dexmedetomidine [Ligand Id: 521] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL778 (Dexmedetomidine, Medetomidine, (s)-, MPV-1440, Precedex) |
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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 | F | 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 | F | 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]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 9.3 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | increased cAMP generation | - | 7.6 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | - | - | 8.5 | pEC50 | - | - | - | Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427] |
| 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 | F | 9.1 | pEC50 | 0.8 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| GtoPdb | increased ERK1/2 phosphorylation | - | 9.5 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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] |
| GtoPdb | inhibition of cAMP production | - | 9.2 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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 | F | 9.32 | pEC50 | 0.48 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| GtoPdb | ERK1/2 phosphorylation | - | 9.6 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 10.9 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 9.2 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | cAMP generation | - | 9.9 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
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]
