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. 2019 Aug 20;63(5):2308–2324. doi: 10.1021/acs.jmedchem.9b01112

Table 2. Effects of Thiophene vs Thiazole Cores on LOXL2 Potency.

graphic file with name jm9b01112_0015.jpg

entry compd X R1 R2 SO2Me position LOXL2, IC50 (μM)a
1 3a CH H H 3 0.176
            [0.105, 0.295]
2 3b CCl H H 3 2.488
            2.164
3 3c CF H H 3 0.671
            0.714
4 7a N H H 3 0.086
            [0.061, 0.119]
5 7b N CH3 H 3 68.26
            [43.77, 106.5]
6 8 CH H CH3 4 0.686
            [0.456, 1.031]
7 9 N H CH3 4 0.423
            [0.302, 0.593]
a

Reported IC50 values were determined using 1 h preincubation in at least two separate experiments (n ≥ 2). When n = 2, individual IC50 values are shown. When n > 2, the values are reported as the geometric mean with the corresponding 95% confidence interval in square brackets.