naphazoline [Ligand Id: 5509] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL761 (Nafazair, Nafazolin, Naphazoline)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [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 Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts. F 7.2 pEC50 63.1 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay F 7.2 pEC50 63.1 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 575-579 [PMID:11844675]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Potency against cloned human alpha 1B adrenoceptor expressed in rat-1 fibroblasts. F 5.3 pEC50 <5011.87 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL In vitro activation of human Alpha-1B receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay F 5.3 pEC50 <5011.87 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 575-579 [PMID:11844675]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Potency against cloned human alpha 1D-adrenoceptor expressed in rat-1 fibroblasts. F 5.3 pEC50 <5011.87 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay F 5.3 pEC50 <5011.87 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 575-579 [PMID:11844675]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis B 8.64 pKi 2.29 nM Ki Bioorg. Med. Chem. (2015) 23: 3991-3999 [PMID:25648685]
ChEMBL Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis F 7.26 pEC50 54.95 nM EC50 Bioorg. Med. Chem. (2015) 23: 3991-3999 [PMID:25648685]
Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1]
ChEMBL Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR B 6.91 pKi 121.62 nM Ki Bioorg. Med. Chem. (2008) 16: 7134-7140 [PMID:18621536]
ChEMBL Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR B 6.92 pKi 121.6 nM Ki Bioorg. Med. Chem. (2008) 16: 7134-7140 [PMID:18621536]
Nischarin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017]
ChEMBL Binding affinity to I1 imidazoline binding site in Rattus norvegicus (rat) PC12 cells B 6.61 pKi 245.47 nM Ki Med Chem Res (2004) 13: 170-189

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]