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Target
Glucocorticoid receptor
Ligand
BDBM18627
Substrate
n/a
Meas. Tech.
ChEMBL_1736311 (CHEMBL4151847)
IC50
20±n/a nM
Citation
Rew, Y; Du, X; Eksterowicz, J; Zhou, H; Jahchan, N; Zhu, L; Yan, X; Kawai, H; McGee, LR; Medina, JC; Huang, T; Chen, C; Zavorotinskaya, T; Sutimantanapi, D; Waszczuk, J; Jackson, E; Huang, E; Ye, Q; Fantin, VR; Sun, D Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101). J Med Chem 61:7767-7784 (2018) [PubMed] Article
More Info.:
Target
Name:
Glucocorticoid receptor
Synonyms:
GCR_PIG | GRL | Glucocorticoid receptor | NR3C1 | Nuclear receptor subfamily 3 group C member 1
Type:
PROTEIN
Mol. Mass.:
85641.70
Organism:
Sus scrofa
Description:
ChEMBL_118201
Residue:
782
Sequence:
MDPKESLTPPSREEIPSSVLGRERAHVMDFYKSLRGGTPVKVSAASPSLAAVSQPDSKQQRLAVDFPKGSGSNAQQPDLSKAVSLSMGLYMGETETKVMGSDLGFPQQGQISLSSGETDFRLLEESIANLSRSTSVPENPKSSASAAGPAAPAEKAFPKTHSDGAPEQPNVKGQTGTNGGNVKLFTTDQSTFDIWRKKLQDLELPSGSPGKETSESPWSSDLLIDENCLLSPLAGEEDPFLLEGSSTEDCKPLVLPDTKPKVKDNGELILPSPNSVPLPQVKTEKEDFIELCTPGVIKQEKLGPAYCQASFSGANIIGGKMSAISVHGVSTSGGQLYHYDMNTAASLSKQQEQKPLFNVIPPIPVGSENWNRCQGSGDDNLTSLGTLNFSGRSVFSNGYSSPGMRPDVSSPPSSSSAATGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATTGVSQETSENSANKTIVPATLPQLTPTLVSLLEVIEPEVLYAGYDSSIPDSTWRIMTALNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSWMFLMVFALGWRSYRQSSASLLCFAPDLVINEQRMALPCMYDQCRHMLYVSSELQRLQVSYEEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTKLLDSMHDVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQLPKYSSGNIKKLLFHQK
Inhibitor
Name:
BDBM18627
Synonyms:
(10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one | Mifeprex | Mifepristone | RU-486 | RU486 (tetramethyl-rhodamine conjugated)
Type:
Small organic molecule
Emp. Form.:
C29H35NO2
Mol. Mass.:
429.5937
SMILES:
[H][C@@]12CC[C@@](O)(C#CC)[C@@]1(C)C[C@@H](C1=C3CCC(=O)C=C3CC[C@@]21[H])c1ccc(cc1)N(C)C |r,c:14,20|