Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM50318888
Substrate
n/a
Meas. Tech.
ChEMBL_633683 (CHEMBL1118308)
EC50
2450±n/a nM
Citation
 Boatman, PDSchrader, TOKasem, MJohnson, BRSkinner, PJJung, JKXu, JCherrier, MCWebb, PJSemple, GSage, CRKnudsen, JChen, RTaggart, AKCarballo-Jane, ERichman, JG Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a). Bioorg Med Chem Lett 20:2797-800 (2010) [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:
BDBM50318888
Synonyms:
(5R,5aS)-5-isobutyl-3-(1H-tetrazol-5-yl)-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazole | CHEMBL1085539
Type:
Small organic molecule
Emp. Form.:
C12H16N6
Mol. Mass.:
244.2956
SMILES:
CC(C)C[C@@H]1[C@H]2Cc3c(n[nH]c3[C@@H]12)-c1nnn[nH]1 |r|
Structure:
Search PDB for entries with ligand similarity: