Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM141378 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1680911 |
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IC50 | 0.290000±n/a nM |
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Citation | Hemmerling, M; Nilsson, S; Edman, K; Eirefelt, S; Russell, W; Hendrickx, R; Johnsson, E; Kärrman Mårdh, C; Berger, M; Rehwinkel, H; Abrahamsson, A; Dahmén, J; Eriksson, AR; Gabos, B; Henriksson, K; Hossain, N; Ivanova, S; Jansson, AH; Jensen, TJ; Jerre, A; Johansson, H; Klingstedt, T; Lepistö, M; Lindsjö, M; Mile, I; Nikitidis, G; Steele, J; Tehler, U; Wissler, L; Hansson, T Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. J Med Chem60:8591-8605 (2017) [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_RAT | Glucocorticoid | Glucocorticoid Receptor (GR) | Glucocorticoid receptor | Grl | Nr3c1 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 87556.83 |
Organism: | RAT |
Description: | Glucocorticoid 0 RAT::P06536 |
Residue: | 795 |
Sequence: | MDSKESLAPPGRDEVPGSLLGQGRGSVMDFYKSLRGGATVKVSASSPSVAAASQADSKQQ
RILLDFSKGSTSNVQQRQQQQQQQQQQQQQQQQQQQPDLSKAVSLSMGLYMGETETKVMG
NDLGYPQQGQLGLSSGETDFRLLEESIANLNRSTSVPENPKSSTSATGCATPTEKEFPKT
HSDASSEQQNRKSQTGTNGGSVKLYPTDQSTFDLLKDLEFSAGSPSKDTNESPWRSDLLI
DENLLSPLAGEDDPFLLEGNTNEDCKPLILPDTKPKIKDTGDTILSSPSSVALPQVKTEK
DDFIELCTPGVIKQEKLGPVYCQASFSGTNIIGNKMSAISVHGVSTSGGQMYHYDMNTAS
LSQQQDQKPVFNVIPPIPVGSENWNRCQGSGEDSLTSLGALNFPGRSVFSNGYSSPGMRP
DVSSPPSSSSAATGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRN
DCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATAGVSQDTSENPNKTIVP
AALPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSAWRIMTTLNMLGGRQVIAAVKWAKAIL
GLRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSGNLLCFAPDLIINEQRMSLPCMYDQ
CKHMLFVSSELQRLQVSYEEYLCMKTLLLLSSVPKEGLKSQELFDEIRMTYIKELGKAIV
KREGNSSQNWQRFYQLTKLLDSMHEVVENLLTYCFQTFLDKTMSIEFPEMLAEIITNQIP
KYSNGNIKKLLFHQK
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BDBM141378 |
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n/a |
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Name | BDBM141378 |
Synonyms: | US8916600, 12 | US9738632, Example 12 |
Type | Small organic molecule |
Emp. Form. | C34H31F2N5O5 |
Mol. Mass. | 627.6372 |
SMILES | C[C@H](NC(=O)C(C)(F)F)[C@H](Oc1ccc2n(ncc2c1)-c1cccc(c1)C(=O)NCc1cccnc1)c1ccc2OCCOc2c1 |r| |
Structure |
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