dexlansoprazole [Ligand Id: 5487] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1201863 (Dexilant, Dexilant solutab, Dexlansoprazole, Kapidex, Lansoprazole, (r)-, Lansoprazole r-form, NSC-758710, (r)-lansoprazole, T-168390, TAK-390)
  • Endo-beta-N-acetylglucosaminidase in Human [ChEMBL: CHEMBL5172] [UniProtKB: Q8NFI3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Endo-beta-N-acetylglucosaminidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5172] [UniProtKB: Q8NFI3]
ChEMBL Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis B 4.6 pIC50 25000 nM IC50 Bioorg Med Chem Lett (2017) 27: 2962-2966 [PMID:28512024]
NAD(+) hydrolase SARM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523350] [UniProtKB: Q6SZW1]
ChEMBL Inhibition of StrepTag-tagged human SARM1 TIR (561 to 724 residues) expressed in NRK1-HEK293T cells assessed as reduction in NADase activity by measuring NAD depletion pre-incubated up to 120 mins before NAD+ addition and further incubated for 60 mins by HPLC analysis B 5.46 pIC50 3500 nM IC50 WO-2018057989-A1. INHIBITORS OF SARM1 NADase ACTIVITY AND USES THEREOF (2018)
ChEMBL Inhibition of StrepTag-tagged human SARM1 TIR (561 to 724 residues) expressed in NRK1-HEK293T cells assessed as reduction in NADase activity by measuring maximal ADPR conversion pre-incubated up to 120 mins before NAD+ addition and further incubated for 60 mins by HPLC analysis B 5.48 pIC50 3300 nM IC50 WO-2018057989-A1. INHIBITORS OF SARM1 NADase ACTIVITY AND USES THEREOF (2018)

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]