cirazoline [Ligand Id: 515] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13852 (Cirazoline)
  • 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]
  • α1D-adrenoceptor in Rat [GtoPdb: 24] [UniProtKB: P23944]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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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 7.9 pEC50 12.59 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway F 7.9 pEC50 12.59 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 471-475 [PMID:11814822]
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 7.9 pEC50 12.59 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 575-579 [PMID:11844675]
ChEMBL Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts F 7.9 pEC50 12.59 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 3449-3452 [PMID:12419381]
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 7.2 pEC50 63.1 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL Activation of recombinant human adrenergic, alpha-1B receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway F 7.2 pEC50 63.1 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 471-475 [PMID:11814822]
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 7.2 pEC50 63.1 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 575-579 [PMID:11844675]
ChEMBL Activation of human alpha-1B adrenergic receptors expressed in rat-1 fibroblasts F 7.2 pEC50 63.1 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 3449-3452 [PMID:12419381]
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 6.9 pEC50 125.89 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 2871-2874 [PMID:11597419]
ChEMBL Activation of recombinant human adrenergic, alpha-1D receptor expressed in rat-1 fibroblasts assayed via calcium mobilization through Gq coupled PLC pathway F 6.9 pEC50 125.89 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 471-475 [PMID:11814822]
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 6.9 pEC50 125.89 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 575-579 [PMID:11844675]
ChEMBL Activation of human Alpha-1D adrenergic receptors expressed in rat-1 fibroblasts F 6.9 pEC50 125.89 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 3449-3452 [PMID:12419381]
α1D-adrenoceptor in Rat [GtoPdb: 24] [UniProtKB: P23944]
GtoPdb - - 6.9 pKi - - - Mol Pharmacol (1994) 46: 929-36 [PMID:7969082]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting B 7.23 pKi 58.88 nM Ki J. Med. Chem. (2009) 52: 7319-7322 [PMID:19886609]
ChEMBL Binding affinity at human alpha2A AR B 7.23 pKi 58.88 nM Ki ACS Med. Chem. Lett. (2013) 4: 875-879 [PMID:24900763]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Displacement of [3H]RX821002 from human alpha2B adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting B 6.28 pKi 524.81 nM Ki J. Med. Chem. (2009) 52: 7319-7322 [PMID:19886609]
ChEMBL Binding affinity at human alpha2B AR B 6.28 pKi 524.81 nM Ki ACS Med. Chem. Lett. (2013) 4: 875-879 [PMID:24900763]
ChEMBL Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry F 6 pEC50 1000 nM EC50 J. Med. Chem. (2009) 52: 7319-7322 [PMID:19886609]
ChEMBL Agonist activity at human alpha2B AR B 6 pEC50 1000 nM EC50 ACS Med. Chem. Lett. (2013) 4: 875-879 [PMID:24900763]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting B 6.26 pKi 549.54 nM Ki J. Med. Chem. (2009) 52: 7319-7322 [PMID:19886609]
ChEMBL Binding affinity at human alpha2C AR B 6.26 pKi 549.54 nM Ki ACS Med. Chem. Lett. (2013) 4: 875-879 [PMID:24900763]
ChEMBL Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry F 6.4 pEC50 398.11 nM EC50 J. Med. Chem. (2009) 52: 7319-7322 [PMID:19886609]
ChEMBL Agonist activity at human alpha2C AR B 6.4 pEC50 398.11 nM EC50 ACS Med. Chem. Lett. (2013) 4: 875-879 [PMID:24900763]
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 7 pKi 99.08 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 7 pKi 99 nM Ki Bioorg. Med. Chem. (2008) 16: 7134-7140 [PMID:18621536]
ChEMBL Binding affinity for imidazoline receptor I-2 in rabbit kidney homogenate (relative to [3H]-Idazoxan radioligand) B 8.4 pKi 3.98 nM Ki J. Med. Chem. (2000) 43: 1109-1122 [PMID:10737743]
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 5.76 pKi 1737.8 nM Ki Med Chem Res (2004) 13: 170-189
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity at human 5HT1A receptor B 7.46 pKi 34.67 nM Ki ACS Med. Chem. Lett. (2013) 4: 875-879 [PMID:24900763]

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]