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. 2018 Jul 14;175(17):3470–3485. doi: 10.1111/bph.14388

Table 1.

SAR of ATV399 led to compounds with increased potency

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Entry Compound Structure EC50 (μM) Entry Compound Structure EC50 (μM)
1 ATV399

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2.90 8 CAT639

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0.48
2 CAT628

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>20 9 CAT636

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3.10
3 CAT640

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>20 10 CBD498

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1.2
4 CAT635

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8.75 11 CBD504

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0.098
5 CAT648

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9.54 12 CBD505

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0.12
6 CAT646

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>20 13 CBD501

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0.91
7 CAT634

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>20 14 CBE173

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8.8

Rat insulin‐producing INS1E cells were pretreated with compounds at different doses (n = 6) for 24 h, followed by co‐treatment with pro‐inflammatory cytokines (10 ng·mL−1 IL‐1β and 100 ng·mL−1 IFNγ) for an additional 24 h. Then cleaved caspase‐9 levels were determined using caspase‐9 Glo, and the luminescence signal evolved was read and used to calculate EC50 values.