Matches in SemOpenAlex for { <https://semopenalex.org/work/W3157029503> ?p ?o ?g. }
- W3157029503 endingPage "835" @default.
- W3157029503 startingPage "827" @default.
- W3157029503 abstract "Structure-activity relationship studies directed toward the replacement of the fused phenyl ring of the lead hexahydrobenzoindole RORγt inverse agonist series represented by 1 with heterocyclic moieties led to the identification of three novel aza analogs 5-7. The hexahydropyrrolo[3,2-f]quinoline series 5 (X = N, Y = Z=CH) showed potency and metabolic stability comparable to series 1 but with improved in vitro membrane permeability and serum free fraction. This structural modification was applied to the hexahydrocyclopentanaphthalene series 3, culminating in the discovery of 8e as a potent and selective RORγt inverse agonist with an excellent in vitro profile, good pharmacokinetic properties, and biologic-like in vivo efficacy in preclinical models of rheumatoid arthritis and psoriasis." @default.
- W3157029503 created "2021-05-10" @default.
- W3157029503 creator A5000059111 @default.
- W3157029503 creator A5000092354 @default.
- W3157029503 creator A5000346544 @default.
- W3157029503 creator A5002931465 @default.
- W3157029503 creator A5003175899 @default.
- W3157029503 creator A5003202592 @default.
- W3157029503 creator A5005778343 @default.
- W3157029503 creator A5006858899 @default.
- W3157029503 creator A5010115884 @default.
- W3157029503 creator A5014087380 @default.
- W3157029503 creator A5017297606 @default.
- W3157029503 creator A5019236230 @default.
- W3157029503 creator A5020311464 @default.
- W3157029503 creator A5022194215 @default.
- W3157029503 creator A5025914970 @default.
- W3157029503 creator A5029301946 @default.
- W3157029503 creator A5029331192 @default.
- W3157029503 creator A5031810848 @default.
- W3157029503 creator A5035812766 @default.
- W3157029503 creator A5036271380 @default.
- W3157029503 creator A5036777383 @default.
- W3157029503 creator A5044920435 @default.
- W3157029503 creator A5051819016 @default.
- W3157029503 creator A5052925180 @default.
- W3157029503 creator A5056566640 @default.
- W3157029503 creator A5056847110 @default.
- W3157029503 creator A5057221602 @default.
- W3157029503 creator A5071458554 @default.
- W3157029503 creator A5073841271 @default.
- W3157029503 creator A5077001547 @default.
- W3157029503 creator A5079494921 @default.
- W3157029503 creator A5082062664 @default.
- W3157029503 creator A5083385424 @default.
- W3157029503 creator A5086340418 @default.
- W3157029503 creator A5089945074 @default.
- W3157029503 creator A5091071516 @default.
- W3157029503 date "2021-04-30" @default.
- W3157029503 modified "2023-10-18" @default.
- W3157029503 title "Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis" @default.
- W3157029503 cites W1663154925 @default.
- W3157029503 cites W1980017607 @default.
- W3157029503 cites W2012077729 @default.
- W3157029503 cites W2024490058 @default.
- W3157029503 cites W2042064755 @default.
- W3157029503 cites W2042721486 @default.
- W3157029503 cites W2086610449 @default.
- W3157029503 cites W2115908495 @default.
- W3157029503 cites W2126162679 @default.
- W3157029503 cites W2142017607 @default.
- W3157029503 cites W2277986268 @default.
- W3157029503 cites W2297560509 @default.
- W3157029503 cites W2558726150 @default.
- W3157029503 cites W2589882987 @default.
- W3157029503 cites W2744361627 @default.
- W3157029503 cites W2884925592 @default.
- W3157029503 cites W2909054118 @default.
- W3157029503 cites W2981523801 @default.
- W3157029503 cites W2981833062 @default.
- W3157029503 cites W3014530086 @default.
- W3157029503 cites W3033752684 @default.
- W3157029503 cites W3047020896 @default.
- W3157029503 cites W3094996529 @default.
- W3157029503 cites W3129885277 @default.
- W3157029503 cites W79750953 @default.
- W3157029503 doi "https://doi.org/10.1021/acsmedchemlett.1c00112" @default.
- W3157029503 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8155243" @default.
- W3157029503 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34055233" @default.
- W3157029503 hasPublicationYear "2021" @default.
- W3157029503 type Work @default.
- W3157029503 sameAs 3157029503 @default.
- W3157029503 citedByCount "2" @default.
- W3157029503 countsByYear W31570295032023 @default.
- W3157029503 crossrefType "journal-article" @default.
- W3157029503 hasAuthorship W3157029503A5000059111 @default.
- W3157029503 hasAuthorship W3157029503A5000092354 @default.
- W3157029503 hasAuthorship W3157029503A5000346544 @default.
- W3157029503 hasAuthorship W3157029503A5002931465 @default.
- W3157029503 hasAuthorship W3157029503A5003175899 @default.
- W3157029503 hasAuthorship W3157029503A5003202592 @default.
- W3157029503 hasAuthorship W3157029503A5005778343 @default.
- W3157029503 hasAuthorship W3157029503A5006858899 @default.
- W3157029503 hasAuthorship W3157029503A5010115884 @default.
- W3157029503 hasAuthorship W3157029503A5014087380 @default.
- W3157029503 hasAuthorship W3157029503A5017297606 @default.
- W3157029503 hasAuthorship W3157029503A5019236230 @default.
- W3157029503 hasAuthorship W3157029503A5020311464 @default.
- W3157029503 hasAuthorship W3157029503A5022194215 @default.
- W3157029503 hasAuthorship W3157029503A5025914970 @default.
- W3157029503 hasAuthorship W3157029503A5029301946 @default.
- W3157029503 hasAuthorship W3157029503A5029331192 @default.
- W3157029503 hasAuthorship W3157029503A5031810848 @default.
- W3157029503 hasAuthorship W3157029503A5035812766 @default.
- W3157029503 hasAuthorship W3157029503A5036271380 @default.
- W3157029503 hasAuthorship W3157029503A5036777383 @default.
- W3157029503 hasAuthorship W3157029503A5044920435 @default.
- W3157029503 hasAuthorship W3157029503A5051819016 @default.