Table 2.

HDAC inhibition and physicochemical properties of full‐sized inhibitors 10 a–c.

	R1	Physicochemical Properties		IC50 [nM]
		LogD7.4	Solubility[a,e] [μg/mL]	HDAC1[b,e]	HDAC2[b,e]	HDAC3[b,e]	HDAC6[c,e]
10 a		3.16	0.21±0.03	41.8±0.2	100.2±2.6	>6,666[d]	>10,000[d]
10 b		2.68	1.99±0.04	41.1±3.7	85.5±11.6	>3,333[d]	>10,000[d]
10 c		2.29	7.48±0.33	26.2±0.9	59.3±7.9	16,820±2,515	>10,000[d]
VK‐1	–	3.19	0.98±0.10	68.6±10.4	128.2±14.5	310.4±7.8	>10,000[d]
entinostat	–	n.d.	n.d.	426.1±58.7	354.0±43.1	310.5±9.8	>10,000[d]
vorinostat	–	0.99	255±3.71	113.0±16.9	191.4±15.4	109.5±9.7	21.7±3.2

[a] PBS buffer, pH=7.4; [b] preincubation of enzyme and inhibitor 1 h at 25 °C; [c] preincubation of enzyme and inhibitor 15 min at 25 °C; [d] <25 % inhibition at stated concentration; n.d.: not determined, [e] mean ±SD, at least two independent experiments.