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ChEMBL ligand: CHEMBL1219 (Aciphex, E3810, E-3810 (PPI), Eraloc, Ly-307640, LY-307640, LY307640, Pariprazole, Rabeprazole) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 |
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 (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 | 5.49 | pIC50 | 3200 | nM | IC50 | WO-2018057989-A1. INHIBITORS OF SARM1 NADase ACTIVITY AND USES THEREOF (null) |
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: P14916, P69996] | ||||||||
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 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]