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Name | 5-hydroxytryptamine receptor 4 |
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Species | Rattus norvegicus (Rat) |
Gene | Htr4 |
Synonym | 5-HT-4 5-HT4 5-HT4 receptor 5-hydroxytryptamine (serotonin) receptor 4, G protein-coupled serotonin receptor 4 |
Disease | N/A for non-human GPCRs |
Length | 406 |
Amino acid sequence | MDRLDANVSSNEGFGSVEKVVLLTFFAMVILMAILGNLLVMVAVCRDRQLRKIKTNYFIVSLAFADLLVSVLVNAFGAIELVQDIWFYGEMFCLVRTSLDVLLTTASIFHLCCISLDRYYAICCQPLVYRNKMTPLRIALMLGGCWVIPMFISFLPIMQGWNNIGIVDVIEKRKFNHNSNSTFCVFMVNKPYAITCSVVAFYIPFLLMVLAYYRIYVTAKEHAQQIQMLQRAGATSESRPQTADQHSTHRMRTETKAAKTLCVIMGCFCFCWAPFFVTNIVDPFIDYTVPEKVWTAFLWLGYINSGLNPFLYAFLNKSFRRAFLIILCCDDERYKRPPILGQTVPCSTTTINGSTHVLRDTVECGGQWESRCHLTATSPLVAAQPVIRRPQDNDLEDSCSLKRSQS |
UniProt | Q62758 |
Protein Data Bank | N/A |
GPCR-HGmod model | N/A |
3D structure model | No available structures or models |
BioLiP | N/A |
Therapeutic Target Database | N/A |
ChEMBL | CHEMBL4317 |
IUPHAR | 9 |
DrugBank | N/A |
Name | cisapride |
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Molecular formula | C23H29ClFN3O4 |
IUPAC name | 4-amino-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-yl]-2-methoxybenzamide |
Molecular weight | 465.95 |
Hydrogen bond acceptor | 7 |
Hydrogen bond donor | 2 |
XlogP | 3.4 |
Synonyms | Colinorm DSSTox_GSID_22825 Guptro (.+/-.)-Cisapride L000938 [ Show all ] |
Inchi Key | DCSUBABJRXZOMT-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C23H29ClFN3O4/c1-30-21-13-19(26)18(24)12-17(21)23(29)27-20-8-10-28(14-22(20)31-2)9-3-11-32-16-6-4-15(25)5-7-16/h4-7,12-13,20,22H,3,8-11,14,26H2,1-2H3,(H,27,29) |
PubChem CID | 2769 |
ChEMBL | CHEMBL1729 |
IUPHAR | 240 |
BindingDB | 50005836 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
Parameter | Value | Reference | Database source |
---|---|---|---|
EC50 | 54.7 nM | PMID16451077 | ChEMBL |
EC50 | 55.0 nM | , PMID16451077, Bioorg. Med. Chem. Lett., (1992) 2:12:1613 | BindingDB,ChEMBL |
ED50 | 54.7 nM | PMID1573641 | ChEMBL |
Ki | 10.0 nM | PMID9225293 | BindingDB |
Ki | 10.0 - 158.489 nM | PMID8813606, PMID9225293 | IUPHAR |
Ki | 25.0 nM | PMID8813606 | BindingDB |
Ki | 79.43 nM | PMID9225293 | BindingDB |
Ki | 122.0 nM | PMID7796807, PMID8813606 | BindingDB |
Ki | 125.89 nM | PMID9349523 | BindingDB |
Ki | 158.48 nM | PMID9225293 | BindingDB |
Relaxation | 7.0 % | PMID9599243 | ChEMBL |
Relaxation | 20.3 % | PMID9599243 | ChEMBL |
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