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Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM23525
Substrate
n/a
Meas. Tech.
ChEMBL_744662 (CHEMBL1772683)
EC50
6±n/a nM
Citation
 Imbriglio, JE; DiRocco, D; Bodner, R; Raghavan, S; Chen, W; Marley, D; Esser, C; Holt, TG; Wolff, MS; Taggart, AK; Waters, MG; Tata, JR; Colletti, SL The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties. Bioorg Med Chem Lett 21:2721-4 (2011) [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:
Homo sapiens (Human)
Description:
Membranes from CHO cells expressing the recombinant human GPR109A were used in competition binding assay.
Residue:
363
Sequence:
MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWKSSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTVVAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSFSICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVFVICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPSFPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGPTSP
  
Inhibitor
Name:
BDBM23525
Synonyms:
2-{3-[2-(2-chloro-4-hydroxyphenyl)-1,3-thiazol-5-yl]propanamido}benzoic acid | Biaryl Anthranilide Analogue, 2g
Type:
Small organic molecule
Emp. Form.:
C19H15ClN2O4S
Mol. Mass.:
402.851
SMILES:
OC(=O)c1ccccc1NC(=O)CCc1cnc(s1)-c1ccc(O)cc1Cl
Structure:
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