apraclonidine [Ligand Id: 7117] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL647 (Apraclonidine, Iopidine)
  • 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 Rat [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
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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 - - 8.5 pKi 2.9 nM Ki J Med Chem (1996) 39: 3533-8 [PMID:8784451]
ChEMBL Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells B 8.54 pKi 2.9 nM Ki J Med Chem (1996) 39: 3533-3538 [PMID:8784451]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328]
ChEMBL Compound was tested in vitro for binding affinity against Alpha-2B adrenergic receptor from cloned rat RNG receptor transfected into Chinese hamster ovary (CHO) cells B 8.32 pKi 4.8 nM Ki J Med Chem (1996) 39: 3533-3538 [PMID:8784451]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb - - 7.52 pKi 30 nM Ki J Med Chem (1996) 39: 3533-8 [PMID:8784451];
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
ChEMBL Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells B 7.52 pKi 30 nM Ki J Med Chem (1996) 39: 3533-3538 [PMID:8784451]

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]