rupatadine [Ligand Id: 10103] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL91397 (Rupatadina, Rupatadine, UR-12592) |
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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 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]
