dexmedetomidine [Ligand Id: 521] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL778 (Dexmedetomidina, Dexmedetomidine, Medetomidine, (s)-, MPV-1440) |
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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 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]
