Reaction Details Report a problem with these data
Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM50313976
Substrate
n/a
Meas. Tech.
ChEMBL_615510 (CHEMBL1105988)
Ki
595±n/a nM
Citation
Shen, HC; Ding, FX; Raghavan, S; Deng, Q; Luell, S; Forrest, MJ; Carballo-Jane, E; Wilsie, LC; Krsmanovic, ML; Taggart, AK; Wu, KK; Wu, TJ; Cheng, K; Ren, N; Cai, TQ; Chen, Q; Wang, J; Wolff, MS; Tong, X; Holt, TG; Waters, MG; Hammond, ML; Tata, JR; Colletti, SL Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. J Med Chem 53:2666-70 (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:
BDBM50313976
Synonyms:
2-({3-[3-(5-hydroxypyridin-2-yl)-1,2,4-oxadiazol-5-yl]-2,2-dimethylpropanoyl}-amino)cyclohex-1-ene-1-carboxylic acid | CHEMBL1086657
Type:
Small organic molecule
Emp. Form.:
C19H22N4O5
Mol. Mass.:
386.4018
SMILES:
CC(C)(Cc1nc(no1)-c1ccc(O)cn1)C(=O)NC1=C(CCCC1)C(O)=O |t:21|