Table 3 Cell based NNMT inhibition and determination of MNA in cells (Target engagement).

From: Novel tricyclic small molecule inhibitors of Nicotinamide N-methyltransferase for the treatment of metabolic disorders

Compound

Cell based inhibition in U2OS EC50 [µM]

% MNA reduction (time point [h])*

(1)

2.5 ± 0.3

30 (0.5)

(2)

2.2 ± 0.1

21 (0.5)

(3)

 > 3

14 (1.0)

(6)

2.5 ± 0.3

75 (1.0)

(8)

1.1 ± 0.2

30

(9)

 > 3

43 (0.25)

(13)

 > 10

40 (1.0)

(18)

2.5 ± 0.2

30 (0.5)

  1. *Time point after addition of compound at which maximal MNA reduction was observed relative to control without compound.
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