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TargetMineralocorticoid receptor
LigandBDBM50013429
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1348998
IC50 4.1±n/a nM
Citation Casimiro-Garcia APiotrowski DWAmbler CArhancet GBBanker MEBanks TBoustany-Kari CMCai CChen XEudy RHepworth DHulford CAJennings SMLoria PMMeyers MJPetersen DNRaheja NKSammons MShe LSong KVrieze DWei L Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist. J Med Chem 57:4273-88 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mineralocorticoid receptor
Name:Mineralocorticoid receptor
Synonyms:MCR | 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50013429
n/a
NameBDBM50013429
Synonyms:CHEMBL3263767
TypeSmall organic molecule
Emp. Form.C23H26N6O4S
Mol. Mass.482.555
SMILESCOc1nc(ccc1C(=O)NS(C)(=O)=O)C1=NN([C@H](C1)C1CCCC1)c1ccc(C#N)c(C)n1 |r,t:16|
Structure
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