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

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ChEMBL ligand: CHEMBL312448 (Balminil, 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 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]