Target
Alpha-2A adrenergic receptor [16-465]/Alpha-2B adrenergic receptor/Alpha-2C adrenergic receptor
Ligand
BDBM50026636
Substrate
n/a
Meas. Tech.
ChEMBL_32755 (CHEMBL641152)
Ki
7.1±n/a nM
Citation
 Clark, RDBerger, JGarg, PWeinhardt, KKSpedding, MKilpatrick, ATBrown, CMMacKinnon, AC Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for alpha-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled alpha 2-adrenoceptor vs the [3H]yohimbine-labeled site. J Med Chem 33:596-600 (1990) [PubMed]  Article 
Target
Name:
Alpha-2A adrenergic receptor [16-465]/Alpha-2B adrenergic receptor/Alpha-2C adrenergic receptor
Synonyms:
Adrenergic receptor alpha-2
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 935397
Components:
This complex has 3 components.
Component 1
Name:
Alpha-2C adrenergic receptor
Synonyms:
ADA2C_RAT | Adra2c | Adrenergic receptor alpha | Alpha-2C adrenergic receptor | adrenergic Alpha2 | adrenergic Alpha2C
Type:
Enzyme Catalytic Domain
Mol. Mass.:
49890.50
Organism:
RAT
Description:
adrenergic Alpha2 0 RAT::P22086
Residue:
458
Sequence:
MASPALAAALAAAAAEGPNGSDAGEWGSGGGANASGTDWGPPPGQYSAGAVAGLAAVVGFLIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFGQVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISAVISFPPLVSFYRRPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLRTRTLSEKRGPAGPDGASPTTENGLGKAAGENGHCAPPRTEVEPDESSAAERRRRRGALRRGGRRREGAEGDTGSADGPGPGLAAEQGARTASRSPGPGGRLSRASSRSVEFFLSRRRRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQLPEPLFKFFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
  
Component 2
Name:
Alpha-2B adrenergic receptor
Synonyms:
ADA2B_RAT | Adra2b | Adrenergic receptor alpha | Adrenergic receptor alpha-2 | Alpha-2B adrenergic receptor | Alpha-2B adrenoceptor | Alpha-2B adrenoreceptor | adrenergic Alpha2B
Type:
Enzyme Catalytic Domain
Mol. Mass.:
50379.83
Organism:
NEONATAL RAT
Description:
adrenergic Alpha2B ADRA2B NEONATAL RAT::P19328
Residue:
453
Sequence:
MSGPTMDHQEPYSVQATAAIASAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLAAADILVATLIIPFSLANELLGYWYFWRAWCEVYLALDVLFCTSSIVHLCAISLDRYWAVSRALEYNSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQRPEPRGLPQCELNQEAWYILASSIGSFFAPCLIMILVYLRIYVIAKRSHCRGLGAKRGSGEGESKKPQPVAGGVPTSAKVPTLVSPLSSVGEANGHPKPPREKEEGETPEDPEARALPPTWSALPRSGQGQKKGTSGATAEEGDEEDEEEVEECEPQTLPASPASVCNPPLQQPQTSRVLATLRGQVLLGKNVGVASGQWWRRRTQLSREKRFTFVLAVVIGVFVVCWFPFFFSYSLGAICPQHCKVPHGLFQFFFWIGYCNSSLNPVIYTVFNQDFRRAFRRILCRPWTQTGW
  
Component 3
Name:
Alpha-2A adrenergic receptor [16-465]
Synonyms:
ADA2A_RAT | Adra2a | Adrenaline 2 | Alpha-2A adrenergic receptor | Alpha-2A adrenoceptor | Alpha-2A adrenoreceptor | Alpha-2AAR | Alpha-2D adrenergic receptor | Alpha2 Adrenoreceptor | CA2-47 | adrenergic Alpha2A
Type:
G-protein coupled receptor
Mol. Mass.:
48961.69
Organism:
Rattus norvegicus (rat)
Description:
P22909[16-465]
Residue:
450
Sequence:
MGSLQPDAGNSSWNGTEAPGGGTRATPYSLQVTLTLVCLAGLLMLFTVFGNVLVIIAVFTSRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKVWCEIYLALDVLFCTSSIVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIVTVWVISAVISFPPLISIEKKGAGGGQQPAEPSCKINDQKWYVISSSIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDACSAPPGGADRRPNGLGPERGAGTAGAEAEPLPTQLNGAPGEPAPTRPRDGDALDLEESSSSEHAERPQGPGKPERGPRAKGKTKASQVKPGDSLPRRGPGAAGPGASGSGQGEERAGGAKASRWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLIAVGCPVPYQLFNFFFWFGYCNSSLNPVIYTIFNHDFRRAFKKILCRGDRKRIV
  
Inhibitor
Name:
BDBM50026636
Synonyms:
17alpha-hydroxy-20alpha-yohimban-16beta-carboxylic acid methyl ester | CHEMBL10347 | RAUWOLSCINE HYDROCHLORIDE | alpha-yohimbine | corynanthidine | isoyohimbine | mesoyohimbine | methyl (16beta,17alpha,20alpha)-17-hydroxyyohimban-16-carboxylate | methyl 17alpha-hydroxy-20alpha-yohimban-16beta-carboxylate | rauwolscine
Type:
Small organic molecule
Emp. Form.:
C21H26N2O3
Mol. Mass.:
354.4427
SMILES:
COC(=O)[C@@H]1[C@@H](O)CC[C@@H]2CN3CCc4c([nH]c5ccccc45)[C@@H]3C[C@H]12 |r|
Structure:
Search PDB for entries with ligand similarity: