Reaction Details |
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Target | Hydroxycarboxylic acid receptor 2 |
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Ligand | BDBM50277634 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_501337 (CHEMBL971523) |
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IC50 | 360±n/a nM |
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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 Chem52:2587-602 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Hydroxycarboxylic acid receptor 2 |
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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: | MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWK
SSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTV
VAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSF
SICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVF
VICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPS
FPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGP
TSP
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BDBM50277634 |
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n/a |
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Name | BDBM50277634 |
Synonyms: | 2-(3-(7-hydroxy-5-methyl-4-oxo-4,5-dihydro-[1,2,3]triazolo[1,5-a]quinoxalin-3-yl)propanamido)benzoic acid | CHEMBL484605 |
Type | Small organic molecule |
Emp. Form. | C20H17N5O5 |
Mol. Mass. | 407.3795 |
SMILES | Cn1c2cc(O)ccc2n2nnc(CCC(=O)Nc3ccccc3C(O)=O)c2c1=O |
Structure |
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