“One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type Macrocycles

Table 1

Competitive FRET-melting results of the 8 ligands selected after the second selection step.

	in Na^+-conditions				in K^+-conditions
	Δ𝑇1/2 (^∘C)			^FRET𝑆	Δ𝑇1/2 (^∘C)			^FRET𝑆
	no competitior	+3𝜇M ds26	+10𝜇M ds26	10𝜇M ds26	no competitior	+3𝜇M ds26	+10𝜇M ds26	10𝜇M ds26
2,9-BisPN	13.7	12.9	8.6	0.62	16.8	10.6	12.0	0.71
2,7-NP/2,7-A	19.9	16.8	13.5	0.68	20.1	17.6	16.1	0.79
BisNP-1PY	31.9	24.3	22.9	0.71	29.7	23.9	21.5	0.72
BisNP-2PY	33.2	11.8	12.0	0.36	25.9	16.5	12.6	0.48
BisNP-1FC	31.8	18.8	16.1	0.50	25.8	19.1	17.2	0.66
BisNP-2FC	18.2	10.7	9.3	0.51	13.6	12.7	11.5	0.84
2,7-TrisNP	23.4	9.5	11.6	0.49	22.8	16.9	13.1	0.57
3,3^-TrisBP	13.0	9.7	13.1	1.01	14.9	14.7	14.7	0.98