cirazoline [Ligand Id: 515] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL13852 (Cirazolina, Cirazoline, Ld-3098) |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
