Table 1 Alk, Met, and EGFR binding properties of the test tricyclic compounds

K_d study (nM)

 ALK

800

340

390

 MET

>1000

250

330

 EGFR^LR*

420

710

780

 EGFR^LR+TM§

110

110

270

K_d values comparing 1 or 6 h incubation times (nM)^†

 EGFR^LR (1 h)

57 (10%)

340 (14%)

170 (65%)

 EGFR^LR+TM (1 h)

25 (13%)

56 (14%)

58 (170%)

 EGFR^LR (6 h)

5.7

47

110

 EGFR^LR+TM (6 h)

3.2

8

100

Apparent K_d values with 30× dilution after 1 h incubation (nM)^‡

 EGFR^LR (30× dilution)

32 (56%)

340 (100%)

2900 (5.9%)

 EGFR^LR+TM (30× diution)

12 (48%)

56 (100%)

4100 (1.4%)