rupatadine [Ligand Id: 10103] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL91397 (Rupatadine, UR-12592)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor in Guinea pig [GtoPdb: 262]
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  • PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
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  • B0AT2/Sodium-dependent neutral amino acid transporter B(0)AT2 in Human [ChEMBL: CHEMBL3351189] [GtoPdb: 940] [UniProtKB: Q9H2J7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method B 8.4 pKi 3.98 nM Ki J Med Chem (2019) 62: 6630-6644 [PMID:31274307]
ChEMBL Inhibitory concentration against histamine H1 receptor B 8.41 pIC50 3.9 nM IC50 J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
GtoPdb - - 8.41 pIC50 3.9 nM IC50 J Med Chem (2005) 48: 6523-43 [PMID:16220969]
H1 receptor in Guinea pig [GtoPdb: 262]
GtoPdb [3H]-pyrilamine binding to guinea pig cerebellum membranes. - 7 pKi 100 nM Ki J Pharmacol Exp Ther (1997) 280: 114-21 [PMID:8996188]
PAF receptor/Platelet activating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
GtoPdb - - 5.43 pKi 3700 nM Ki J Med Chem (2005) 48: 6523-43 [PMID:16220969]
ChEMBL Inhibitory concentration against platelet activating factor receptor B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
B0AT2/Sodium-dependent neutral amino acid transporter B(0)AT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351189] [GtoPdb: 940] [UniProtKB: Q9H2J7]
ChEMBL Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay B 4.4 pIC50 >40000 nM IC50 J. Med. Chem. (2014) 57: 9473-9479 [PMID:25318072]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]