rupatadine [Ligand Id: 10103] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL91397 (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 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]
