DZNep [Ligand Id: 8392] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL154745 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| S-Adenosylhomocysteine hydrolase/Adenosylhomocysteinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2664] [GtoPdb: 1233] [UniProtKB: P23526] | ||||||||
| ChEMBL | Inhibition of SAH hydrolase (unknown origin) assessed as inhibition constant | B | 11 | pKi | 0.01 | nM | Ki | J Med Chem (2022) 65: 7016-7043 [PMID:35531606] |
| ChEMBL | Inhibition of recombinant human placental AdoHcy hydrolase expressed in Escherichia coli BL21 using AdoHcy as substrate preincubated for 10 mins followed by substrate addition measured after 20 mins by DTNB coupled assay | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (2015) 58: 5108-5120 [PMID:26010585] |
| S-Adenosylhomocysteine hydrolase in Hamster [GtoPdb: 1233] | ||||||||
| GtoPdb | Inhibition of a SAHH preparation isolated from hamster liver. | - | 12.3 | pKi | 0 | nM | Ki | Biochem Biophys Res Commun (1986) 135: 688-94 [PMID:3457563] |
| AdoHcyase_NAD domain-containing protein in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295548] [UniProtKB: G1SVH0] | ||||||||
| ChEMBL | S-Adenosylhomocysteine Hydrolase (SAHase) Inhibition: As a consequence of "D"-Isoneplanocin and "L"-Isoneplanocin, being isomers of Neplanocin A, which on one hand is a potent inhibitor of S-adenosylhomocysteine hydrolase (SAHase), a mechanism agreed upon as one source of its antiviral activity and on the other hand thought to contribute to cytotoxicity, the inhibitory efficiency on SAHase activity was assayed (source: rabbit erythrocytes). The inhibition of SAHase activity can be quantitated by the release of free homocysteine. SAHase from rabbit erythrocytes (Sigma) is dialyzed at 4° C. for 2 h in a buffer containing 20% glycerol and 50 mM potassium phosphate pH 7.4. The presence of adenosine deaminase insures that the reaction will proceed in the forward (hydrolysis) direction only. The enzyme preparation is incubated with or without the target compounds at different concentrations in 50 mM potassium phosphate buffer pH 7.4 for 5 minutes at 37° C. before SAH is added. The formation of homocysteine is detected using the Measure-iT thiol quantitation reagent according to the manufacturer's instructions (Life technologies, Carlsbad, Calif.). Plates are read on Spectra Max M2 (Molecular Devices). | B | 8.5 | pIC50 | 3.19 | nM | IC50 | US-10227373-B2. Enantiomers of the 1′,6′-isomer of neplanocin A (2019) |
| enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910] | ||||||||
| ChEMBL | Inhibition of EZH2 (unknown origin) | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2022) 65: 7016-7043 [PMID:35531606] |
ChEMBL data shown on this page come from version 36:
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]
