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. 2021 Feb 18;26(6):1473–1481. doi: 10.1016/j.drudis.2021.02.009

Table 1.

Summary of currently available KMO inhibitors

KMO inhibitor IC50 (nM)a Structures Refs
m-NBA 900b graphic file with name fx1_lrg.gif [61]
Ro 61-8048 37b graphic file with name fx2_lrg.gif [62]
UPF-648 40 graphic file with name fx3_lrg.gif [63]
JM6 37b, c graphic file with name fx4_lrg.gif [64]
CHDI-340246 0.5 graphic file with name fx5_lrg.gif [65]
GSK180 6 graphic file with name fx6_lrg.gif [66]
Prodrug 1b 2600d graphic file with name fx7_lrg.gif [67]
a

IC50 values are for inhibition of human KMO unless stated otherwise.

b

IC50 with rat KMO.

c

The IC50 value for JM6 relates to the IC50 of the active compound Ro 61-8048 following release from the prodrug. Subsequent analyses of JM6 led to debate over this prodrug mechanism [68].

d

The IC50 value for prodrug 1b relates to the IC50 of the active compound 1 following release from the prodrug.