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Target
Glucocorticoid receptor
Ligand
BDBM50124591
Substrate
n/a
Meas. Tech.
ChEMBL_71398 (CHEMBL874034)
Ki
2.3±n/a nM
Citation
 Kym, PR; Kort, ME; Coghlan, MJ; Moore, JL; Tang, R; Ratajczyk, JD; Larson, DP; Elmore, SW; Pratt, JK; Stashko, MA; Falls, HD; Lin, CW; Nakane, M; Miller, L; Tyree, CM; Miner, JN; Jacobson, PB; Wilcox, DM; Nguyen, P; Lane, BC Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines. J Med Chem 46:1016-30 (2003) [PubMed]  Article 
Target
Name:
Glucocorticoid receptor
Synonyms:
GCR_HUMAN | GR | GRL | Glucocorticoid | Glucocorticoid receptor (GRFP) | NR3C1 | Nuclear receptor subfamily 3 group C member 1
Type:
Enzyme
Mol. Mass.:
85656.87
Organism:
Homo sapiens (Human)
Description:
P04150
Residue:
777
Sequence:
MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRRLLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLKLLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGNVKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGNSNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTVYCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVGSENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSYEEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTKLLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
  
Inhibitor
Name:
BDBM50124591
Synonyms:
5-Allyl-7-bromo-10-chloro-2,2,4-trimethyl-2,5-dihydro-1H-6-oxa-1-aza-chrysen-9-ol | CHEMBL7781
Type:
Small organic molecule
Emp. Form.:
C22H21BrClNO2
Mol. Mass.:
446.765
SMILES:
CC1=CC(C)(C)Nc2ccc-3c(C(CC=C)Oc4c(Br)cc(O)c(Cl)c-34)c12 |t:1|
Structure:
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