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TargetAlpha-2A adrenergic receptor [16-465]/Alpha-2B adrenergic receptor/Alpha-2C adrenergic receptor
LigandBDBM50002338
Substrate/Competitorn/a
Meas. Tech.ChEMBL_33792 (CHEMBL648118)
IC50 1300±n/a nM
Citation DeWald, HABeeson, NWHershenson, FMWise, LDDowns, DAHeffner, TGCoughenour, LLPugsley, TA Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines. J Med Chem31:454-61 (1988) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Alpha-2A adrenergic receptor [16-465]/Alpha-2B adrenergic receptor/Alpha-2C adrenergic receptor
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:
MASPALAAALAAAAAEGPNGSDAGEWGSGGGANASGTDWGPPPGQYSAGAVAGLAAVVGF
LIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFG
QVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISA
VISFPPLVSFYRRPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLR
TRTLSEKRGPAGPDGASPTTENGLGKAAGENGHCAPPRTEVEPDESSAAERRRRRGALRR
GGRRREGAEGDTGSADGPGPGLAAEQGARTASRSPGPGGRLSRASSRSVEFFLSRRRRAR
SSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQLPEPLFKFFFW
IGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
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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:
MSGPTMDHQEPYSVQATAAIASAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLA
AADILVATLIIPFSLANELLGYWYFWRAWCEVYLALDVLFCTSSIVHLCAISLDRYWAVS
RALEYNSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQRPEPRGLPQCELNQEAWYILA
SSIGSFFAPCLIMILVYLRIYVIAKRSHCRGLGAKRGSGEGESKKPQPVAGGVPTSAKVP
TLVSPLSSVGEANGHPKPPREKEEGETPEDPEARALPPTWSALPRSGQGQKKGTSGATAE
EGDEEDEEEVEECEPQTLPASPASVCNPPLQQPQTSRVLATLRGQVLLGKNVGVASGQWW
RRRTQLSREKRFTFVLAVVIGVFVVCWFPFFFSYSLGAICPQHCKVPHGLFQFFFWIGYC
NSSLNPVIYTVFNQDFRRAFRRILCRPWTQTGW
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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:
MGSLQPDAGNSSWNGTEAPGGGTRATPYSLQVTLTLVCLAGLLMLFTVFGNVLVIIAVFT
SRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKVWCEIYLALDVLFCTSS
IVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIVTVWVISAVISFPPLISIEKKGAGGG
QQPAEPSCKINDQKWYVISSSIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDACS
APPGGADRRPNGLGPERGAGTAGAEAEPLPTQLNGAPGEPAPTRPRDGDALDLEESSSSE
HAERPQGPGKPERGPRAKGKTKASQVKPGDSLPRRGPGAAGPGASGSGQGEERAGGAKAS
RWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLIAVGCPVPYQLFNFFFWFGYCNSS
LNPVIYTIFNHDFRRAFKKILCRGDRKRIV
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BDBM50002338
n/a
NameBDBM50002338
Synonyms:(Thioridazine)10-[2-(1-Methyl-piperidin-2-yl)-ethyl]-2-methylsulfanyl-10H-phenothiazine | 10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine | 10-[2-(1-Methyl-piperidin-2-yl)-ethyl]-2-methylsulfanyl-10H-phenothiazine | 10-[2-(1-Methyl-piperidin-2-yl)-ethyl]-2-methylsulfanyl-10H-phenothiazine (thioridazine) | CHEMBL479 | MELLARIL | MELLARIL-S | THIORIDAZINE | TP-21 | US9504692, Thioridazine
TypeSmall organic molecule
Emp. Form.C21H26N2S2
Mol. Mass.370.575
SMILESCSc1ccc2Sc3ccccc3N(CCC3CCCCN3C)c2c1
Structure
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