Reaction Details Report a problem with these data
Target
5-hydroxytryptamine receptor 4
Ligand
BDBM29529
Substrate
BDBM29525
Meas. Tech.
Radioligand Binding Assay (Ki) and cAMP Accumulation Assay (EC50)
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
14±7 nM
EC50
9±4 nM
Comments
Emax=70%.
Citation
 Russo, O; Cachard-Chastel, M; Rivière, C; Giner, M; Soulier, JL; Berthouze, M; Richard, T; Monti, JP; Sicsic, S; Lezoualc'h, F; Berque-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:
BDBM29529
Synonyms:
ML10302 scaffold, 14
Type:
Small organic molecule
Emp. Form.:
C50H72Cl2N8O8
Mol. Mass.:
984.061
SMILES:
COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CC1)NC(=O)CCCNCCCc1ccc(CCCNCCCC(=O)NC2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM29525
Synonyms:
3H-GR113808 | CHEMBL518682 | GR 113808 | [3H] GR 113808 | [3H]GR113808
Type:
radiolabeled ligand
Emp. Form.:
C19H27N3O4S
Mol. Mass.:
393.5
SMILES:
Cn1cc(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)c2ccccc12
Structure:
Search PDB for entries with ligand similarity: