Reaction Details Report a problem with these data
Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM50319241
Substrate
n/a
Meas. Tech.
ChEMBL_633873 (CHEMBL1120319)
IC50
5±n/a nM
Citation
Ding, FX; Shen, HC; Wilsie, LC; Krsmanovic, ML; Taggart, AK; Ren, N; Cai, TQ; Wang, J; Tong, X; Holt, TG; Chen, Q; Waters, MG; Hammond, ML; Tata, JR; Colletti, SL Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A. Bioorg Med Chem Lett 20:3372-5 (2010) [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:
Human
Description:
Membranes from CHO cells expressing the recombinant human GPR109A were used in competition binding assay.
Residue:
363
Sequence:
MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWKSSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTVVAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSFSICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVFVICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPSFPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGPTSP
Inhibitor
Name:
BDBM50319241
Synonyms:
5-(3,5-difluorophenyl)-2-(3-(1-(5-hydroxypyridin-2-yl)-1H-pyrazol-3-yl)-2-methylpropanamido)cyclohex-1-enecarboxylicacid | CHEMBL1085616
Type:
Small organic molecule
Emp. Form.:
C25H24F2N4O4
Mol. Mass.:
482.4793
SMILES:
CC(Cc1ccn(n1)-c1ccc(O)cn1)C(=O)NC1=C(CC(CC1)c1cc(F)cc(F)c1)C(O)=O |t:20|