[3H]RX821002 [Ligand Id: 528] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL10332 (RX-821002)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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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 - - 9.5 pKd - - - J Pharmacol Exp Ther (1996) 278: 1215-27 [PMID:8819505];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
ChEMBL Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells B 9.44 pKi 0.36 nM Ki J. Med. Chem. (2008) 51: 4289-4299 [PMID:18578476]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 9.1 pKd - - - J Pharmacol Exp Ther (1996) 278: 1215-27 [PMID:8819505];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
ChEMBL Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2B receptor expressed in CHO cells B 8.79 pKi 1.62 nM Ki J. Med. Chem. (2008) 51: 4289-4299 [PMID:18578476]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb - - 9.2 pKd - - - J Pharmacol Exp Ther (1996) 278: 1215-27 [PMID:8819505];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]
ChEMBL Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells B 9.1 pKi 0.79 nM Ki J. Med. Chem. (2008) 51: 4289-4299 [PMID:18578476]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]