-2-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C21H28N4OS	1
1	IC50 = 214 nM Bioactivity Info	TI LI LO TS
CP0575918 Compound Info	CHEMBL4791287 Show/Hide	C21H28N4OS	1
1	IC50 = 240 nM Bioactivity Info	TI LI LO TS
CP0571041 Compound Info	N-[5-[[(5S)-2-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	1
1	IC50 = 281.84 nM Bioactivity Info	TI LI LO TS
CP0486711 Compound Info	CHEMBL4757711 Show/Hide	C21H28N4OS	1
1	IC50 = 295 nM Bioactivity Info	TI LI LO TS
CP0565748 Compound Info	4-(4-methylpiperidin-1-yl)-N-(2-pyridin-2-ylethyl)pyrimidin-2-amine Show/Hide	C17H23N5	1
1	IC50 = 360 nM Bioactivity Info	TI LI LO TS
CP0471573 Compound Info	N-[5-[[2-[2-methyl-6-(trifluoromethyl)pyridin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H24F3N5OS	1
1	IC50 = 380 nM Bioactivity Info	TI LI LO TS
CP0557292 Compound Info	5-[1-[7-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-2-yl]ethyl]-2-methyl-1,3-benzothiazole Show/Hide	C24H30N4S	1
1	IC50 = 380.19 nM Bioactivity Info	TI LI LO TS
CP0426275 Compound Info	N-[5-[[2-(5-methylimidazo[1,2-a]pyrimidin-7-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H25N7OS	1
1	IC50 = 437 nM Bioactivity Info	TI LI LO TS
CP0533292 Compound Info	N-[5-[[8-[(2,6-dimethylpyridin-4-yl)oxymethyl]-2-azaspiro[4.4]nonan-2-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C22H30N4O2S	1
1	IC50 = 501 nM Bioactivity Info	TI LI LO TS
CP0486712 Compound Info	N-[5-[[8-[(2,6-dimethylpyridin-4-yl)methyl]-2-azaspiro[4.4]nonan-2-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C22H30N4OS	1
1	IC50 = 537 nM Bioactivity Info	TI LI LO TS
CP0533293 Compound Info	N-[5-[[(3S,5S)-3-(2,6-dimethylpyridin-4-yl)oxy-1-oxa-7-azaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H26N4O3S	1
1	IC50 = 537 nM Bioactivity Info	TI LI LO TS
CP0572974 Compound Info	N-[5-[[2-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C19H24N8OS	1
1	IC50 = 575 nM Bioactivity Info	TI LI LO TS
CP0573034 Compound Info	N-[5-[[3-(2,6-dimethylpyridin-4-yl)-1-oxa-7-azaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H26N4O2S	1
1	IC50 = 603 nM Bioactivity Info	TI LI LO TS
CP0532282 Compound Info	4-(4-methoxypiperidin-1-yl)-N-(2-phenylethyl)pyrimidin-2-amine Show/Hide	C18H24N4O	1
1	IC50 = 970 nM Bioactivity Info	TI LI LO TS
CP0523224 Compound Info	N-[5-[[2-(6-cyclopropylpyrazin-2-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H26N6OS	1
1	IC50 = 1000 nM Bioactivity Info	TI LI LO TS
CP0560997 Compound Info	4-morpholin-4-yl-N-(2-phenylethyl)pyrimidin-2-amine Show/Hide	C16H20N4O	1
1	IC50 = 4700 nM Bioactivity Info	TI LI LO TS
CP0532967 Compound Info	N-[5-[[2-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-2,7-diazaspiro[3.4]octan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C18H22N8OS	1
1	IC50 = 9333 nM Bioactivity Info	TI LI LO TS
CP0436019 Compound Info	6-[[(5R)-2-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]quinoxaline Show/Hide	C23H27N5	1
1	IC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0528317 Compound Info	7-(2,7-diazaspiro[4.4]nonan-2-yl)-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine Show/Hide	C13H18N6	1
1	IC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0535147 Compound Info	N-[5-[[7-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-2,7-diazaspiro[3.4]octan-2-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C18H22N8OS	1
1	IC50 = 10000 nM Bioactivity Info	TI LI LO TS
CP0535148 Compound Info	6-[[2-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]quinoxaline Show/Hide	C22H24N8	1
1	IC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0516924 Compound Info	4-(4-methylpiperazin-1-yl)-N-(2-phenylethyl)pyrimidin-2-amine Show/Hide	C17H23N5	1
1	IC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0561816 Compound Info	1-[2-(2-phenylethylamino)pyrimidin-4-yl]piperidin-4-ol Show/Hide	C17H22N4O	1
1	IC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0571042 Compound Info	2-[1-(2,3-dihydro-1,4-benzodioxin-6-yl)ethyl]-7-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonane Show/Hide	C24H31N3O2	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0533295 Compound Info	7-[7-(1,3-benzodioxol-5-ylmethyl)-2,7-diazaspiro[4.4]nonan-2-yl]-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine Show/Hide	C21H24N6O2	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0553232 Compound Info	2-methyl-5-[[2-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-benzothiazole Show/Hide	C22H25N7S	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000004 , SH-SY5Y

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0495621 Compound Info	N-[(1-methylimidazol-4-yl)methyl]-4-(4-methylpiperidin-1-yl)pyrimidin-2-amine Show/Hide	C15H22N6	2
1	EC50 ~ 450 nM
2	IC50 ~ 46 nM
CP0571041 Compound Info	N-[5-[[(5S)-2-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	1
1	IC50 = 3.715 nM
CP0330307 Compound Info	N-[5-[[2-(3,5-dimethylpyridin-2-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	1
1	IC50 = 3.89 nM
CP0471574 Compound Info	N-[5-[[2-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	1
1	IC50 = 6.026 nM
CP0519318 Compound Info	N-[5-[[2-(2,6-dimethylpyrimidin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C19H26N6OS	1
1	IC50 = 13.18 nM
CP0225389 Compound Info	N-[5-[[2-(2,5-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H27N5OS	1
1	IC50 = 13.49 nM
CP0557292 Compound Info	5-[1-[7-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-2-yl]ethyl]-2-methyl-1,3-benzothiazole Show/Hide	C24H30N4S	1
1	IC50 = 18.2 nM
CP0523224 Compound Info	N-[5-[[2-(6-cyclopropylpyrazin-2-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H26N6OS	1
1	IC50 = 20.42 nM
CP0160370 Compound Info	N-[5-[[2-[2-methyl-5-(trifluoromethyl)pyridin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]-1,3-thiazol-2-yl]acetamide Show/Hide	C20H24F3N5OS	1
1	IC50 = 36.31 nM
CP0571042 Compound Info	2-[1-(2,3-dihydro-1,4-benzodioxin-6-yl)ethyl]-7-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonane Show/Hide	C24H31N3O2	1
1	IC50 = 181.97 nM
CP0436019 Compound Info	6-[[(5R)-2-(2,6-dimethylpyridin-4-yl)-2,7-diazaspiro[4.4]nonan-7-yl]methyl]quinoxaline Show/Hide	C23H27N5	1
1	IC50 = 223.87 nM
CP0516924 Compound Info	4-(4-methylpiperazin-1-yl)-N-(2-phenylethyl)pyrimidin-2-amine Show/Hide	C17H23N5	1
1	IC50 > 10000 nM

Clinical Information about the Protein

Target 1 ( Beta-N-acetylhexosaminidase (OGA) )

Target Type	Clinical trial Target
Disease	1 Target-related Disease				1
1	Progressive supranuclear palsy [ICD-11: 8A00.10]
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	MK-8719	Drug Info	Phase 1	Progressive supranuclear palsy

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han