Table 6 Thermodynamic data for MAI-516 binding to APC and mutated APC

From: Rational design of a sensitivity-enhanced tracer for discovering efficient APC–Asef inhibitors

Compound

Protein

L/P ratio

Kd [µM]

ΔG [kJ mol−1]

ΔH [kJ mol−1]

-TΔS [kJ mol−1]a

MAI-516

APC WT

0.97

0.0044

−48.5

−68.8

20.3

MAI-516

APC W593A

0.92

0.40

−37.1

−48.1

11.0

MAI-516

APC N641A

0.88

0.012

−46.0

−68.8

22.8

MAI-516

APC W593A, N641A

0.77

0.86

−35.3

−55.8

20.5

MAIT-516

APC WT

1.6

0.067

−41.7

−36.8

−4.90

TAT + linker

APC WT

N.A.

N.A.

N.A.

N.A.

N.A.

  1. aAll experiments were performed at 30 °C. The L/P ratio indicates the number of sites per APC. ΔH: change in enthalpy; -TΔS: change in entropy; Kd: equilibrium dissociation constant determined by ITC.
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