[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];
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 - - 8.1 pKd - - - J Pharmacol Exp Ther (1996) 278: 1215-27 [PMID:8819505];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642];
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 - - 9.2 pKd - - - J Pharmacol Exp Ther (1996) 278: 1215-27 [PMID:8819505];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642];
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 35:

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]