xylometazoline [Ligand Id: 517] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL312448 (Balminil, Xilometazolina, Xylometazoline)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • α1D-adrenoceptor in Rat [GtoPdb: 24] [UniProtKB: P23944]
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  • α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding affinity towards human Alpha-1 adrenergic receptor B 7.04 pKi 91 nM Ki Bioorg Med Chem Lett (2004) 14: 4697-4699 [PMID:15324890]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand B 7.85 pKi 14 nM Ki J Med Chem (1998) 41: 2243-2251 [PMID:9632357]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1B receptor B 7.89 pKi 13 nM Ki Bioorg Med Chem Lett (2004) 14: 4697-4699 [PMID:15324890]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1D receptor using [3H]5-HT trifluoroacetate as radioligand B 9.15 pKi 0.7 nM Ki J Med Chem (1998) 41: 2243-2251 [PMID:9632357]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1D receptor B 9.15 pKi 0.7 nM Ki Bioorg Med Chem Lett (2004) 14: 4697-4699 [PMID:15324890]
ChEMBL Tested for 5-hydroxytryptamine 1D like receptor-mediated vascular effect in rabbit saphenous vein (RSV) F 6.43 pEC50 369 nM EC50 J Med Chem (1998) 41: 2243-2251 [PMID:9632357]
α1D-adrenoceptor in Rat [GtoPdb: 24] [UniProtKB: P23944]
GtoPdb - - 6 pKi - - - Mol Pharmacol (1994) 46: 929-36 [PMID:7969082]
α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb - - 7.6 pKi - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb inhibition of forskolin stimulated cAMP generation - 8.1 pIC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 5.4 pKi - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb inhibition of forskolin stimulated cAMP generation - 8.8 pIC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb cAMP generation - 7.8 pEC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb - - 7 pKi - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb inhibition of cAMP production - 7.2 pIC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]

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]