ChEMBL ligand: CHEMBL289480 (Hyperium, Rilmenidina, Rilmenidine)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] There should be some charts here, you may need to enable JavaScript!
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] There should be some charts here, you may need to enable JavaScript!
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] There should be some charts here, you may need to enable JavaScript!
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] There should be some charts here, you may need to enable JavaScript!
Nischarin in Human [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] Nischarin in Rat [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL	Binding affinity towards human Alpha-1A adrenergic receptor by the displacement of [3H]prazosin	B	5.05	pKi	8912.51	nM	Ki	Bioorg Med Chem Lett (1994) 4: 2317-2322
ChEMBL	Binding affinity towards human Alpha-1C adrenergic receptor by the displacement of [3H]prazosin	B	5.22	pKi	6025.6	nM	Ki	Bioorg Med Chem Lett (1994) 4: 2317-2322
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL	Binding affinity towards human Alpha-2A adrenergic receptor by the displacement of [3H]rauwolscine	B	6.74	pKi	181.97	nM	Ki	Bioorg Med Chem Lett (1994) 4: 2317-2322
ChEMBL	Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter	B	7.44	pKi	36.31	nM	Ki	Bioorg Med Chem (2012) 20: 4710-4715 [PMID:22750139]
ChEMBL	Agonistic activity towards human Alpha-2A adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate	F	6.56	pEC50	275.42	nM	EC50	Bioorg Med Chem Lett (1994) 4: 2317-2322
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL	Binding affinity towards human Alpha-2B adrenergic receptor by the displacement of [3H]rauwolscine	B	7.15	pKi	70.79	nM	Ki	Bioorg Med Chem Lett (1994) 4: 2317-2322
ChEMBL	Displacement of [3H]RX821001 from human alpha2B adrenoceptor expressed in CHO cells after 60 mins by gamma counter	B	7.37	pKi	42.66	nM	Ki	Bioorg Med Chem (2012) 20: 4710-4715 [PMID:22750139]
ChEMBL	Agonistic activity towards human Alpha-2B adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate	F	6.14	pEC50	724.44	nM	EC50	Bioorg Med Chem Lett (1994) 4: 2317-2322
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL	Binding affinity towards human Alpha-2C adrenergic receptor by the displacement of [3H]rauwolscine	B	6.54	pKi	288.4	nM	Ki	Bioorg Med Chem Lett (1994) 4: 2317-2322
ChEMBL	Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counter	B	7.9	pKi	12.59	nM	Ki	Bioorg Med Chem (2012) 20: 4710-4715 [PMID:22750139]
ChEMBL	Agonistic activity towards human Alpha-2C adrenergic receptor was measured as ability to inhibit forskolin-stimulated synthesis of cyclic adenosine monophosphate	F	6.72	pEC50	190.55	nM	EC50	Bioorg Med Chem Lett (1994) 4: 2317-2322
Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1]
ChEMBL	Displacement of [3H]clonidine from imidazoline receptor I-1 of bovine chromaffin cell membranes	B	7.13	pKi	74.13	nM	Ki	J Med Chem (2001) 44: 1588-1593 [PMID:11334568]
ChEMBL	Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR	B	7.23	pKi	59.2	nM	Ki	Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536]
ChEMBL	Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR	B	7.23	pKi	59.16	nM	Ki	Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536]
Nischarin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017]
ChEMBL	Displacement of [125I] PIC from I1 imidazoline receptor in rat PC12 cells after 45 mins by gamma counting	B	7.08	pKi	83.1	nM	Ki	J Med Chem (2015) 58: 878-887 [PMID:25521963]
ChEMBL	Displacement of [125I]PIC from Imidazoline-1 receptor in rat PC12 cell membrane incubated for 30 mins by gamma counting method	B	7.9	pKi	12.59	nM	Ki	Bioorg Med Chem (2016) 24: 3174-3183 [PMID:27265687]
ChEMBL	Displacement of [3H]paraiodoclonidine from imidazoline I1 receptor in rat PC12 cells after 30 mins by gamma counter	B	7.95	pKi	11.22	nM	Ki	Bioorg Med Chem (2012) 20: 4710-4715 [PMID:22750139]
ChEMBL	Binding affinity to I1 imidazoline binding site in Rattus norvegicus (rat) PC12 cells	B	7.95	pKi	11.22	nM	Ki	Med Chem Res (2004) 13: 170-189

ChEMBL data shown on this page come from version 34:

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]