Skip to main content
. Author manuscript; available in PMC: 2015 Jul 7.
Published in final edited form as: Sci Transl Med. 2015 Jan 7;7(269):269ra3. doi: 10.1126/scitranslmed.3010597

Table 3. Interaction of 4-hydroxy-2-pyridones with InhA.

Compound Mtb MIC50 (μM) InhA IC50 (μM) Thermaflor assay (Tm °C) ITC (+NADH)
E-NAD+-I E-NADH-I ΔTm Kd (μM) ΔH (cal.mol-1) ΔS (cal.mol-1) N
NITD-529 1.54 9.6±0.7 50.3 54.7 4.4 25 ± 7 13100 ± 4202 -22.9 0.97 ± 0.23
NITD-564 0.16 0.59±0.05 56.3 57.8 1.5 0.56 ± 0.07 11440 ± 250 -9.8 1.04 ± 0.02
NITD-916 0.05 0.57±0.04 55 56.3 1.3 - - - -
NITD-560 > 20 > 20 - - - - - - -
NITD-716 2.67 4.3±0.5 - - - - - - -
NITD-526 >20 > 20 - - - - - - -
PT70a 11a <0.05a 66.7 60.1 -6.6 - - - -
PT166b 10.5b <0.05b 52.3 71.5 19.2 - - - -

- ‘not determined’;

a

Pan et al 2014 (19);

b

Schiebel et al 2014 (18)