EGFR Kinase Mutant Profiler Service

Activity-based EGFR mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.

Target Overview
CAT#

EGFR

Enzyme

Human EGFR

HGNC

EGFR

Synonym

Epidermal growth factor receptor, Receptor tyrosine-protein kinase ErbB-1

Assay Properties
Reaction

Substrate + [γ-33P]-ATP = 33P-Substrate + ADP

Readout

Enzymatic activity

Reference Compound IC50s (nM)
Mutant Staurosporine PP2 AG1478 PDGFR I-III EGFR/ErbB Inhibitor D-64406
WT 63 380 <0.1 21,000 n.a. 14,000
K716A 250 1,100 1.18 n.a. 0.1 8,700
K716A/T790M/C797S/L858R 1.2 1,200 1,100 n.a. >100,000 26,000
K716A/C797S/L858R 6.1 3,100 1,800 n.a. >100,000 58,000
K716Q/L718Q 10,000 >100,000 1.6 n.a. 0.2 >100,000
L718Q 29,000 61,000 1.6 n.a. 0.3 >100,000
G719C 240 220 0.5 80,000 n.a. 13,000
G719D 410 160 <1.0 48,000 n.a. 13,000
G719S 480 250 0.15 >100,000 n.a. 16,000
K728A 210 78 <1.0 n.a. 0.06 3,500
K728A/T790M/C797S/L858R 0.5 780 570 n.a. >100,000 9,300
d746 40 95 <1.0 38,000 n.a. 7,300
d746-750 27 320 0.2 >50,000 n.a. 6,300
d746-750/C775S/T790M/L858R 6.1 59 1,440 n.a. 3.2 >100,000
d746-750/T790M 0.9 4,700 2,900 >100,000 n.a. 29,000
d746-750/T790M/C797S 0.5 260 190 >100,000 n.a. 8,500
d746-750/T790M/C797S/L858R 0.8 174 350 n.a. >100,000 4,800
d746-750/C797A 16 53 <1.0 >100,000 n.a. 8,500
d746-750/C797S 14 37 <1.0 22,800 n.a. 3,000
L747S 175 230 <1.0 42,000 n.a. 21,000
d747-749 40 218 <1.0 31,000 n.a. 8,100
d747-749/A750P 6.0 63 <0.1 20,000 n.a. 5,400
d747-752/P753S 18 90 <0.1 62,000 n.a. 11,000
d752-579 67 167 <0.1 >100,000 n.a. 17,000
D761Y 78 210 <1.0 26,000 n.a. 12,500
A763_Y764insFHEA 124 220 <1.0 12,200 n.a. 6,300
A763_Y764insFQEA 260 61 <0.1 n.a. 0.2 5,500
A767_S768insTLA 14 105 2.1 n.a. 0.30 6,800
V769_D770insGE 190 210 2.4 n.a. 0.18 25,000
D770_N771insNPG 72 425 3.5 >100,000 n.a. 14,100
D770_N771insNPG/T790M 11 >100,000 2,000 n.a. 0.96 72,000
D770GY 110 216 <1.0 45,000 n.a. 20,000
N771_P772insH 57 290 1.7 n.a. 0.20 16,000
C775S/T790M/L858R 7.2 550 3,500 n.a. 0.99 >100,000
T790M 6.8 2,200 2,200 n.a. n.a. >20,000
T790M/L792F/C797S/L858R 0.5 7,500 2,200 n.a. >100,000 5,000
T790M/L792F/L858R 0.5 1,600 1,800 n.a. 1.7 6,900
T790M/L792H/C797S/L858R 1.7 9,800 25,000 n.a. >100,000 21,000
T790M/L792H/L858R 9.5 15,000 23,000 n.a. 17 28,000
T790M/C797S 9 4,300 2,200 >100,000 n.a. >100,000
T790M/C797S/L858R 0.8 2,200 1,200 >100,000 n.a. 69,000
L792F 14 130 <1.0 n.a. 0.08 2,200
L792F/L858R 65 530 0.9 n.a. 0.5 9,400
L792H 35 960 3.4 n.a. 0.22 9,500
L792H/C797S/L858R 78 1,900 2.4 n.a. 13 30,000
C797A 45 130 <1.0 8,800 n.a. 8,900
C797S 55 150 <1.0 9,100 n.a. 7,200
C797S/L858R 24 240 <0.5 36,000 n.a. 20,000
L858R 58 220 <0.5 n.a. 0.5 24,000
L858R/T790M 1.6 3,800 4,500 n.a. n.a. n.a.
L861Q 22.8 53.1 <0.1 n.a. n.a. 9,400
R999A 71 220 <0.1 n.a. 0.1 7,400
Screening Location

Malvern, USA

Further information

More information can be found on our website Kinase Assays.