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. 2024 Nov 6;63(49):e202410139. doi: 10.1002/anie.202410139

Figure 2.

Figure 2

SR2211‐based azologues MROR 1–5 as photoswitchable RORγ ligands. a) A SR2211 azologue. b) Docking of SR2211 and E/Z‐MROR 3 into the RORγ LBD (PDB: 6NWT; [29] the low score for E‐MROR 3, and its unrealistic pose, are coherent with a steric clash). c) Synthesis of MROR 3. d) Structures of MROR 1–5. e) Docking scores of E/Z‐azologues. f) Representative UV/Vis spectra, as all‐E (dark) or mostly‐Z (PSS 365 nm) (Figure S2a). g–h) Mostly‐Z‐MROR 1–5 are submicromolar inverse RORγ agonists, similar to SR2211; [22] but their E‐isomers are not weaker enough to qualify as usefully switchable ligands (Figure S3a), data shown as mean±S. E. M. from at least three independent experiments each with two technical replicates.