Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM50264263
Substrate
n/a
Meas. Tech.
ChEMBL_535242 (CHEMBL981701)
IC50
1300±n/a nM
Citation
 Shen, HCTaggart, AKWilsie, LCWaters, MGHammond, MLTata, JRColletti, SL Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A. Bioorg Med Chem Lett 18:4948-51 (2008) [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:
BDBM50264263
Synonyms:
CHEMBL492020 | rac-3-(4-isopropylphenyl)-7-methyl-N-(1-phenoxypropan-2-yl)pyrazolo[1,5-a]pyrimidine-6-carboxamide
Type:
Small organic molecule
Emp. Form.:
C26H28N4O2
Mol. Mass.:
428.5261
SMILES:
CC(COc1ccccc1)NC(=O)c1cnc2c(cnn2c1C)-c1ccc(cc1)C(C)C
Structure:
Search PDB for entries with ligand similarity: