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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) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 (null) |
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 (null) |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]