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. Author manuscript; available in PMC: 2024 May 20.
Published in final edited form as: J Med Chem. 2024 Mar 29;67(7):5333–5350. doi: 10.1021/acs.jmedchem.3c01596

Table 6.

Off-targets interactions of SI-12 (6c) and SI-10 (6p)a

Compound Target Class Assay Name Assay Target Mode RC50 (µM)b

SI-12 GPCR Calcium Flux EDNRA Agonist 6.4c
Calcium Flux EDNRA Antagonist 4.0
Calcium Flux HTR2B Antagonist 4.1
cAMP OPRM1 Antagonist 3.1
Ion Channel Ion Channel hERG Blocker 2.7
Non-Kinase Enzymes Enzymatic COX1 Inhibitor 3.1
Enzymatic COX2 Inhibitor 3.0

SI-10 Non-Kinase Enzymes Enzymatic COX1 Inhibitor 2.9
Enzymatic COX2 Inhibitor 2.4
a

Data was obtained by using SafetyScreen panel provided by Eurofins Discovery.

b

RC50 is described as IC50 unless otherwise specified.

c

RC50 is EC50.