Reaction Details
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Hydroxycarboxylic acid receptor 2
Ligand
BDBM23515
Substrate
n/a
Meas. Tech.
ChEMBL_501337 (CHEMBL971523)
IC50
140±n/a nM
Citation
Shen, HC; Ding, FX; Deng, Q; Wilsie, LC; Krsmanovic, ML; Taggart, AK; Carballo-Jane, E; Ren, N; Cai, TQ; Wu, TJ; Wu, KK; Cheng, K; Chen, Q; Wolff, MS; Tong, X; Holt, TG; Waters, MG; Hammond, ML; Tata, JR; Colletti, 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 More Info.:
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:
BDBM23515
Synonyms:
CHEMBL573 | Niacin | Nicotinic Acid | [5, 6-3H]-niacin | pyridine-3-carboxylic acid | wampocap
Type:
Small organic molecule
Emp. Form.:
C6H5NO2
Mol. Mass.:
123.1094
SMILES:
OC(=O)c1cccnc1
Structure:
