Target
Alpha-2A adrenergic receptor [16-465]/Alpha-2B adrenergic receptor/Alpha-2C adrenergic receptor
Ligand
BDBM50048589
Substrate
n/a
Meas. Tech.
ChEMBL_34058 (CHEMBL643915)
IC50
24±n/a nM
Citation
 Klein, JTDavis, LOlsen, GEWong, GSHuger, FPSmith, CPPetko, WWCornfeldt, MWilker, JCBlitzer, RDLandau, EHaroutunian, VMartin, LLEffland, RC Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. J Med Chem 39:570-81 (1996) [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:
BDBM50048589
Synonyms:
CHEMBL152842 | Indol-1-yl-methyl-pyridin-4-yl-amine
Type:
Small organic molecule
Emp. Form.:
C14H13N3
Mol. Mass.:
223.2731
SMILES:
CN(c1ccncc1)n1ccc2ccccc12
Structure:
Search PDB for entries with ligand similarity: