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Target
Alpha-1A/Alpha-1B/Alpha-1D adrenergic receptor
Ligand
BDBM50002338
Substrate
n/a
Meas. Tech.
ChEMBL_33719 (CHEMBL647542)
IC50
17±n/a nM
Citation
 DeWald, HA; Beeson, NW; Hershenson, FM; Wise, LD; Downs, DA; Heffner, TG; Coughenour, LL; Pugsley, TA Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines. J Med Chem 31:454-61 (1988) [PubMed]  Article 
Target
Name:
Alpha-1A/Alpha-1B/Alpha-1D adrenergic receptor
Synonyms:
Adrenergic receptor alpha-1 | Alpha-1 Adrenergic Receptor/ adrenergic receptor/ adrenergic receptor | alpha-1 Adrenergic Receptor
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 303470
Components:
This complex has 3 components.
Component 1
Name:
Alpha-1B adrenergic receptor
Synonyms:
ADA1B_RAT | Adra1b | Alpha 1B-adrenoceptor | Alpha 1B-adrenoreceptor | Alpha adrenergic receptor 1A and 1B | Alpha-1 Adrenergic Receptor | Alpha-1Adrenoceptor | Alpha-1B adrenergic receptor | Alpha-1B adrenoreceptor | adrenergic Alpha1B
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
56606.71
Organism:
Rattus norvegicus (rat)
Description:
Receptor binding assays were performed using rat cortical membranes.
Residue:
515
Sequence:
MNPDLDTGHNTSAPAHWGELKDDNFTGPNQTSSNSTLPQLDVTRAISVGLVLGAFILFAIVGNILVILSVACNRHLRTPTNYFIVNLAIADLLLSFTVLPFSATLEVLGYWVLGRIFCDIWAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGPLLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAGVMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVVGMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFMRILGCQCRGGRRRRRRRRLGACAYTYRPWTRGGSLERSQSRKDSLDDSGSCMSGTQRTLPSASPSPGYLGRGTQPPVELCAFPEWKPGALLSLPEPPGRRGRLDSGPLFTFKLLGDPESPGTEGDTSNGGCDTTTDLANGQPGFKSNMPLAPGHF
  
Component 2
Name:
Alpha-1A adrenergic receptor
Synonyms:
ADA1A_RAT | Adra1a | Adra1c | Alpha-1 adrenoreceptor | Alpha-1A adrenoceptor | Alpha-1A adrenoreceptor | Alpha-1C adrenergic receptor | adrenergic Alpha1A
Type:
Protein
Mol. Mass.:
51620.15
Organism:
Rattus norvegicus (Rat)
Description:
P43140
Residue:
466
Sequence:
MVLLSENASEGSNCTHPPAPVNISKAILLGVILGGLIIFGVLGNILVILSVACHRHLHSVTHYYIVNLAVADLLLTSTVLPFSAIFEILGYWAFGRVFCNIWAAVDVLCCTASIMGLCIISIDRYIGVSYPLRYPTIVTQRRGVRALLCVWVLSLVISIGPLFGWRQPAPEDETICQINEEPGYVLFSALGSFYVPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKNVPAEGGGVSSAKNKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPDFKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLRRRQSSKHALGYTLHPPSQALEGQHRDMVRIPVGSGETFYKISKTDGVCEWKFFSSMPQGSARITVPKDQSACTTARVRSKSFLQVCCCVGSSAPRPEENHQVPTIKIHTISLGENGEEV
  
Component 3
Name:
Alpha-1D adrenergic receptor
Synonyms:
ADA1D_RAT | Adra1a | Adra1d | Alpha adrenergic receptor 1A and 1D | Alpha-1D adrenergic receptor | Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1
Type:
Protein
Mol. Mass.:
59375.97
Organism:
Rattus norvegicus (Rat)
Description:
P23944
Residue:
561
Sequence:
MTFRDILSVTFEGPRSSSSTGGSGAGGGAGTVGPEGGAVGGVPGATGGGAVVGTGSGEDNQSSTGEPGAAASGEVNGSAAVGGLVVSAQGVGVGVFLAAFILTAVAGNLLVILSVACNRHLQTVTNYFIVNLAVADLLLSAAVLPFSATMEVLGFWAFGRTFCDVWAAVDVLCCTASILSLCTISVDRYVGVRHSLKYPAIMTERKAAAILALLWAVALVVSVGPLLGWKEPVPPDERFCGITEEVGYAIFSSVCSFYLPMAVIVVMYCRVYVVARSTTRSLEAGIKREPGKASEVVLRIHCRGAATSAKGYPGTQSSKGHTLRSSLSVRLLKFSREKKAAKTLAIVVGVFVLCWFPFFFVLPLGSLFPQLKPSEGVFKVIFWLGYFNSCVNPLIYPCSSREFKRAFLRLLRCQCRRRRRRLWAVYGHHWRASTGDARSDCAPSPRIAPPGAPLALTAHPGAGSADTPETQDSVSSSRKPASALREWRLLGPLQRPTTQLRAKVSSLSHKIRSGARRAETACALRSEVEAVSLNVPQDGAEAVICQAYEPGDYSNLRETDI
  
Inhibitor
Name:
BDBM50002338
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
Type:
Small organic molecule
Emp. Form.:
C21H26N2S2
Mol. Mass.:
370.575
SMILES:
CSc1ccc2Sc3ccccc3N(CCC3CCCCN3C)c2c1
Structure:
Search PDB for entries with ligand similarity: