moxonidine [Ligand Id: 12574] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19236 (BDF-5896, BDF5896, BE-5895, BE5895, Cynt, Fisiotens, LY-326869, LY326869, Moxonidine, Norcynt, Normatens, Nucynt, Physiotens) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 5 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Binding affinity for human Alpha-2A adrenergic receptor | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 7.5 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | increased cAMP generation | - | 5.8 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | increased ERK1/2 phosphorylation | - | 8.5 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 4.6 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 7.5 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | cAMP generation | - | 6.5 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 7.1 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328] | ||||||||
| ChEMBL | Binding affinity for rat Alpha-2B adrenergic receptor | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | - | - | 4.8 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Binding affinity for human Alpha-2C adrenergic receptor | B | 5.7 | pKi | 2000 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| GtoPdb | inhibition of cAMP production | - | 6.6 | pIC50 | - | - | - |
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]; Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| GtoPdb | 4.73 =value for β-arrestin recruitment and internalization | - | 5.35 | pEC50 | - | - | - | Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| GtoPdb | ERK1/2 phosphorylation | - | 6.9 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
| ChEMBL | Displacement of [3H]-clonidine from bovine imidazoline receptor I-1 | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 8.38 | pKi | 4.2 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| ChEMBL | Displacement of [3H]clonidine from I1IR in human brain frontal cortex in presence of adrenaline incubated for 45 mins by liquid scintillation spectrometry | B | 8.45 | pIC50 | 3.55 | nM | IC50 | J Med Chem (2020) 63: 3610-3633 [PMID:32150414] |
| Nischarin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017] | ||||||||
| ChEMBL | Displacement of [125I] PIC from I1 imidazoline receptor in rat PC12 cells after 45 mins by gamma counting | B | 7.11 | pKi | 77.8 | nM | Ki | J Med Chem (2015) 58: 878-887 [PMID:25521963] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 6.4 | pKi | 401.2 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 6.15 | pIC50 | 702.1 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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]
