Ki Summary

Reaction Details

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Target

5-hydroxytryptamine receptor 4

Ligand

BDBM50388698

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_841618 (CHEMBL2092044)

10±n/a nM

Citation

Long, DD; Armstrong, SR; Beattie, DT; Choi, SK; Fatheree, PR; Gendron, RA; Genov, D; Goldblum, AA; Humphrey, PP; Jiang, L; Marquess, DG; Shaw, JP; Smith, JA; Turner, SD; Vickery, RG Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. Bioorg Med Chem Lett22:6048-52 (2012) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

5-hydroxytryptamine receptor 4

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:

MDKLDANVSSEEGFGSVEKVVLLTFLSTVILMAILGNLLVMVAVCWDRQLRKIKTNYFIV
SLAFADLLVSVLVMPFGAIELVQDIWIYGEVFCLVRTSLDVLLTTASIFHLCCISLDRYY
AICCQPLVYRNKMTPLRIALMLGGCWVIPTFISFLPIMQGWNNIGIIDLIEKRKFNQNSN
STYCVFMVNKPYAITCSVVAFYIPFLLMVLAYYRIYVTAKEHAHQIQMLQRAGASSESRP
QSADQHSTHRMRTETKAAKTLCIIMGCFCLCWAPFFVTNIVDPFIDYTVPGQVWTAFLWL
GYINSGLNPFLYAFLNKSFRRAFLIILCCDDERYRRPSILGQTVPCSTTTINGSTHVLRD
AVECGGQWESQCHPPATSPLVAAQPSDT

BDBM50388698

n/a

Name

BDBM50388698

Synonyms:

CHEMBL2059590

Type

Small organic molecule

Emp. Form.

C26H38N6O2

Mol. Mass.

466.6189

SMILES

CC(C)n1nc(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3CCN2CCN(CC2)C(C)=O)c2ccccc12 |r,THB:17:16:9.15.10:12.13|

Structure