Reaction Details |
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Target | Mineralocorticoid receptor |
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Ligand | BDBM19199 |
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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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BDBM19199 |
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BDBM19214 |
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Name | BDBM19199 |
Synonyms: | (R)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4aH,5H,6H,7H,8H-cyclohexa[f]indazol-5-yl](3,4-difluoro-5-methoxyphenyl)methanol | CHEMBL313062 | N-Arylpyrazolo[3,2-c]-Based Ligand, 18 |
Type | Small organic molecule |
Emp. Form. | C26H25F3N2O2 |
Mol. Mass. | 454.4841 |
SMILES | [H][C@@]1(CCCC2=Cc3c(C[C@]12C)cnn3-c1ccc(F)cc1)[C@@H](O)c1cc(F)c(F)c(OC)c1 |r,t:5| |
Structure |
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