Binding kinetics of pirtobrutinib with BTK and BTK C481 substitution mutants
| Pirtobrutinib . | Average kon, M-1s-1 . | Average koff, s-1 . | Average KD, nM . | Average t1/2, h . | n . |
|---|---|---|---|---|---|
| BTK | 8.2 E+04 | 7.9 E−05 | 1.0 | 2.4 | 3 |
| BTK C481S | 8.5 E+04 | 1.3 E−04 | 1.5 | 1.5 | 3 |
| Pirtobrutinib . | Average kon, M-1s-1 . | Average koff, s-1 . | Average KD, nM . | Average t1/2, h . | n . |
|---|---|---|---|---|---|
| BTK | 8.2 E+04 | 7.9 E−05 | 1.0 | 2.4 | 3 |
| BTK C481S | 8.5 E+04 | 1.3 E−04 | 1.5 | 1.5 | 3 |
KD, dissociation equilibrium constant (nM) = koff/kon; koff, dissociation rate constant (s–1); kon, association rate constant (M–1s–1); n, number of samples; t1/2, complex half-life (hours) = ln 2/koff.