Reaction Details |
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Target | Mineralocorticoid receptor |
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Ligand | BDBM18623 |
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Substrate/Competitor | BDBM18207 |
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Meas. Tech. | Competitive Ligand Binding Assay, GR-Mediated Agonist Activity Assay, and IL-6 Repression Assay |
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Ki | 48±n/a nM |
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Citation | Hudson, AR; Roach, SL; Higuchi, RI; Phillips, DP; Bissonnette, RP; Lamph, WW; Yen, J; Li, Y; Adams, ME; Valdez, LJ; Vassar, A; Cuervo, C; Kallel, EA; Gharbaoui, CJ; Mais, DE; Miner, JN; Marschke, KB; Rungta, D; Negro-Vilar, A; Zhi, L Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma. J Med Chem50:4699-709 (2007) [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 | MCR_HUMAN | MLR | MR | NR3C2 | Nuclear receptor subfamily 3 group C member 2 |
Type: | Enzyme |
Mol. Mass.: | 107076.42 |
Organism: | Homo sapiens (Human) |
Description: | P08235 |
Residue: | 984 |
Sequence: | METKGYHSLPEGLDMERRWGQVSQAVERSSLGPTERTDENNYMEIVNVSCVSGAIPNNST
QGSSKEKQELLPCLQQDNNRPGILTSDIKTELESKELSATVAESMGLYMDSVRDADYSYE
QQNQQGSMSPAKIYQNVEQLVKFYKGNGHRPSTLSCVNTPLRSFMSDSGSSVNGGVMRAV
VKSPIMCHEKSPSVCSPLNMTSSVCSPAGINSVSSTTASFGSFPVHSPITQGTPLTCSPN
VENRGSRSHSPAHASNVGSPLSSPLSSMKSSISSPPSHCSVKSPVSSPNNVTLRSSVSSP
ANINNSRCSVSSPSNTNNRSTLSSPAASTVGSICSPVNNAFSYTASGTSAGSSTLRDVVP
SPDTQEKGAQEVPFPKTEEVESAISNGVTGQLNIVQYIKPEPDGAFSSSCLGGNSKINSD
SSFSVPIKQESTKHSCSGTSFKGNPTVNPFPFMDGSYFSFMDDKDYYSLSGILGPPVPGF
DGNCEGSGFPVGIKQEPDDGSYYPEASIPSSAIVGVNSGGQSFHYRIGAQGTISLSRSAR
DQSFQHLSSFPPVNTLVESWKSHGDLSSRRSDGYPVLEYIPENVSSSTLRSVSTGSSRPS
KICLVCGDEASGCHYGVVTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRL
QKCLQAGMNLGARKSKKLGKLKGIHEEQPQQQQPPPPPPPPQSPEEGTTYIAPAKEPSVN
TALVPQLSTISRALTPSPVMVLENIEPEIVYAGYDSSKPDTAENLLSTLNRLAGKQMIQV
VKWAKVLPGFKNLPLEDQITLIQYSWMCLSSFALSWRSYKHTNSQFLYFAPDLVFNEEKM
HQSAMYELCQGMHQISLQFVRLQLTFEEYTIMKVLLLLSTIPKDGLKSQAAFEEMRTNYI
KELRKMVTKCPNNSGQSWQRFYQLTKLLDSMHDLVSDLLEFCFYTFRESHALKVEFPAML
VEIISDQLPKVESGNAKPLYFHRK
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BDBM18623 |
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BDBM18207 |
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Name | BDBM18623 |
Synonyms: | (18Z)-12-methoxy-18-({3-[(1E)-1-(methoxyimino)ethyl]thiophen-2-yl}methylidene)-3,5,5-trimethyl-17-oxa-6-azatetracyclo[8.8.0.0^{2,7}.0^{11,16}]octadeca-1(10),2(7),3,8,11,13,15-heptaen-13-ol | Oxime, 23 |
Type | Small organic molecule |
Emp. Form. | C28H28N2O4S |
Mol. Mass. | 488.598 |
SMILES | CO\N=C(/C)c1ccsc1\C=C1/Oc2ccc(O)c(OC)c2-c2ccc3NC(C)(C)C=C(C)c3c12 |t:32| |
Structure |
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