dexmedetomidine [Ligand Id: 521] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL778 (Dexmedetomidine, MPV-1440, Precedex)
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
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  • Alpha-1B adrenergic receptor in Cricetulus griseus [ChEMBL: CHEMBL3988626] [UniProtKB: G3HDX1]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay B 6.42 pEC50 376 nM EC50 US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005)
Alpha-1B adrenergic receptor in Cricetulus griseus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988626] [UniProtKB: G3HDX1]
ChEMBL Agonist activity at hamster recombinant alpha-1B receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay B 6.44 pEC50 364 nM EC50 US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005)
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL In vitro binding affinity against alpha-2D adrenergic receptor of male Wistar rat B 10.82 pKi 0.01 nM Ki J. Med. Chem. (2001) 44: 863-872 [PMID:11300868]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb - - 9.6 pKi - - - Biochim Biophys Acta (1998) 1448: 135-46 [PMID:9824686];
Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427];
Eur J Pharmacol (1998) 355: 275-9 [PMID:9760042];
Trends Pharmacol Sci (1997) 18: 211-9 [PMID:9227000]
ChEMBL Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting F 8.82 pEC50 1.5 nM EC50 Bioorg. Med. Chem. (2011) 19: 321-329 [PMID:21129985]
ChEMBL Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay B 9.1 pEC50 0.8 nM EC50 US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005)
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
ChEMBL in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand B 8.3 pKi 5 nM Ki J. Med. Chem. (2000) 43: 1423-1426 [PMID:10753480]
ChEMBL Binding affinity towards alpha-2D adrenergic receptor B 10.82 pKi 0.01 nM Ki J. Med. Chem. (2000) 43: 765-768 [PMID:10715142]
ChEMBL In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine B 10.82 pKi 0.01 nM Ki J. Med. Chem. (2000) 43: 1423-1426 [PMID:10753480]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Displacement of [3H]RX 821002 from human adrenergic alpha-2c receptor expressed in CHO cells in presence of GppNHp/Na B 7.51 pKi 30.9 nM Ki J. Med. Chem. (2007) 50: 3964-3968 [PMID:17630725]
ChEMBL Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells B 8.26 pKi 8.26 - pKiL J. Med. Chem. (2007) 50: 3964-3968 [PMID:17630725]
GtoPdb - - 9.3 pKi - - - Biochim Biophys Acta (1998) 1448: 135-46 [PMID:9824686];
Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427];
Eur J Pharmacol (1998) 355: 275-9 [PMID:9760042]
ChEMBL Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed in CHO cells B 10.04 pKi 10.04 - pKiH J. Med. Chem. (2007) 50: 3964-3968 [PMID:17630725]
ChEMBL Agonist activity at human recombinant alpha-2C receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay B 9.32 pEC50 0.48 nM EC50 US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005)
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 9.7 pKi - - - Biochim Biophys Acta (1998) 1448: 135-46 [PMID:9824686];
Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427];
Eur J Pharmacol (1998) 355: 275-9 [PMID:9760042];
Trends Pharmacol Sci (1997) 18: 211-9 [PMID:9227000]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]