Table 4. Physicochemical Properties and Cellular Potency for Key Analogues.

Cmpd	1	13	29
LogD, TPSA, LEa	–, 100, 0.3	3.5, 89, 0.34	2.7, 86, 0.34
Kinetic sol. (μM)	11	4	61
TMLR Ki (μM)b	0.065	0.019	0.015
wtEGFR Select.c	<1×	58×	29×
pEGFR H1975 EC50 (μM)b	0.412	1.09	0.433
pEGFR Select. vs H292d		5×	>23×
H/RLMe	11/31	14/41	11/29
H/R CLhepf	13/35	12,24	8/25

^aLE calculated using TMLR K_i.

^bK_i and EC₅₀ data are an average of at least two independent experiments.

^cRatio of wtEGFR K_iapp over EGFR(TMLR) K_iapp.

^dRatio of pEGFR EC₅₀ in H292 cells over pEGFR EC₅₀ in H1975 cells.

^eH/RLM defined as predicted hepatic clearance in liver microsomes for human (H) and rat (R). Reported in units of mL/min/kg.

^fH/R CLhep defined as predicted hepatic clearance in hepatocytes for human (H) and rat (R). Reported in units of mL/min/kg.