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ChEMBL ligand: CHEMBL761 (Nafazair, Nafazolin, Naphazoline) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]