Reaction Details |
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Target | Alpha-1A/Alpha-1B/Alpha-1D adrenergic receptor |
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Ligand | BDBM50497440 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1442353 (CHEMBL3378311) |
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Ki | 2320±n/a nM |
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Citation | Wasilewska, A; S?czewski, F; Hudson, AL; Ferdousi, M; Scheinin, M; Laurila, JM; Rybczy?ska, A; Boblewski, K; Lehmann, A Fluorinated analogues of marsanidine, a highly ?2-AR/imidazoline I1 binding site-selective hypotensive agent. Synthesis and biological activities. Eur J Med Chem87:386-97 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Alpha-1A/Alpha-1B/Alpha-1D adrenergic receptor |
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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: | MNPDLDTGHNTSAPAHWGELKDDNFTGPNQTSSNSTLPQLDVTRAISVGLVLGAFILFAI
VGNILVILSVACNRHLRTPTNYFIVNLAIADLLLSFTVLPFSATLEVLGYWVLGRIFCDI
WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP
LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG
VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV
GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFM
RILGCQCRGGRRRRRRRRLGACAYTYRPWTRGGSLERSQSRKDSLDDSGSCMSGTQRTLP
SASPSPGYLGRGTQPPVELCAFPEWKPGALLSLPEPPGRRGRLDSGPLFTFKLLGDPESP
GTEGDTSNGGCDTTTDLANGQPGFKSNMPLAPGHF
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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: | MVLLSENASEGSNCTHPPAPVNISKAILLGVILGGLIIFGVLGNILVILSVACHRHLHSV
THYYIVNLAVADLLLTSTVLPFSAIFEILGYWAFGRVFCNIWAAVDVLCCTASIMGLCII
SIDRYIGVSYPLRYPTIVTQRRGVRALLCVWVLSLVISIGPLFGWRQPAPEDETICQINE
EPGYVLFSALGSFYVPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN
VPAEGGGVSSAKNKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD
FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLRRRQSSKHALGYTL
HPPSQALEGQHRDMVRIPVGSGETFYKISKTDGVCEWKFFSSMPQGSARITVPKDQSACT
TARVRSKSFLQVCCCVGSSAPRPEENHQVPTIKIHTISLGENGEEV
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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: | MTFRDILSVTFEGPRSSSSTGGSGAGGGAGTVGPEGGAVGGVPGATGGGAVVGTGSGEDN
QSSTGEPGAAASGEVNGSAAVGGLVVSAQGVGVGVFLAAFILTAVAGNLLVILSVACNRH
LQTVTNYFIVNLAVADLLLSAAVLPFSATMEVLGFWAFGRTFCDVWAAVDVLCCTASILS
LCTISVDRYVGVRHSLKYPAIMTERKAAAILALLWAVALVVSVGPLLGWKEPVPPDERFC
GITEEVGYAIFSSVCSFYLPMAVIVVMYCRVYVVARSTTRSLEAGIKREPGKASEVVLRI
HCRGAATSAKGYPGTQSSKGHTLRSSLSVRLLKFSREKKAAKTLAIVVGVFVLCWFPFFF
VLPLGSLFPQLKPSEGVFKVIFWLGYFNSCVNPLIYPCSSREFKRAFLRLLRCQCRRRRR
RLWAVYGHHWRASTGDARSDCAPSPRIAPPGAPLALTAHPGAGSADTPETQDSVSSSRKP
ASALREWRLLGPLQRPTTQLRAKVSSLSHKIRSGARRAETACALRSEVEAVSLNVPQDGA
EAVICQAYEPGDYSNLRETDI
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BDBM50497440 |
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n/a |
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Name | BDBM50497440 |
Synonyms: | CHEMBL3343698 |
Type | Small organic molecule |
Emp. Form. | C10H10FN5 |
Mol. Mass. | 219.2183 |
SMILES | Fc1ccc2n(\[#7]=[#6]-3\[#7]-[#6]-[#6]-[#7]-3)ncc2c1 |
Structure |
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