Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50368933 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1736311 (CHEMBL4151847) |
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IC50 | 39±n/a nM |
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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 Chem61:7767-7784 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Glucocorticoid receptor |
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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: | MDPKESLTPPSREEIPSSVLGRERAHVMDFYKSLRGGTPVKVSAASPSLAAVSQPDSKQQ
RLAVDFPKGSGSNAQQPDLSKAVSLSMGLYMGETETKVMGSDLGFPQQGQISLSSGETDF
RLLEESIANLSRSTSVPENPKSSASAAGPAAPAEKAFPKTHSDGAPEQPNVKGQTGTNGG
NVKLFTTDQSTFDIWRKKLQDLELPSGSPGKETSESPWSSDLLIDENCLLSPLAGEEDPF
LLEGSSTEDCKPLVLPDTKPKVKDNGELILPSPNSVPLPQVKTEKEDFIELCTPGVIKQE
KLGPAYCQASFSGANIIGGKMSAISVHGVSTSGGQLYHYDMNTAASLSKQQEQKPLFNVI
PPIPVGSENWNRCQGSGDDNLTSLGTLNFSGRSVFSNGYSSPGMRPDVSSPPSSSSAATG
PPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPA
CRYRKCLQAGMNLEARKTKKKIKGIQQATTGVSQETSENSANKTIVPATLPQLTPTLVSL
LEVIEPEVLYAGYDSSIPDSTWRIMTALNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTL
LQYSWMFLMVFALGWRSYRQSSASLLCFAPDLVINEQRMALPCMYDQCRHMLYVSSELQR
LQVSYEEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRF
YQLTKLLDSMHDVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQLPKYSSGNIKKLLFH
QK
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BDBM50368933 |
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n/a |
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Name | BDBM50368933 |
Synonyms: | CHEMBL4161754 |
Type | Small organic molecule |
Emp. Form. | C34H47NO2 |
Mol. Mass. | 501.7425 |
SMILES | [H][C@@]12CC[C@@](O)(C#CC(C)(C)C)[C@@]1(C)C[C@H](c1ccc(cc1)N(C)C(C)C)[C@]1([H])[C@@]3([H])CCC(=O)C=C3CC[C@@]21[H] |r,c:37| |
Structure |
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