Target
5-hydroxytryptamine receptor 4
Ligand
BDBM29528
Substrate
BDBM10852
Meas. Tech.
Inhibition of A-beta Fibril Formation
Comments
14 +/- 2 inhibition.
Citation
 Russo, OCachard-Chastel, MRivière, CGiner, MSoulier, JLBerthouze, MRichard, TMonti, JPSicsic, SLezoualc'h, FBerque-Bestel, I Design, synthesis, and biological evaluation of new 5-HT4 receptor agonists: application as amyloid cascade modulators and potential therapeutic utility in Alzheimer's disease. J Med Chem 52:2214-25 (2009) [PubMed]  Article 
Target
Name:
5-hydroxytryptamine receptor 4
Synonyms:
5-HT-4 | 5-HT4 | 5-HT4S | 5-HT4a | 5-HT4b | 5-HT4c | 5-HT4d | 5-HT4hb | 5-hydroxytryptamine receptor 4 | 5-hydroxytryptamine receptor 4 (5-HT4) | 5HT4R_HUMAN | HTR4 | Serotonin (5-HT) receptor | Serotonin (5-HT3) receptor | Serotonin 4 (5-HT4) receptor | Serotonin Receptor 4
Type:
Enzyme
Mol. Mass.:
43767.54
Organism:
Homo sapiens (Human)
Description:
Q13639
Residue:
388
Sequence:
MDKLDANVSSEEGFGSVEKVVLLTFLSTVILMAILGNLLVMVAVCWDRQLRKIKTNYFIVSLAFADLLVSVLVMPFGAIELVQDIWIYGEVFCLVRTSLDVLLTTASIFHLCCISLDRYYAICCQPLVYRNKMTPLRIALMLGGCWVIPTFISFLPIMQGWNNIGIIDLIEKRKFNQNSNSTYCVFMVNKPYAITCSVVAFYIPFLLMVLAYYRIYVTAKEHAHQIQMLQRAGASSESRPQSADQHSTHRMRTETKAAKTLCIIMGCFCLCWAPFFVTNIVDPFIDYTVPGQVWTAFLWLGYINSGLNPFLYAFLNKSFRRAFLIILCCDDERYRRPSILGQTVPCSTTTINGSTHVLRDAVECGGQWESQCHPPATSPLVAAQPSDT
  
Inhibitor
Name:
BDBM29528
Synonyms:
ML10302 scaffold, 9{a;y}
Type:
Small organic molecule
Emp. Form.:
C33H38ClN5O6
Mol. Mass.:
636.138
SMILES:
COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CC1)NC(=O)CCCCCN1C(=O)c2cccc3c(N)ccc(C1=O)c23
Structure:
Search PDB for entries with ligand similarity:
Substrate