Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM50277754
Substrate
n/a
Meas. Tech.
ChEMBL_501337 (CHEMBL971523)
IC50
13±n/a nM
Citation
 Shen, HCDing, FXDeng, QWilsie, LCKrsmanovic, MLTaggart, AKCarballo-Jane, ERen, NCai, TQWu, TJWu, KKCheng, KChen, QWolff, MSTong, XHolt, TGWaters, MGHammond, MLTata, JRColletti, SL Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats. J Med Chem 52:2587-602 (2009) [PubMed]  Article 
Target
Name:
Hydroxycarboxylic acid receptor 2
Synonyms:
G-protein coupled receptor 109A | G-protein coupled receptor HM74A | GPR109A | HCA2 | HCAR2 | HCAR2_HUMAN | HM74A | Hydroxycarboxylic acid receptor 2 | NIACR1 | Niacin Receptor GPR109A | Nicotinic acid receptor 1
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
41868.22
Organism:
Human
Description:
Membranes from CHO cells expressing the recombinant human GPR109A were used in competition binding assay.
Residue:
363
Sequence:
MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWKSSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTVVAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSFSICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVFVICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPSFPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGPTSP
  
Inhibitor
Name:
BDBM50277754
Synonyms:
2-(3-(7-hydroxy-4,5-dihydronaphtho[2,1-d]isoxazol-3-yl)propanamido)cyclopent-1-enecarboxylic acid | CHEMBL485326
Type:
Small organic molecule
Emp. Form.:
C20H20N2O5
Mol. Mass.:
368.3832
SMILES:
OC(=O)C1=C(CCC1)NC(=O)CCc1noc-2c1CCc1cc(O)ccc-21 |t:3|
Structure:
Search PDB for entries with ligand similarity: