Reaction Details |
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Target | Mineralocorticoid receptor |
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Ligand | BDBM19200 |
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Substrate/Competitor | BDBM19214 |
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IC50 | >5000±n/a nM |
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Citation | Ali, A; Thompson, CF; Balkovec, JM; Graham, DW; Hammond, ML; Quraishi, N; Tata, JR; Einstein, M; Ge, L; Harris, G; Kelly, TM; Mazur, P; Pandit, S; Santoro, J; Sitlani, A; Wang, C; Williamson, J; Miller, DK; Thompson, CM; Zaller, DM; Forrest, MJ; Carballo-Jane, E; Luell, S Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity. J Med Chem47:2441-52 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Mineralocorticoid receptor |
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Name: | Mineralocorticoid receptor |
Synonyms: | MCR_RAT | MR | Mineralocorticoid Receptor (MR) | Mineralocorticoid receptor | Mlr | Nr3c2 | Nuclear receptor subfamily 3 group C member 2 | mineralocorticoid |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 106748.15 |
Organism: | RAT |
Description: | mineralocorticoid 0 RAT::P22199 |
Residue: | 981 |
Sequence: | METKGYHSLPEGLDMERRWSQVSQTLERSSLGPAERTTENNYMEIVNVSCVSGAIPNNST
QGSSKEKHELLPYIQQDNSRSGILPSDIKTELESKELSATVAESMGLYMDSVRDAEYTYD
QQNQQGSLSPTKIYQNMEQLVKFYKENGHRSSTLSAMSRPLRSFMPDSAASMNGGALRAI
VKSPIICHEKSSSVSSPLNMASSVCSPVGINSMSSSTTSFGSFPVHSPITQGTSLTCSPS
VENRGSRSHSPTHASNVGSPLSSPLSSMKSPISSPPSHCSVKSPVSSPNNVPLRSSVSSP
ANLNNSRCSVSSPSNNTNNRSTLSSPTASTVGSIGSPISNAFSYATSGASAGAGAIQDVV
PSPDTHEKGAHDVPFPKTEEVEKAISNGVTGPLNIVQYIKSEPDGAFSSSCLGGNSKISP
SSPFSVPIKQESSKHSCSGASFKGNPTVNPFPFMDGSYFSFMDDKDYYSLSGILGPPVPG
FDGSCEDSAFPVGIKQEPDDGSYYPEASIPSSAIVGVNSGGQSFHYRIGAQGTISLSRSP
RDQSFQHLSSFPPVNTLVESWKPHGDLSSRRSDGYPVLEYIPENVSSSTLRSVSTGSSRP
SKICLVCGDEASGCHYGVVTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACR
LQKCLQAGMNLGARKSKKLGKLKGLHEEQPQQPPPPPPQSPEEGTTYIAPTKEPSVNSAL
VPQLTSITHALTPSPAMILENIEPETVYAGYDNSKPDTAESLLSTLNRLAAKQMIQVVKW
AKVLPGFKNLPLEDQITLIQYSWMCLSSFALSWRSYKHTNSQLLYFAPDLVFNEEKMHQS
AMYELCQGMRQISLQFVRLQLTFEEYSIMKVLLLLSTVPKDGLKSQAAFEEMRTNYIKEL
RKMVTKCPNSSGQSWQRFYQLTKLLDSMHDLVSDLLEFCFYTFRESQALKVEFPAMLVEI
ITDQLPKVESGNAKPLYFHRK
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BDBM19200 |
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BDBM19214 |
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Name | BDBM19200 |
Synonyms: | (S)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4aH,5H,6H,7H,8H-cyclohexa[f]indazol-5-yl](4-fluorophenyl)methanol | BMCL173354 benzo[f]indazole, 7 | N-Arylpyrazolo[3,2-c]-Based Ligand, 20 |
Type | Small organic molecule |
Emp. Form. | C25H24F2N2O |
Mol. Mass. | 406.4677 |
SMILES | [H][C@@]1(CCCC2=Cc3c(C[C@]12C)cnn3-c1ccc(F)cc1)[C@H](O)c1ccc(F)cc1 |r,t:5| |
Structure |
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