Ki Summary

Reaction Details

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Target

G-protein coupled bile acid receptor 1

Ligand

BDBM50300199

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_943955 (CHEMBL2339922)

EC50

166±n/a nM

Citation

Piotrowski, DW; Futatsugi, K; Warmus, JS; Orr, ST; Freeman-Cook, KD; Londregan, AT; Wei, L; Jennings, SM; Herr, M; Coffey, SB; Jiao, W; Storer, G; Hepworth, D; Wang, J; Lavergne, SY; Chin, JE; Hadcock, JR; Brenner, MB; Wolford, AC; Janssen, AM; Roush, NS; Buxton, J; Hinchey, T; Kalgutkar, AS; Sharma, R; Flynn, DA Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. ACS Med Chem Lett4:63-8 (2013) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

G-protein coupled bile acid receptor 1

Name:

G-protein coupled bile acid receptor 1

Synonyms:

BG37 | GPBAR1 | GPBAR_HUMAN | M-BAR | TGR5 | hBG37 | hGPCR19

Type:

G Protein-Coupled Receptor (GPCR)

Mol. Mass.:

35260.02

Organism:

Homo sapiens (Human)

Description:

CHO cells transiently transfected with hTGR5.

Residue:

330

Sequence:

MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLA
GLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQP
PGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGA
AAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPY
VATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQ
GLWGRASRDSPGPSIAYHPSSQSSVDLDLN

BDBM50300199

n/a

Name

BDBM50300199

Synonyms:

6alpha-ethyl-23(S)-methyl-cholic acid | CHEMBL567640

Type

Small organic molecule

Emp. Form.

C27H46O5

Mol. Mass.

450.6511

SMILES

CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)C[C@H](C)C(O)=O)[C@@]3(C)[C@@H](O)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 |r|

Structure