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, Moxonidine, Normatens, Physiotens)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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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 Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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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]