rabeprazole [Ligand Id: 7290] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1219 (Aciphex, E3810, E-3810 (PPI), Eraloc, Ly-307640, LY-307640, LY307640, Pariprazole, Rabeprazol, Rabeprazole)
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • Endo-beta-N-acetylglucosaminidase in Human [ChEMBL: CHEMBL5172] [UniProtKB: Q8NFI3]
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  • fatty acid synthase/Fatty acid synthase in Human [ChEMBL: CHEMBL4158] [GtoPdb: 2608] [UniProtKB: P49327]
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  • insulin degrading enzyme/Insulin-degrading enzyme in Human [ChEMBL: CHEMBL1293287] [GtoPdb: 2371] [UniProtKB: P14735]
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  • NG,NG-Dimethylarginine dimethylaminohydrolase 1/N(G),N(G)-dimethylarginine dimethylaminohydrolase 1 in Human [ChEMBL: CHEMBL6036] [GtoPdb: 1247] [UniProtKB: O94760]
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  • Urease subunit alpha/Urease subunit beta in Helicobacter pylori (strain ATCC 700392 / 26695) (Campylobacterpylori) [ChEMBL: CHEMBL3885651] [UniProtKB: P14916P69996]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.74 pKi 1820 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.49 pIC50 3219 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.1 pKi 793 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.76 pIC50 1737 nM IC50 DrugMatrix in vitro pharmacology data
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of human ABCG2 expressed in human HEK293 cells membrane vesicles mediated transport of 3[H]-MTX for 2 mins using [3H]-methotrexate as substrate by rapid filtration technique B 5.07 pIC50 8500 nM IC50 Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.1 pKi 790 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.63 pIC50 2326 nM IC50 DrugMatrix in vitro pharmacology data
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 5.35 pIC50 4470 nM IC50 Bioorg Med Chem Lett (2017) 27: 2962-2966 [PMID:28512024]
fatty acid synthase/Fatty acid synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4158] [GtoPdb: 2608] [UniProtKB: P49327]
ChEMBL Inhibition of purified recombinant FASN TE activity (unknown origin) using 4-MUH as substrate preincubated for 30 mins before substrate addition measured after 1 hr by fluorescence assay B 5.23 pKi 5900 nM Ki J Med Chem (2015) 58: 778-784 [PMID:25513712]
ChEMBL Inhibition of purified recombinant FASN TE activity (unknown origin) using 4-MUH as substrate preincubated for 30 mins before substrate addition measured after 1 hr by fluorescence assay B 4.28 pIC50 52000 nM IC50 J Med Chem (2015) 58: 778-784 [PMID:25513712]
insulin degrading enzyme/Insulin-degrading enzyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293287] [GtoPdb: 2371] [UniProtKB: P14735]
ChEMBL Inhibition of human recombinant IDE expressed in Escherichia coli BL21 (DE3) cells using ATTO 655- Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Trp as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by spectrophotometric analysis B 4.96 pIC50 11000 nM IC50 Eur J Med Chem (2019) 179: 557-566 [PMID:31276900]
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 5.48 pIC50 3300 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 5.49 pIC50 3200 nM IC50 WO-2018057989-A1. INHIBITORS OF SARM1 NADase ACTIVITY AND USES THEREOF (2018)
NG,NG-Dimethylarginine dimethylaminohydrolase 1/N(G),N(G)-dimethylarginine dimethylaminohydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6036] [GtoPdb: 1247] [UniProtKB: O94760]
ChEMBL Inhibition of human recombinant DDAH1 reduction in L-citrulline formation using ADMA as substrate B 4.28 pIC50 53000 nM IC50 Eur J Med Chem (2019) 179: 557-566 [PMID:31276900]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 5.15 pIC50 7000 nM IC50 Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316]
Urease subunit alpha/Urease subunit beta in Helicobacter pylori (strain ATCC 700392 / 26695) (Campylobacterpylori) (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885651] [UniProtKB: P14916P69996]
ChEMBL Inhibition of Helicobacter pylori ATCC 43504 urease assessed as amount of ammonia after 15 mins by indophenol method B 6.54 pIC50 290 nM IC50 J Med Chem (2016) 59: 8125-8133 [PMID:27524377]

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]