atipamezole [Ligand Id: 12576] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL353972 (4-(2-ethyl-2-indanyl)imidazole., Antisedan, Atipamezole, MPV-1248) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Displacement of [3H]-prazosin from human adrenergic alpha-1b receptor expressed in CHO cells after 120 mins by liquid scintillation counting | B | 5.71 | pKi | 1949.84 | nM | Ki | J Med Chem (2010) 53: 6986-6995 [PMID:20809632] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 8.5 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cell | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (2001) 44: 787-805 [PMID:11262089] |
| ChEMBL | Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting | B | 8.73 | pKi | 1.86 | nM | Ki | J Med Chem (2010) 53: 6986-6995 [PMID:20809632] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 7.9 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting | B | 8.65 | pKi | 2.24 | nM | Ki | J Med Chem (2010) 53: 6986-6995 [PMID:20809632] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting | B | 8.38 | pKi | 4.17 | nM | Ki | J Med Chem (2010) 53: 6986-6995 [PMID:20809632] |
| GtoPdb | - | - | 8.5 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
| ChEMBL | In vitro binding affinity was determined against NA (noradrenaline) reuptake site of rat in presence of [3H]nisoxetine radioligand | F | 5 | pKi | <10000 | nM | Ki | J Med Chem (2001) 44: 787-805 [PMID:11262089] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | In vitro binding affinity was determined against serotonin reuptake site of rat in presence of [3H]paroxetine radioligand | F | 5.5 | pKi | <3162.28 | nM | Ki | J Med Chem (2001) 44: 787-805 [PMID:11262089] |
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]
