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Table 1 On and off target profile of pentacyclic acridinium salts 1, 2 and 3

From: On and off-target effects of telomere uncapping G-quadruplex selective ligands based on pentacyclic acridinium salts

Compound Off-target effects: cardiac receptor inhibition On-target effects: ligand-quadruplex interaction
hERG % inhib. (10 μM) B2 adrenergic % inhib. (10 μM) Surface plasmon resonancea(K x 107 M-1) CD study thermal stabilityd
Quadruplex (Q) DNAb Duplex (D) DNAc Ratio Q/D Tm/°C ∆Tme
1 100 100 0.83 0.06 13.8 86 ± 3 16
2 42.5 24 1.5 0.04 37.5 89 ± 3 19
3 21 29 0.8 0.07 11.4 85 ± 3 15
  1. aBuffer solution: 10 mM HEPES, 200 mM KCl, 3 mM EDTA and 0.01% P20 surfactant with the final pH adjusted to 7.4.
  2. bHuman telomeric sequence 5′-d[AGGG(TTAGGG)3]-3′.
  3. c5′-d[CGA3T3C(CT)2GA3T3CG]-3′ hairpin sequence.
  4. dThermal stability data for h-Tel (anti-parallel) determined by CD in the absence and presence of compounds.
  5. eTm for unaligned h-Tel = 70 ± 3.