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] |