Reaction Details |
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Target | Beta-3 adrenergic receptor |
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Ligand | BDBM50092644 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_216187 (CHEMBL818914) |
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EC50 | 19±n/a nM |
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Citation | Mathvink, RJ; Tolman, JS; Chitty, D; Candelore, MR; Cascieri, MA; Colwell, LF; Deng, L; Feeney, WP; Forrest, MJ; Hom, GJ; MacIntyre, DE; Miller, RR; Stearns, RA; Tota, L; Wyvratt, MJ; Fisher, MH; Weber, AE Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide. J Med Chem43:3832-6 (2000) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Beta-3 adrenergic receptor |
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Name: | Beta-3 adrenergic receptor |
Synonyms: | ADRB3 | ADRB3R | ADRB3_HUMAN | B3AR | Beta-2 adrenergic receptor and beta-3 adrenergic receptor | Beta-3 adrenoceptor | Beta-3 adrenoreceptor | adrenergic Beta3 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 43534.88 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 408 |
Sequence: | MAPWPHENSSLAPWPDLPTLAPNTANTSGLPGVPWEAALAGALLALAVLATVGGNLLVIV
AIAWTPRLQTMTNVFVTSLAAADLVMGLLVVPPAATLALTGHWPLGATGCELWTSVDVLC
VTASIETLCALAVDRYLAVTNPLRYGALVTKRCARTAVVLVWVVSAAVSFAPIMSQWWRV
GADAEAQRCHSNPRCCAFASNMPYVLLSSSVSFYLPLLVMLFVYARVFVVATRQLRLLRG
ELGRFPPEESPPAPSRSLAPAPVGTCAPPEGVPACGRRPARLLPLREHRALCTLGLIMGT
FTLCWLPFFLANVLRALGGPSLVPGPAFLALNWLGYANSAFNPLIYCRSPDFRSAFRRLL
CRCGRRLPPEPCAAARPALFPSGVPAARSSPAQPRLCQRLDGASWGVS
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BDBM50092644 |
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n/a |
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Name | BDBM50092644 |
Synonyms: | 4-[4-(2,4-Difluoro-phenyl)-thiazol-2-yl]-N-{4-[2-(2-hydroxy-2-pyridin-3-yl-ethylamino)-ethyl]-phenyl}-benzenesulfonamide | CHEMBL338976 |
Type | Small organic molecule |
Emp. Form. | C30H26F2N4O3S2 |
Mol. Mass. | 592.679 |
SMILES | O[C@@H](CNCCc1ccc(NS(=O)(=O)c2ccc(cc2)-c2nc(cs2)-c2ccc(F)cc2F)cc1)c1cccnc1 |
Structure |
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