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ChEMBL ligand: CHEMBL1502 (Altopan, BY 1023, BY-1023, NSC-759257, Pantocid, Pantoloc, Pantoloc control, Pantoprazole, Pantozol, Protium, Protium i.v., Protonix, SK-96022, SK&F 96022, SK&F-96022, SKF-96022, Zovanta) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of MTX uptake in membrane vesicle from BCRP-expressing Sf9 cell | F | 5 | pIC50 | 10000 | nM | IC50 | Cancer Res (2004) 64: 5804-5811 [PMID:15313923] |
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 | 5.39 | pKi | 4100 | 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 | 4.44 | pIC50 | 36200 | nM | IC50 | J Med Chem (2015) 58: 778-784 [PMID:25513712] |
indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5] | ||||||||
ChEMBL | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis | B | 4.9 | pIC50 | 12600 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7641-7646 [PMID:23122865] |
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 4.36 | pIC50 | 43200 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
ChEMBL | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
ChEMBL | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay | B | 4.36 | pIC50 | 43200 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
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 recombinant human DDAH1 expressed in Escherichia coli BL21 Star (DE3) using ADMA as substrate assessed as decrease in citrulline production after 4 hrs by colorimetric method | B | 4.2 | pIC50 | 63000 | nM | IC50 | WO-2014160947-A1. Dimethylarginine Dimethylaminohydrolase inhibitors and methods of use thereof (2014) |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells | F | 4.75 | pIC50 | 17900 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2001) 364: 551-557 [PMID:11770010] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antimicrobial activity against Plasmodium falciparum | F | 4.41 | pIC50 | 39000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316] |
ATP4A/ATP4B/Potassium-transporting ATPase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095173] [GtoPdb: 849, 851] [UniProtKB: P20648, P51164] | ||||||||
ChEMBL | In vitro evaluation for the inhibition of H+/K+ ATPase at pH < 3 in the gastric glands of isolated rabbit stomach. | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1992) 35: 1049-1057 [PMID:1313110] |
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
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]