Reaction Details
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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
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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