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TargetHydroxycarboxylic acid receptor 2
LigandBDBM23522
Substrate/CompetitorBDBM23515
Meas. Tech.Tritiated Niacin Binding Assay and [35S]-GTP-gammaS Binding Assay
pH7.4±n/a
Temperature296.15±n/a K
IC50 9±n/a nM
EC50 86±n/a nM
Citation Shen, HCDing, FXLuell, SForrest, MJCarballo-Jane, EWu, KKWu, TJCheng, KWilsie, LCKrsmanovic, MLTaggart, AKRen, NCai, TQDeng, QChen, QWang, JWolff, MSTong, XHolt, TGWaters, MGHammond, MLTata, JRColletti, SL Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. J Med Chem50:6303-6 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Hydroxycarboxylic acid receptor 2
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:Homo sapiens (Human)
Description:Membranes from CHO cells expressing the recombinant human GPR109A were used in competition binding assay.
Residue:363
Sequence:
MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWK
SSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTV
VAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSF
SICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVF
VICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPS
FPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGP
TSP
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  Blast E-value cutoff:
BDBM23522
BDBM23515
NameBDBM23522
Synonyms:2-{3-[4-(5-hydroxypyridin-2-yl)phenyl]propanamido}benzoic acid | Biaryl Anthranilide Analogue, 2b
TypeSmall organic molecule
Emp. Form.C21H18N2O4
Mol. Mass.362.3786
SMILESOC(=O)c1ccccc1NC(=O)CCc1ccc(cc1)-c1ccc(O)cn1
Structure
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