Reaction Details |
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Target | Hydroxycarboxylic acid receptor 2 |
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Ligand | BDBM50342521 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_744662 (CHEMBL1772683) |
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EC50 | 410±n/a nM |
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Citation | Imbriglio, JE; DiRocco, D; Bodner, R; Raghavan, S; Chen, W; Marley, D; Esser, C; Holt, TG; Wolff, MS; Taggart, AK; Waters, MG; Tata, JR; Colletti, SL The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties. Bioorg Med Chem Lett21:2721-4 (2011) [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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BDBM50342521 |
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n/a |
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Name | BDBM50342521 |
Synonyms: | (R)-2-(3-(3-(5-fluoropyridin-2-yl)-1,2,4-oxadiazol-5-yl)propanamido)-4-methylcyclohex-1-enecarboxylic acid | CHEMBL1770359 |
Type | Small organic molecule |
Emp. Form. | C18H19FN4O4 |
Mol. Mass. | 374.3663 |
SMILES | C[C@@H]1CCC(C(O)=O)=C(C1)NC(=O)CCc1nc(no1)-c1ccc(F)cn1 |r,c:7| |
Structure |
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