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

From: Data driven polypharmacological drug design for lung cancer: analyses for targeting ALK, MET, and EGFR

Compound 1 2a 2b
Kd study (nM)
 ALK 800 340 390
 MET >1000 250 330
 EGFRLR* 420 710 780
 EGFRLR+TM§ 110 110 270
Kd values comparing 1 or 6 h incubation times (nM)
 EGFRLR (1 h) 57 (10%) 340 (14%) 170 (65%)
 EGFRLR+TM (1 h) 25 (13%) 56 (14%) 58 (170%)
 EGFRLR (6 h) 5.7 47 110
 EGFRLR+TM (6 h) 3.2 8 100
Apparent Kd values with 30× dilution after 1 h incubation (nM)
 EGFRLR (30× dilution) 32 (56%) 340 (100%) 2900 (5.9%)
 EGFRLR+TM (30× diution) 12 (48%) 56 (100%) 4100 (1.4%)
  1. *EGFR (L858R)
  2. §EGFR (L858R, T790M)
  3. Percentages significantly lower than 100% indicate slow association
  4. Percentages significantly higher than 3% indicate slow dissociation