| Assay Method Information | |
| | Evaluation of Pyrazolopyrimidine and Triazine Derivatives |
| Description: | The binding affinities of the compounds to EphA2 were investigated by microscale thermophoresis (MST) (M. Jerabek-Willemsen et al., J. Mol. Struct. 2014, 1077, 101-113). The dissociation constants of compounds @1 and @3 determined by MST (towards EphA2) are in the low nanomolar range (KD=3-4 nM), whereas the corresponding NVPiso derivative @2 (KD=132 nM) shows 44-fold lower binding affinity towards EphA2. The derivatives @4 and @5 are less potent than the pyrazolopyrimidine derivatives @1 and @3, showing an increased KD of 86 and 225 nM, respectively (Table 2). The affinities of the triazine derivatives towards EphA2 cover a broad range from low nanomolar to micromolar. Correlation with the substitution patterns indicates that a nitrogen at position 3 (3-pyridyl or imidazole) of the triazine substituent may be important for generating affinity. |
| Affinity data for this assay | |
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