Table 1.

The inhibitor binding constant (Kd) of crenolanib for RTKs

RTKCrenolanib Kd (nmol/L)
CFS1R30
FLT30.74
KIT78
PDGFRA2.1
PDGFRB3.2

NOTE: Crenolanib was profiled using the commercially available KINOMEscan: Kd ELECT screening service as previously described (18, 19). Kd measurements were based on a competition-binding assay that quantitatively measures the ability of a compound to compete with an immobilized, active-site directed ligand. Inhibitor binding constants (Kd values) were calculated from duplicate 11-point dose–response curves. Measurements were made under optimized conditions that generate true thermodynamic Kd values that facilitate direct comparison of inhibitor affinity across kinases.