EGFR Kinase Mutant Profiler Service

Target Overview

CAT#

EGFR

Enzyme

Human EGFR

HGNC

EGFR

Synonym

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

Scientific Information

P00533 (http://www.uniprot.org/uniprot/P00533)

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_N771insG	29	370	0.9	n.a.	0.01	12,500
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
N771_P772insN	22	150	0.4	n.a.	0.03	12,400
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	27	240	<1.0	n.a.	0.06	3,700
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
S768I	59	260	<0.1	n.a.	0.05	12,400
d746-750/T790M/L792F	0.6	1,100	1,000	n.a.	1.4	1,900
d746-750/T790M/L792H	0.5	2,500	13,000	n.a.	6.6	23,000
d746-750/T790M/L858R	0.7	330	740	n.a.	1.0	12,000
d746-750/T790M/L798I	0.5	1,100	380	n.a.	0.8	24,000
T790M/C797G/L858R	0.7	2,800	1,900	n.a.	>1,000	67,000
C797G/L858R	15	310	<1.0	n.a.	1.9	7,700
d746-750/G724S	1,500	4,400	6.5	n.a.	6.4	>100,000
d746-750/S768I	21	76	1.9	n.a.	2.0	7,300
L792H/L858R	18	810	8.0	n.a.	0.76	9,200
V948R	200	65	0.8	n.a.	0.4	10,000

Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website Kinase Assays.