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Target
Alpha-2A adrenergic receptor
Ligand
BDBM50084959
Substrate
n/a
Meas. Tech.
ChEMBL_33205 (CHEMBL643230)
Ki
>1000±n/a nM
Citation
 Gaster, LM; Blaney, FE; Davies, S; Duckworth, DM; Ham, P; Jenkins, S; Jennings, AJ; Joiner, GF; King, FD; Mulholland, KR; Wyman, PA; Hagan, JJ; Hatcher, J; Jones, BJ; Middlemiss, DN; Price, GW; Riley, G; Roberts, C; Routledge, C; Selkirk, J; Slade, PD The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J Med Chem 41:1218-35 (1998) [PubMed]  Article 
Target
Name:
Alpha-2A adrenergic receptor
Synonyms:
ADA2A_HUMAN | ADRA2A | ADRA2R | ADRAR | Adrenergic alpha2A | Adrenergic receptor alpha | Alpha-2 adrenergic receptor subtype C10 | Alpha-2A adrenoceptor | Alpha-2A adrenoreceptor | Alpha-2AAR | alpha-2A adrenergic receptor [Homo sapiens]
Type:
Enzyme
Mol. Mass.:
48979.91
Organism:
Homo sapiens (Human)
Description:
P08913
Residue:
450
Sequence:
MGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLMLLTVFGNVLVIIAVFTSRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAWCEIYLALDVLFCTSSIVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVISFPPLISIEKKGGGGGPQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDAVAAPPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGPRDTDALDLEESSSSDHAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTPAAGPGEERVGAAKASRWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPRTLFKFFFWFGYCNSSLNPVIYTIFNHDFRRAFKKILCRGDRKRIV
  
Inhibitor
Name:
BDBM50084959
Synonyms:
11'-Methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo-[2,3-f]indole-3,4'-piperidine](SB-224289) | 4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl-1'-methylspiro[3,5,6,7-tetrahydro-2H-furo[2,3-f]indole-3,4'-(hexahydropyridine)]-5-ylmethanone | CHEMBL281350 | SB-224289 | [2'-Methyl-4'-(5-methyl-[1,2,4]oxadiazol-3-yl)-biphenyl-4-yl]-[3-(1-methyl-piperidine)-2,3,6,7-tetrahydro-1-oxa-5-aza-s-indacen-5-yl]-methanone
Type:
Small organic molecule
Emp. Form.:
C32H32N4O3
Mol. Mass.:
520.6215
SMILES:
CN1CCC2(COc3cc4CCN(C(=O)c5ccc(cc5)-c5ccc(cc5C)-c5noc(C)n5)c4cc23)CC1
Structure:
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