ResidenceTimer™ Off-the-Shelf Assays

Kinase Panel

The table contains an overview of kinase assays that are available for measurement of target residence time.

Kinase Domain Reference therapeutics Preview details
ABL (ABL1) Full-length bosutinib, dasatinib, imatinib, ponatinib [pdf]
ACVR2A Cytoplasmic domain dasatinib [pdf]
AKT1 Catalytic domain GSK690693 [pdf]
AKT2 Catalytic domain GSK690693 [pdf]
ALK Cytoplasmic domain alectinib, crizotinib [pdf]
ALK [C1156Y] Cytoplasmic domain GSK1838705 [pdf]
ALK [I1171N] Cytoplasmic domain brigatinib [pdf]
ALK [I1171N/L1198F] Cytoplasmic domain brigatinib [pdf]
ALK [I1171S] Cytoplasmic domain ceritinib [pdf]
ALK [I1171T] Cytoplasmic domain brigatinib [pdf]
ALK [F1174L] Cytoplasmic domain crizotinib [pdf]
ALK [F1174L/G1202R] Cytoplasmic domain brigatinib [pdf]
ALK [L1196M] Cytoplasmic domain brigatinib, crizotinib [pdf]
ALK [L1196M/G1202R] Cytoplasmic domain TAE684 [pdf]
ALK [L1198F] Cytoplasmic domain gilteritinib [pdf]
ALK [V1180L] Cytoplasmic domain TAE684 [pdf]
ALK [G1202R] Cytoplasmic domain lorlatinib [pdf]
ALK [G1269A] Cytoplasmic domain brigatinib [pdf]
ALK [R1275Q] Cytoplasmic domain brigatinib [pdf]
AMPKα1/β1/γ1 Full-length GSK690693, WZ4003 [pdf]
AMPKα1/β2/γ1 Full-length fasudil, GSK690693, TAE684, WZ4003 [pdf]
AurA (AURKA) Full-length MK-5108, pan-Aurora inhibitors [pdf]
AurB (AURKB)* Full-length MK-5108, pan-Aurora inhibitors [pdf]
AXL Cytoplasmic domain crizotinib, sunitinib [pdf]
BMX Full-length bosutinib, dasatinib [pdf]
BRAF Catalytic domain dabrafenib, vemurafenib [pdf]
BRK (PTK6)* Full-length ibrutinib [pdf]
BTK* Full-length dasatinib, ibrutinib, ponatinib [pdf]
BTK Full-length dasatinib, ibrutinib, ponatinib [pdf]
BTK [T316A]* Full-length fenebrutinib, ibrutinib [pdf]
BTK [T316A] Full-length acalabrutinib, fenebrutinib [pdf]
BTK [T474I]* Full-length ARQ-531, ibrutinib [pdf]
BTK [T474I] Full-length ARQ-531, ibrutinib [pdf]
BTK [T474S]* Full-length ARQ-531, ibrutinib [pdf]
BTK [C481S]* Full-length fenebrutinib [pdf]
BTK [C481S] Full-length fenebrutinib, ibrutinib [pdf]
CaMK2β (CAMK2B) Full-length midostaurin [pdf]
CaMK2δ (CAMK2D) Full-length sunitinib [pdf]
CDK1 (CDC2)/CycA2 Full-length dinaciclib, staurosporine [pdf]
CDK1 (CDC2)/CycB1 Full-length AT7519, dinaciclib, flavopiridol, PHA-793887, PHA-848125 [pdf]
CDK2/CycA2 Full-length dinaciclib, PHA-793887 [pdf]
CDK2/CycE1 Full-length SNS-032 [pdf]
CDK3/CycE1 Full-length AT7519 [pdf]
CDK4/CycD1 Full-length dinaciclib [pdf]
CDK4/CycD3 Full-length abemaciclib, dinaciclib, palbociclib, ribociclib [pdf]
CDK5/p25 Full-length dinaciclib, SNS-032 [pdf]
CDK6/CycD1 Full-length dinaciclib [pdf]
CDK6/CycD3* Full-length ribociclib [pdf]
CDK6/CycD3 Full-length ribociclib [pdf]
CDK7/CycH/MAT1 Full-length dinaciclib, pan-CDK inhibitors [pdf]
CDK8/CycC Full-length staurosporine [pdf]
CDK9/CycK Full-length dinaciclib, PHA-793887 [pdf]
CDK9/CycT1 Full-length dinaciclib, pan-CDK inhibitors [pdf]
CDK9/CycT2 Full-length dinaciclib, staurosporine [pdf]
CHK1 (CHEK1) Full-length bosutinib, sunitinib [pdf]
DDR1 Cytoplasmic domain imatinib [pdf]
DDR2* Cytoplasmic domain dasatinib, imatinib, ponatinib, sorafenib [pdf]
EGFR Cytoplasmic domain afatinib, erlotinib, gefitinib [pdf]
EGFR [d746-750] Cytoplasmic domain afatinib, erlotinib, gefitinib [pdf]
EGFR [d746-750/C797S] Cytoplasmic domain afatinib, erlotinib, gefitinib [pdf]
EGFR [d746-750/T790M/C797S/L858R] Cytoplasmic domain brigatinib [pdf]
EGFR [T790M] Cytoplasmic domain afatinib [pdf]
EGFR [T790M/L858R] Cytoplasmic domain osimertinib [pdf]
EGFR [C797S] Cytoplasmic domain afatinib [pdf]
EGFR [C797S/L858R] Cytoplasmic domain afatinib, erlotinib, gefitinib [pdf]
EGFR [L858R] Cytoplasmic domain afatinib [pdf]
EPHA2* Cytoplasmic domain BMS-777607, dasatinib, staurosporine [pdf]
EPHA2 Cytoplasmic domain dasatinib [pdf]
FAK (PTK2) Truncated crizotinib [pdf]
FGFR1* Cytoplasmic domain infigratinib, ponatinib [pdf]
FGFR1 Cytoplasmic domain infigratinib, ponatinib [pdf]
FGFR2* Cytoplasmic domain ponatinib [pdf]
FGFR2 Cytoplasmic domain ponatinib [pdf]
FGFR2 [C491A]* Cytoplasmic domain ponatinib [pdf]
FGFR2 [C491A] Cytoplasmic domain ponatinib [pdf]
FGFR2 [C491A/V564I]* Cytoplasmic domain dovitinib [pdf]
FGFR2 [C491A/V564I] Cytoplasmic domain ponatinib [pdf]
FGFR2 [N549H]* Cytoplasmic domain axitinib [pdf]
FGFR2 [N549H] Cytoplasmic domain axitinib [pdf]
FGFR2 [V564I]* Cytoplasmic domain axitinib [pdf]
FGFR2 [V564I] Cytoplasmic domain axitinib [pdf]
FGFR2 [V564L]* Cytoplasmic domain axitinib [pdf]
FGFR2 [V564L] Cytoplasmic domain axitinib [pdf]
FGFR3* Cytoplasmic domain infigratinib, sunitinib [pdf]
FGFR4 Cytoplasmic domain infigratinib, sunitinib [pdf]
FLT3* Cytoplasmic domain dasatinib, imatinib [pdf]
FLT3 Cytoplasmic domain crenolanib, gilteritinib, midostaurin, sunitinib [pdf]
FMS (CSF1R)* Cytoplasmic domain dasatinib [pdf]
FMS (CSF1R) Cytoplasmic domain dasatinib [pdf]
FYN [isoform a] Full-length dasatinib, ponatinib, regorafenib [pdf]
GCN2 (EIF2AK4) Full-length A-92 [pdf]
GSK3β (GSK3B) Full-length abemaciclib, staurosporine [pdf]
HPK1 (MAP4K1) Catalytic domain bosutinib [pdf]
IGF1R* Cytoplasmic domain cabozantinib, GSK1838705, staurosporine [pdf]
IGF1R Cytoplasmic domain brigatinib [pdf]
IKKα (CHUK)  Full-length IKKβ inhibitor [pdf]
IKKα (CHUK) [K44A] [inactive mutant] Full-length IKKβ inhibitor [pdf]
INSR* Cytoplasmic domain BMS-754807, ceritinib, GSK1838705A, linsitinib, NVP-ADW742 [pdf]
INSR Cytoplasmic domain BMS-754807, ceritinib, GSK1838705A, linsitinib, NVP-ADW742 [pdf]
IRAK4 Full-length crizotinib, sunitinib [pdf]
ITK* Full-length crizotinib, sunitinib [pdf]
JAK2 Catalytic domain staurosporine [pdf]
KDR (VEGFR2) Cytoplasmic domain vandetanib [pdf]
KIT* Cytoplasmic domain masitinib, pazopanib, staurosporine [pdf]
LATS2/MOBKL1A Catalytic domain staurosporine [pdf]
LCK Full-length ponatinib, regorafenib [pdf]
LIMK2 Full-length dasatinib [pdf]
LYNa Full-length ponatinib, regorafenib, tamatinib [pdf]
MAP2K1 [inactive] Full-length crizotinib, dasatinib, trametinib [pdf]
MAP3K5 Catalytic domain bosutinib, staurosporine, sunitinib [pdf]
MER (MERTK) Cytoplasmic domain BMS-777607 [pdf]
MET Cytoplasmic domain crizotinib [pdf]
MET [D1228H] Cytoplasmic domain foretinib [pdf]
MET [D1228N] Cytoplasmic domain foretinib [pdf]
MET [Y1230C] Cytoplasmic domain crizotinib [pdf]
MET [Y1230H] Cytoplasmic domain MET/RON inhibitor [pdf]
MET [M1250T] Cytoplasmic domain MET/RON inhibitor [pdf]
MLK1 (MAP3K9) Cytoplasmic domain bosunitib, dabrafenib, midostaurin, sunitinib [pdf]
MLK2 (MAP3K10) Cytoplasmic domain bosunitib, dabrafenib, midostaurin, sunitinib [pdf]
MLK3 (MAP3K11) Cytoplasmic domain bosunitib, dabrafenib, midostaurin, sunitinib [pdf]
MST2 (STK3) Full-length midostaurin [pdf]
MYLK4 Full-length dovitinib [pdf]
NuaK2 Full-length staurosporine [pdf]
p38α (MAPK14) Truncated sorafenib, p38 MAPK inhibitors [pdf]
p38α (MAPK14) [inactive] Truncated sorafenib, p38 MAPK inhibitors [pdf]
PAK4 Full-length bosutinib, GSK690693, staurosporine [pdf]
PAK6 Full-length staurosporine [pdf]
PDGFRα (PDGRFA)* Cytoplasmic domain axitinib, crenolanib, gilteritinib, nintedanib [pdf]
PDGFRα (PDGRFA) Cytoplasmic domain axitinib, crenolanib, gilteritinib, nintedanib [pdf]
PDGFRβ (PDGRFB)* Cytoplasmic domain axitinib, crenolanib, gilteritinib, nintedanib [pdf]
PDGFRβ (PDGRFB) Cytoplasmic domain axitinib, crenolanib, gilteritinib, nintedanib [pdf]
PIK3CA/PIK3R1 Full-length dactolisib, pictilisib [pdf]
PIK3CA [R88Q]/PIK3R1 Full-length idelalisib [pdf]
PIK3CA [P539R]/PIK3R1 Full-length idelalisib [pdf]
PIK3CA [E542K]/PIK3R1 Full-length idelalisib [pdf]
PIK3CA [E545K]/PIK3R1 Full-length idelalisib [pdf]
PIK3CA [H1047R]/PIK3R1 Full-length idelalisib [pdf]
PIK3CB/PIK3R1 Full-length apitolisib [pdf]
PIK3CD/PIK3R1 Full-length duvelisib, idelalisib [pdf]
PIK3CG Full-length apitolisib, dactolisib, duvelisib [pdf]
PIK3CG/PIK3R5 Full-length apitolisib, duvelisib [pdf]
PIKFYVE (PIP5K3) Full-length YM201636 [pdf]
PKACα (PRKACA) Full-length A-674563 [pdf]
PKCα (PRKCA) Full-length A-674563, enzastaurin, sotrastaurin [pdf]
PKCη (PRKCH) Full-length staurosporine [pdf]
PKN1 Full-length GSK690693 [pdf]
PLK1 Full-length GSK461364 [pdf]
PYK2 (PTK2B)* Full-length crizotinib [pdf]
RAF1 (CRAF) Catalytic domain dabrafenib [pdf]
RET Cytoplasmic domain dasatinib, ponatinib, regorafenib, sorafenib, vandetanib [pdf]
RET [G691S]* Cytoplasmic domain staurosporine [pdf]
RET [G691S] Cytoplasmic domain cabozantinib [pdf]
RET [Y791F]* Cytoplasmic domain staurosporine [pdf]
RET [Y791F] Cytoplasmic domain cediranib [pdf]
RET [V804M]* Cytoplasmic domain staurosporine [pdf]
RET [V804M] Cytoplasmic domain staurosporine [pdf]
RET [S891A]* Cytoplasmic domain staurosporine [pdf]
RET [S891A] Cytoplasmic domain quizartinib [pdf]
RET [M918T]* Cytoplasmic domain staurosporine [pdf]
RET [M918T] Cytoplasmic domain staurosporine [pdf]
ROCK1 Catalytic domain GSK 429286A [pdf]
SPHK1 Full-length PF-543 citrate [pdf]
SRC Full-length A-770041, ponatinib, regorafenib [pdf]
SRPK1 Full-length staurosporine [pdf]
SYK* Full-length staurosporine [pdf]
SYK Full-length staurosporine [pdf]
TBK1 Full-length staurosporine [pdf]
TGFβR1 (TGFBR1) Catalytic domain SB 431542 [pdf]
TIE2 (TEK)* Cytoplasmic domain ponatinib, vandetanib [pdf]
TNIK* Catalytic domain bosutinib, sunitinib [pdf]
TRKA (NTRK1)* Cytoplasmic domain AZ23, ponatinib [pdf]
TRKA (NTRK1) Cytoplasmic domain AZ23, ponatinib [pdf]
TRKB (NTRK2)* Cytoplasmic domain ponatinib [pdf]
TRKB (NTRK2) Cytoplasmic domain AZ23, ponatinib [pdf]
TRKC (NTRK3)* Cytoplasmic domain AZ23, sorafenib [pdf]
TYRO3* Cytoplasmic domain BMS-777607 [pdf]
TYRO3 Cytoplasmic domain BMS-777607 [pdf]
WEE1 Catalytic domain AZD1775 [pdf]
WNK1 Catalytic domain WNK463 [pdf]
WNK4 Catalytic domain WNK463 [pdf]
YES (YES1) Full-length saracatinib, staurosporine [pdf]
* Pre-activated by treatment with ATP after purification and before immobilization