Reaction Details |
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Target | Hydroxycarboxylic acid receptor 2 |
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Ligand | BDBM23518 |
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Substrate/Competitor | BDBM23515 |
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Meas. Tech. | Tritiated Niacin Binding Assay and [35S]-GTP-gammaS Binding Assay |
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pH | 7.4±n/a |
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Temperature | 296.15±n/a K |
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IC50 | 140±n/a nM |
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EC50 | 1000±n/a nM |
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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 Chem50:6303-6 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, 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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BDBM23518 |
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BDBM23515 |
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Name | BDBM23518 |
Synonyms: | 2-[3-(naphthalen-2-yl)propanamido]benzoic acid | Biaryl Anthranilide Analogue, 1b | CHEMBL235740 |
Type | Small organic molecule |
Emp. Form. | C20H17NO3 |
Mol. Mass. | 319.3539 |
SMILES | OC(=O)c1ccccc1NC(=O)CCc1ccc2ccccc2c1 |
Structure |
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