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

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 1.2 21 350 >20,000 n.a. 250
G691S 1.1 8.2 185 18,000 n.a. 240
R749T 2.0 5.5 140 2,600 n.a. 48
E762Q 1.5 20 380 26,000 n.a. 350
V778I 5.0 4.0 82 16,600 n.a. 66
L790F 5.1 1.4 39 10,000 n.a. 78
Y791F 0.5 5.2 94 10,000 n.a. 230
V804E 4.2 3,100 9,200 12,000 n.a. 420
V804L 4.9 84,000 130,000 n.a. n.a. 1,900
V804L-KIF5B 1.1 >100,000 48,000 n.a. >100,000 310
V804M 0.53 11,600 47,000 29,400 n.a. 561
V804M-KIF5B 2.8 >100,000 31,000 n.a. >100,000 340
Y806H 4.7 17 850 >100,000 n.a. 340
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
R813Q 1.0 4.8 150 12,000 n.a. 260
A883F 9.6 4.0 75 19,600 n.a. 550
S891A 2.6 3.5 26 8,500 n.a. 16
S904A 3.5 11 230 12,000 n.a. 55
S904F 2.3 9.0 150 13,000 n.a. 130
R912P 3.6 9.3 210 n.a. >100,000 103
M918T 1.0 15 340 26,000 n.a. 360
BCR 2.2 13 160 15,700 n.a. 120
CCDC6-PTC1 3.4 4.2 51 17,000 n.a. 41
KIF5B-Kex15Rex14 11 6.8 120 n.a. >100,000 72
NCOA4-PTC3 4.5 4.2 72 18,000 n.a. 74
PRKAR1A-PTC2 4.4 3.7 91 27,000 n.a. 54
Screening Location

Malvern, USA