Reaction Details Report a problem with these data
Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM23530
Substrate
BDBM23515
Meas. Tech.
Tritiated Niacin Binding Assay and [35S]-GTP-gammaS Binding Assay
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
26±n/a nM
EC50
430±n/a nM
Citation
 Shen, HC; Ding, FX; Luell, S; Forrest, MJ; Carballo-Jane, E; Wu, KK; Wu, TJ; Cheng, K; Wilsie, LC; Krsmanovic, ML; Taggart, AK; Ren, N; Cai, TQ; Deng, Q; Chen, Q; Wang, J; Wolff, MS; Tong, X; Holt, TG; Waters, MG; Hammond, ML; Tata, JR; Colletti, SL Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. J Med Chem 50:6303-6 (2007) [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:
BDBM23530
Synonyms:
2-{3-[2-(5-hydroxypyridin-2-yl)-1,3-thiazol-5-yl]propanamido}benzoic acid | Biaryl Anthranilide Analogue, 2l
Type:
Small organic molecule
Emp. Form.:
C18H15N3O4S
Mol. Mass.:
369.394
SMILES:
OC(=O)c1ccccc1NC(=O)CCc1cnc(s1)-c1ccc(O)cn1
Structure:
Search PDB for entries with ligand similarity:
Substrate
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:
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