RET Kinase Mutant Profiler Service

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

Target Overview
CAT#

RET

Enzyme

Human RET

HGNC

RET

Synonym

Proto-oncogene tyrosine-protein kinase receptor ret [Precursor], C-ret

Scientific Information

P07949 (http://www.uniprot.org/uniprot/P07949)

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 7.1 24 260 n.a. >100,000 104
G691S 4.3 20 280 n.a. >100,000 180
R749T 4.9 17 230 n.a. >100,000 130
E762Q 8.0 28 480 n.a. >100,000 260
V778I 5.2 36 500 n.a. >100,000 250
L790F 15 13 140 n.a. >100,000 330
Y791F 9.8 37 34 n.a. >100,000 240
V804E 2.3 9,200 28,000 n.a. >100,000 400
V804L 2.2 >100,000 >100,000 n.a. >100,000 540
V804L-KIF5B 1.7 >100,000 >100,000 n.a. >100,000 350
V804M/G810S 17 >100,000 >100,000 n.a. >100,000 2,700
V804M 0.3 4,100 11,000 n.a. >100,000 150
V804M-KIF5B 1.4 >100,000 >100,000 n.a. >100,000 320
Y806H 8.0 78 1,900 n.a. >100,000 790
G810C 260 50 15,300 n.a. >100,000 3,600
G810R 460 35 21,700 n.a. >100,000 5,800
G810S 340 240 6,700 n.a. >100,000 4,100
G810S/M918T 194 70 1,500 n.a. >100,000 1,800
R813Q 3.9 6.7 120 n.a. >100,000 120
A883F 6.2 10 140 n.a. >100,000 440
S891A 1.0 26 110 n.a. >100,000 73
S904A 6.3 21 200 n.a. >100,000 110
S904F 7.7 27 310 n.a. >100,000 120
R912P 5.2 24 260 n.a. >100,000 130
M918T 4.3 21 290 n.a. >100,000 130
BCR 6.2 31 510 n.a. >100,000 140
CCDC6-PTC1 5.1 28 450 n.a. >100,000 140
KIF5B-Kex15Rex14 4.3 23 290 n.a. >100,000 115
NCOA4-PTC3 5.0 27 330 n.a. >100,000 160
PRKAR1A-PTC2 3.8 33 320 n.a. >100,000 120
E732K 6.0 30 610 n.a. >100,000 220
L730I 190 120 5,000 n.a. >100,000 1,500
L730M 43 20 360 n.a. >100,000 270
V738A 30 410 3,700 n.a. >100,000 1,000
Y806C 110 110 2,100 n.a. >100,000 1,000
Y806N 80 130 6,900 n.a. >100,000 2,200
Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website Kinase Assays