CRTh2 antagonist 3 is a potentchemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2)antagonist^[1]. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with anEC₅₀of 2 μM and aK_dof 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation^[2].

CRTh2^[1]
EC50: 2 μM (PDK1)^[2]
Ki: 8.4 μM (PDK1)^[2]

CRTh2 antagonist 3 (compound 4) is a small-molecule allosteric modulator of the protein kinase PDK1 from structure-based docking. CRTh2 antagonist 3 is 5-fold more potent than its parent compound^[2].

356.44

C₁₉H₂₀N₂O₃S

312928-72-6

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