moxonidine [Ligand Id: 12574] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19236 (BDF-5896, BDF5896, BE-5895, BE5895, Fisiotens, LY-326869, LY326869, Moxonidina, Moxonidine, Normatens, 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 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]
