Skip to main content
. Author manuscript; available in PMC: 2019 Dec 27.
Published in final edited form as: J Med Chem. 2019 Dec 5;62(24):11232–11259. doi: 10.1021/acs.jmedchem.9b01411

Table 3.

Structures and biochemical data for salicylamide derived WDR5 WBM-site inhibitors

graphic file with name nihms-1061210-t0024.jpg

Compound R1 R2 R3 R4 FPA Kd (μM) a
7a graphic file with name nihms-1061210-t0025.jpg graphic file with name nihms-1061210-t0026.jpg OH H 0.746 ± 0.033
7b Cl 0.298 ± 0.087


7c graphic file with name nihms-1061210-t0027.jpg OH H 1.42 ± 1.59
7d Cl 0.238 ± 0.089


7e graphic file with name nihms-1061210-t0028.jpg H H 0.848 ± 0.187
7f OH H 0.204 ± 0.030
7g Cl 0.190 ± 0.032


7h graphic file with name nihms-1061210-t0029.jpg H H 1.08 ± 0.43
7i Cl 0.128 ± 0.020
7j OH H 0.566 ± 0.024
7k Cl 0.069 ± 0.034


7l graphic file with name nihms-1061210-t0030.jpg OH H 0.779 ± 0.484
7m Cl 0.362 ± 0.040

7n b graphic file with name nihms-1061210-t0031.jpg graphic file with name nihms-1061210-t0032.jpg OH H 0.046 ± 0.014
7o 0.757 ± 0.017

7p graphic file with name nihms-1061210-t0033.jpg graphic file with name nihms-1061210-t0034.jpg H H 1.88 ± 0.48
7q Cl 0.220 ± 0.031
7r OH H 1.07 ± 0.30
7s Cl 0.123 ± 0.05


7t graphic file with name nihms-1061210-t0035.jpg H H 0.511 ± 0.050
7u Cl 0.093 ± 0.001
7v OH H 0.167 ± 0.049
7w Cl 0.045 ± 0.013


7x graphic file with name nihms-1061210-t0036.jpg H Cl 0.215 ± 0.058
7y OH H 0.349 ± 0.174
7z Cl 0.110 ± 0.057
a

Data displayed is the average of at least 3 independent replicates ± standard deviation;

b

Data is the average of two independent replicates.