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

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ChEMBL ligand: CHEMBL91397 (Rupatadina, Rupatadine, UR-12592)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor in Guinea pig [GtoPdb: 262]
Created with Highcharts 10.3.3ValuesChart context menuHistamine H1 receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig0246810Highcharts.com
  • PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
Created with Highcharts 10.3.3ValuesChart context menuPlatelet activating factor receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • B0AT2/Sodium-dependent neutral amino acid transporter B(0)AT2 in Human [ChEMBL: CHEMBL3351189] [GtoPdb: 940] [UniProtKB: Q9H2J7]
Created with Highcharts 10.3.3ValuesChart context menuSodium-dependent neutral amino acid transporter B(0)AT2pKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
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 35:

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]