Table 1 Potency and selectivity of cyclic peptide hits from the RaPID system.
From: Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
IC 50 (nM) | |||||
|---|---|---|---|---|---|
D Tyr-Library | L Tyr-Library | ||||
CP1 | CP2 | CP3 | CP4 | CP5 | |
KDM4A | >105 | 42 | >105 | 20 | 313 |
KDM4B | — | 33 | — | 6 | 472 |
KDM4C | — | 39 | >105 | 17 | 123 |
KDM4D | — | 6,270 | — | 6,260 | >104 |
KDM4E | — | 9,200 | — | 4,700 | 8,900 |
KDM2A | — | >104 | — | >104 | >104 |
KDM3A | — | >104 | — | 9,900 | >104 |
KDM5C | — | >104 | — | >104 | >104 |
KDM6B | — | 6,800 | — | 7,200 | >104 |
KDM1A | — | >104 | — | >104 | >104 |
PHD2 | — | >106 | — | >106 | >106 |
FIH | — | >106 | — | >106 | >106 |
KDM4A Binding | |||||
Kd (nM) | 29.8 | 36.0 | 173 | ||
kon (1/Ms) | 1.37 × 105 | 2.18 × 104 | 6.2 × 104 | ||
kdiss (1/s) | 4.07 × 10−3 | 7.84 × 10−4 | 1.07 × 10−2 | ||
