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Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM50298000
Substrate
n/a
Meas. Tech.
ChEMBL_585069 (CHEMBL1054335)
IC50
67±n/a nM
Citation
 Schmidt, D; Smenton, A; Raghavan, S; Carballo-Jane, E; Lubell, S; Ciecko, T; Holt, TG; Wolff, M; Taggart, A; Wilsie, L; Krsmanovic, M; Ren, N; Blom, D; Cheng, K; McCann, PE; Gerard Waters, M; Tata, J; Colletti, S Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia. Bioorg Med Chem Lett 19:4768-72 (2009) [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:
BDBM50298000
Synonyms:
(+/-)-5-(2,3,5-trifluorophenyl)-4,5,6,7-tetrahydro-1H-indazole-3-carboxylic acid | CHEMBL558463
Type:
Small organic molecule
Emp. Form.:
C14H11F3N2O2
Mol. Mass.:
296.2445
SMILES:
OC(=O)c1n[nH]c2CCC(Cc12)c1cc(F)cc(F)c1F
Structure:
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