RX821002 [Ligand Id: 526] 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 - - 9.2 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
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 - - 8.4 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
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 - - 8.7 pKi - - - J Pharmacol Exp Ther (1994) 271: 1558-65 [PMID:7996470];
Br J Pharmacol (2007) 150: 391-402 [PMID:17220913];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
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 32:

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]