ChEMBL ligand: CHEMBL4111094
Beta-hexosaminidase subunit beta in Human [ChEMBL: CHEMBL5877] [UniProtKB: P07686] There should be some charts here, you may need to enable JavaScript!
O-GlcNAcase/Bifunctional protein NCOAT in Human [ChEMBL: CHEMBL5921] [GtoPdb: 3101] [UniProtKB: O60502] O-GlcNAcase in Rat [GtoPdb: 3101] [UniProtKB: Q8VIJ5] There should be some charts here, you may need to enable JavaScript!
O-GlcNAcase in Human [GtoPdb: 3101] [UniProtKB: O60502] O-GlcNAcase/Protein O-GlcNAcase in Rat [ChEMBL: CHEMBL3351213] [GtoPdb: 3101] [UniProtKB: Q8VIJ5] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Beta-hexosaminidase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5877] [UniProtKB: P07686]
ChEMBL	Inhibition of human beta hexosaminidase assessed as inhibitory constant using 4-methylumbelliferyl N-acetyl-beta-D-glucosaminide dihydrate as substrate measured every 60 sec for 45 mins by fluorescence spectrophotometry	B	5	pKi	>10000	nM	Ki	J Med Chem (2019) 62: 10062-10097 [PMID:31487175]
O-GlcNAcase/Bifunctional protein NCOAT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5921] [GtoPdb: 3101] [UniProtKB: O60502]
GtoPdb	In vitro enzyme inhibition assay.	-	8.1	pKi	7.9	nM	Ki	J Med Chem (2019) 62: 10062-10097 [PMID:31487175]
ChEMBL	Inhibition of recombinant human OGA	B	8.1	pKi	7.9	nM	Ki	J Med Chem (2019) 62: 10062-10097 [PMID:31487175]
ChEMBL	null: Enzymatic reactions were carried out in a reaction containing 50 mM NaH2PO4, 100 mM NaCl and 0.1% BSA (pH 7.0) using 2 mM 4-Methylumbelliferyl N-acetyl-β-D-glucosaminide dihydrate (Sigma M2133) dissolved in ddH2O, as a substrate. The amount of purified human O-GlcNAcase enzyme used in the reaction was 0.7 nM. Test compound of varying concentrations was added to the enzyme prior to initiation of the reaction. The reaction was performed at room temperature in a 96-well plate and was initiated with the addition of substrate. The production of fluorescent product was measured every 60 sec for 45 min with a Tecan Infinite M200 plate-reader with excitation at 355 nM and emission detected at 460 nM, with 4-Methylumbelliferone (Sigma M1381) used to produce a standard curve.	B	8.24	pKi	5.7	nM	Ki	US-9243020-B2. Selective glycosidase inhibitors and uses thereof (2016)
ChEMBL	Inhibition of human O-GlcNAcase	B	8.1	pIC50	7.9	nM	IC50	J Med Chem (2019) 62: 10059-10061 [PMID:31668062]
ChEMBL	Cell-based ELISA Assay: The ELISA portion of the assay was performed in a black Maxisorp 96-well plate that was coated overnight at 4° C. with 100 uL/well of the cell lysate (1:10 dilution of the lysate with PBS containing protease inhibitors, phosphatase inhibitors, and PMSF). The following day the wells were washed 3 times with 300 uL/well of Wash buffer (Tris-buffered saline with 0.1% Tween 20). The wells were blocked with 100 ul/well Blocking buffer (Tris buffered saline w/0.05% Tween 20 and 2.5% Bovine serum albumin). Each well was then washed two times with 300 uL/well of wash buffer. The anti O-GlcNAc antibody RL-2 (Abeam, Cambridge, Mass.), diluted 1:1000 in blocking buffer, was added at 100 uL/well. The plate was sealed and incubated at 37° C. for 2 h with gentle shaking. The wells were then washed 3-times with 300 uL/well wash buffer. To detect the amount of RL-2 bound horse-radish peroxidase (HRP) conjugated goat anti-mouse secondary antibody (diluted 1:3000 in blocking buffer) was added at100 uL/well. The plate was incubated for 60 min at 37° C. with gentle shaking. Each well was then washed 3-times with 300 uL/well wash buffer. The detection reagent was added, 100 uL/well of Amplex Ultra RED reagent (prepared by adding 30 uL of 10 mM Amplex Ultra Red stock solution to 10 mL PBS with 18 uL 3% hydrogen peroxide, H2O2). The detection reaction was incubated for 15 minutes at room temperature and then read with excitation at 530 nm and emission at 590 nm.	B	7.28	pEC50	53	nM	EC50	US-9243020-B2. Selective glycosidase inhibitors and uses thereof (2016)
O-GlcNAcase in Rat [GtoPdb: 3101] [UniProtKB: Q8VIJ5]
GtoPdb	Determined in an ELISA-based assay with rat PC12 cells to measure EC50 values for elevation of all protein O-GlcNAc levels in the presence of test compound.	-	7.28	pEC50	52.7	nM	EC50	J Med Chem (2019) 62: 10062-10097 [PMID:31487175]
O-GlcNAcase in Human [GtoPdb: 3101] [UniProtKB: O60502]
GtoPdb	In vitro enzyme inhibition assay.	-	8.1	pKi	7.9	nM	Ki	J Med Chem (2019) 62: 10062-10097 [PMID:31487175]
O-GlcNAcase/Protein O-GlcNAcase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351213] [GtoPdb: 3101] [UniProtKB: Q8VIJ5]
ChEMBL	Inhibition of OGA in rat PC12 cells assessed as OGlcNAcylated protein level incubated for 24 hrs by ELISA	B	7.28	pEC50	52.7	nM	EC50	J Med Chem (2019) 62: 10062-10097 [PMID:31487175]
GtoPdb	Determined in an ELISA-based assay with rat PC12 cells to measure EC50 values for elevation of all protein O-GlcNAc levels in the presence of test compound.	-	7.28	pEC50	52.7	nM	EC50	J Med Chem (2019) 62: 10062-10097 [PMID:31487175]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]