Target
5-hydroxytryptamine receptor 3A
Ligand
BDBM50258431
Substrate
n/a
Meas. Tech.
ChEMBL_523350 (CHEMBL1006686)
Ki
0.8±n/a nM
Citation
 Morelli, EGemma, SBudriesi, RCampiani, GNovellino, EFattorusso, CCatalanotti, BCoccone, SSRos, SBorrelli, GPersico, MFiorini, INacci, VIoan, PChiarini, AHamon, MCagnotto, AMennini, TFracasso, CColovic, MCaccia, SButini, S Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships. J Med Chem 52:3548-62 (2009) [PubMed]  Article 
Target
Name:
5-hydroxytryptamine receptor 3A
Synonyms:
5-HT3 | 5-hydroxytryptamine receptor 3A | 5HT3A_RAT | 5ht3 | Htr3 | Htr3a | Serotonin (5-HT) receptor | Zacopride site-R
Type:
Enzyme Catalytic Domain
Mol. Mass.:
55428.70
Organism:
RAT
Description:
5-HT3 HTR3A RAT::P35563
Residue:
483
Sequence:
MPLCIPQVLLALFLSVLIAQGEGSRRRATQAHSTTQPALLRLSDHLLANYKKGVRPVRDWRKPTLVSIDVIMYAILNVDEKNQVLTTYIWYRQFWTDEFLQWTPEDFDNVTKLSIPTDSIWVPDILINEFVDVGKSPSIPYVYVHHQGEVQNYKPLQLVTACSLDIYNFPFDVQNCSLTFTSWLHTIQDINISLWRTPEEVRSDKSIFINQGEWELLGVFTKFQEFSIETSNSYAEMKFYVVIRRRPLFYAVSLLLPSIFLMVVDIVGFCLPPDSGERVSFKITLLLGYSVFLIIVSDTLPATAIGTPLIGVYFVVCMALLVISLAETIFIVQLVHKQDLQRPVPDWLRHLVLDRIAWLLCLGEQPMAHRPPATFQANKTDDCSAMGNHCSHVGSPQDLEKTSRSRDSPLPPPREASLAVRGLLQELSSIRHSLEKRDEMREVARDWLRVGYVLDRLLFRIYLLAVLAYSITLVTLWSIWHYS
  
Inhibitor
Name:
BDBM50258431
Synonyms:
CHEMBL523716 | [4-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)piperazin-1-yl]hydroxyacetamidine
Type:
Small organic molecule
Emp. Form.:
C17H19FN6O
Mol. Mass.:
342.3708
SMILES:
ONC(=N)CN1CCN(CC1)c1nc2cc(F)ccc2n2cccc12
Structure:
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