cirazoline [Ligand Id: 515] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL13852 (Cirazoline) |
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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] | ||||||||
| GtoPdb | - | - | 6.7 | pKi | - | - | - |
Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| 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] |
| GtoPdb | - | - | 9.2 | pEC50 | - | - | - |
Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| GtoPdb | - | - | 5.1 | pKi | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| 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] |
| GtoPdb | - | - | 8.1 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| GtoPdb | - | - | 5.5 | pKi | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| GtoPdb | - | - | 6.9 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| 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 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]
