AssayQuantのKinSight™ Kinase Profilingでは、独自のPhosphoSens® Technologyを用いることにより、反応全体を通じて基質のリン酸化/脱リン酸化をリアルタイムで直接測定することが可能です。PhosphoSens®の中核をなすは、Chelation-enhancedのSox(スルホンアミドオキシン)蛍光色素です。Nativeなペプチド配列に基づいて設計されたPhosphoSens®基質により、基質レベルのリン酸化活性を、リアルタイムかつ定量的に測定します。Timie-dependent-inhibition (TDI)の特性評価も可能で、End-pointの阻害率評価だけでは分からない、化合物の選択性、最適化、オフターゲットの早期発見等に有用です。[ATP]はKmもしくは1 mMの選択が可能です。

Deliverables;
Detailed Kinetic Report for each compound that includes % inhibition presented in:
Numerical Format (Tabular), % inhibition for each enzyme
Graphical Format (Waterfall Plot), % inhibition for each enzyme
Graphical Format (Waterfall Plot), >70% inhibition
Visual Format (Kinome Tree), >70% inhibition
Also includes annotated progress curves for any exploitable mechanisms of actions (TDI).

KinSight™ Kinase Profiling

Target nameSer(S)/Thr(T) or Tyr(Y)Full panelWT panelTyrosine panelCDK panelMutant panelKinode panel
1AAK1S/T
2ABL1Y
3ABL1 [E255K]Y
4ABL1 [E255V]Y
5ABL1 [H396P]Y
6ABL1 [Q252H]Y
7ABL1 [T315I]Y
8ABL1 [Y253F]Y
9ABL1 [Y253H]Y
10ABL2 (ARG)Y
11AKT1 (PKB)S/T
12AKT2 (PKBb)S/T
13AKT3 (PKBg)S/T
14ALKY
15ALK [C1156Y]Y
16ALK [F1174L]Y
17ALK [G1202R]Y
18ALK [G1269A]Y
19ALK [L1196M/G1202R]Y
20ALK [L1196M]Y
21ALK [R1275Q]Y
22ALK [T1151‐L1152 INS T]Y
23ALK:NPM1 (NPM1‐ALK)Y
24AURKA (AURA)S/T
25AURKB (AURB)S/T
26AURKB (AURB) [G160L]S/T
27AURKC (AURC)S/T
28AXLY
29BCKDKS/T
30BCR RET (fusion)Y
31BLKY
32BMP2K (BIKE)S/T
33BMXY
34BRAF (BRAF1, RAFB1)S/T
35BRAF, b-[V600E]S/T
36BRAF, b-[V600E]S/T
37BRSK1S/T
38BRSK2S/T
39BTKY
40BTK [C481S]Y
41BUB1S/T
42BUB1B (BUBR1)S/T
43CAMK1 (CAMK1α)S/T
44CAMK1D (CAMK1δ)S/T
45CAMK1G (CAMK1γ)S/T
46CAMK2A (CAMK2α)S/T
47CAMK2B (CAMK2β)S/T
48CAMK2D (CAMK2δ)S/T
49CAMK2G (CAMK2γ)S/T
50CAMK4S/T
51CAMKK1S/T
52CAMKK2S/T
53CDC42BPA (MRCKA)S/T
54CDC42BPB (MRCKB)S/T
55CDC42BPG (DMPK2)S/T
56CDC7/DBF4 (CDC7)S/T
57CDK1 (CDC2)/CycA1S/T
58CDK1 (CDC2)/CycA2S/T
59CDK1 (CDC2)/CycB1S/T
60CDK1 (CDC2)/CycE1S/T
61CDK2/CycA1S/T
62CDK2/CycA2S/T
63CDK2/CycE1S/T
64CDK2/CycE2S/T
65CDK2/CycOS/T
66CDK3/CycE1S/T
67CDK3/CycE2S/T
68CDK4/CycD1S/T
69CDK4/CycD2S/T
70CDK4/CycD3S/T
71CDK5/p25S/T
72CDK5/p35NCKS/T
73CDK6/CycD1S/T
74CDK6/CycD2S/T
75CDK6/CycD3S/T
76CDK7/CycH/MAT1S/T
77CDK7/CycH1S/T
78CDK9 (TAK)/CycKS/T
79CDK9 (TAK)/CycT1S/T
80CDK9 (TAK)/CycT2S/T
81CDK12 (CRK7)/CycKS/T
82CDK13 (CHED)/CycKS/T
83CDK14 (PFTAIRE1, PFTK1)/CycYS/T
84CDK15 (PFTAIRE2, PFTK2)/CycB1S/T
85CDK16 (PCTAIRE1, PCTK1)/CycYS/T
86CDK17 (PCTAIRE2, PCTK2)/CycYS/T
87CDK17 (PCTAIRE2, PCTK2)/p35NCKS/T
88CDK18 (PCTAIRE3, PCTK3)/CycYS/T
89CDK19 (CDK11)/CycCS/T
90CDKL5S/T
91CHEK1 (CHK1)S/T
92CHEK2 (CHK2)S/T
93CHUK (IKKA, IKKa)S/T
94CIT (CRIK)S/T
95CLK1S/T
96CLK2S/T
97CLK3S/T
98CLK4S/T
99CSF1R (FMS)Y
100CSKY
101CSNK1A1 (CK1A1, CK1α)S/T
102CSNK1A1L (CK1A1L, CK1a2)S/T
103CSNK1D (CK1D, CK1δ)S/T
104CSNK1E (CK1E, CK1ε)S/T
105CSNK1G1 (CK1G1, CK1γ1)S/T
106CSNK1G2 (CK1G2, CK1γ2)S/T
107CSNK1G3 (CK1G3, CK1γ3)S/T
108CSNK2A1 (CK2A1, CK2α1)S/T
109CSNK2A2 (CK2A2, CK2α2)S/T
110DAPK1S/T
111DAPK2 (DRP-1)S/T
112DAPK3 (ZIPK)S/T
113DCLK1 (DCAMKL1)S/T
114DCLK2 (DCAMKL2)S/T
115DDR1 [SRC treated]Y
116DDR2Y
117DMPK (DMPK1)S/T
118DSTYK (RIPK5, SGK496)S/T
119DYRK1AS/T
120DYRK1BS/T
121DYRK2S/T
122DYRK3S/T
123DYRK4S/T
124EEF2K (eEF2K)S/T
125EGFR (ERBB1)Y
126EGFR (ERBB1)Y
127EGFR [C797S/L858R]Y
128EGFR [d746‐750/C797S/T790M]Y
129EGFR [d746‐750/C797S]Y
130EGFR [d746‐750/T790M]Y
131EGFR [d746‐750]Y
132EGFR [L858R]Y
133EGFR [L861Q]Y
134EGFR [T790M/C797S/L858R]Y
135EGFR [T790M/L858R]Y
136EGFR [T790M]Y
137EIF2AK1 (HRI)S/T
138EIF2AK2 (PKR)S/T
139EIF2AK3 (PERK/PEK)S/T
140EIF2AK4 (GCN2)S/T
141EPHA1Y
142EPHA2Y
143EPHA3Y
144EPHA4Y
145EPHA5Y
146EPHA6Y
147EPHA7Y
148EPHA8Y
149EPHB1Y
150EPHB2Y
151EPHB3Y
152EPHB4Y
153ERBB2 (HER2)Y
154ERBB2 (HER2) [A775/G776insYVMA]Y
155ERBB4 (HER4)Y
156ERN1 (IRE1)S/T
157ERN1 [R727A/R728A]S/T
158ERN1 [R727A]S/T
159ERN1 [R728A]S/T
160ERN2 (IRE2)S/T
161FAM20CS/T
162FERY
163FESY
164FGFR1Y
165FGFR2Y
166FGFR3Y
167FGFR3 [G697C]Y
168FGFR3 [K650E]Y
169FGFR3 [K650M]Y
170FGFR3 [V555L]Y
171FGFR3 [V555M]Y
172FGFR4Y
173FGRY
174FLT1 (VEGFR1)Y
175FLT3Y
176FLT4 (VEGFR3)Y
177FRKY
178FYNa (FYN)Y
179FYNb (FYN)Y
180GAKS/T
181GRK1 (RHOK)S/T
182GRK2 (ADRBK1, BARK1)S/T
183GRK3 (ADRBK2, BARK2)S/T
184GRK4 (GPRK4)S/T
185GRK5 (GPRK5)S/T
186GRK6 (GPRK6)S/T
187GRK7 (GPRK7)S/T
188GSK3A (GSK3α)S/T
189GSK3B (GSK3β)S/T
190HASPINS/T
191HCKY
192HIPK1S/T
193HIPK2S/T
194HIPK3S/T
195HIPK4S/T
196HUNKS/T
197ICKS/T
198IGF1RY
199IKKB (IKKβ)S/T
200IKKE (IKKe)S/T
201INSR (IR)Y
202INSRR (IRR)Y
203IRAK1S/T
204IRAK4S/T
205ITKY
206JAK1 [JH1]Y
207JAK1 [JH1-JH2]Y
208JAK2 [JH1]Y
209JAK2 [JH1-JH2]Y
210JAK3 [JH1]Y
211KDR (VEGFR2)Y
212KIT (SCFR, CD117)Y
213LATS1S/T
214LATS2S/T
215LCKY
216LIMK1S/T
217LIMK2S/T
218LRRK2S/T
219LRRK2 [G2019S]S/T
220LRRK2 [R1441G]S/T
221LRRK2 [R1441H]S/T
222LTKY
223LYNA (LYNa)Y
224LYNB (LYNb)Y
225MAKS/T
226MAP2K1 (MEK1)S/T
227MAP2K2 (MEK2)S/T
228MAP2K3 (MEK3)S/T
229MAP3K1 (MEKK1)S/T
230MAP3K2 (MEKK2)S/T
231MAP3K3 (MEKK3)S/T
232MAP3K5 (ASK1)S/T
233MAP3K6 (ASK2)S/T
234MAP3K7 (TAK1)S/T
235MAP3K8 (COT, Tpl2)S/T
236MAP3K9 (MLK1)S/T
237MAP3K10 (MLK2)S/T
238MAP3K11 (MLK3)S/T
239MAP3K12 (DLK)S/T
240MAP3K13 (LZK)S/T
241MAP3K14 (NIK)S/T
242MAP3K19 (YSK4)S/T
243MAP3K20 (MLK7, ZAK)S/T
244MAP3K21 (MLK4)S/T
245MAP4K1 (HPK1)S/T
246MAP4K2 (GCK)S/T
247MAP4K3 (GLK, KHS2)S/T
248MAP4K4 (HGK, ZC1)S/T
249MAP4K5 (KHS1)S/T
250MAPK1 (ERK2)S/T
251MAPK3 (ERK1)S/T
252MAPK7 (BMK, ERK5)S/T
253MAPK8 (JNK1)S/T
254MAPK9 (JNK2)S/T
255MAPK10 (JNK3)S/T
256MAPK11 (p38β)S/T
257MAPK12 (p38γ)S/T
258MAPK13 (p38δ)S/T
259MAPK14 (p38α)S/T
260MAPK15 (ERK7)S/T
261MAPKAPK2 (MK2)S/T
262MAPKAPK3 (MK3)S/T
263MAPKAPK5 (MK5)S/T
264MARK1S/T
265MARK2S/T
266MARK3S/T
267MARK4S/T
268MAST3S/T
269MASTLS/T
270MATK (CTK)Y
271MELKS/T
272MERTK (MER)Y
273MET (c-MET, HGFR)Y
274MET [Y1230H]Y
275MINK1 (MAP4K6, MINK, ZC3)S/T
276MKNK1 (MNK1)S/T
277MKNK2 (MNK2)S/T
278MST1R (RON)Y
279mTOR (FRAP)S/T
280MUSKY
281MYLK (smMLCK)S/T
282MYLK2 (skMLCK)S/T
283MYLK3 (caMLCK)S/T
284MYLK4 (SgK085)S/T
285MYO3AS/T
286MYO3BS/T
287NEK1S/T
288NEK2S/T
289NEK3S/T
290NEK4S/T
291NEK5S/T
292NEK6S/T
293NEK7S/T
294NEK8S/T
295NEK9S/T
296NEK10S/T
297NEK11S/T
298NIM1 (NIM1K)S/T
299NLK (LAK1)S/T
300NTRK1 (TRKA)Y
301NTRK2 (TRKB)Y
302NTRK3 (TRKC)Y
303NUAK1 (ARK5)S/T
304NUAK2 (SNARK)S/T
305PAK1S/T
306PAK2S/T
307PAK3S/T
308PAK4S/T
309PAK5 (PAK7)S/T
310PAK6S/T
311PASKS/T
312PBK (TOPK)S/T
313PDGFRA (PDGFRα)Y
314PDGFRB (PDGFRβ)Y
315PDK1 (PDHK1)S/T
316PDK2 (PDHK2)S/T
317PDK3 (PDHK3)S/T
318PDK4 (PDHK4)S/T
319PDPK1 (PDK1)S/T
320PHKG1S/T
321PHKG2S/T
322PIM1S/T
323PIM2S/T
324PIM3S/T
325PINK1 (PINK)S/T
326PKN1S/T
327PKN2S/T
328PKN3S/T
329PLK1S/T
330PLK2S/T
331PLK3S/T
332PLK4S/T
333PNCK (CAMK1β)S/T
334PRKAA1‐B1‐G1 (AMPKα1β1γ1)S/T
335PRKAA1-B1-G2 (AMPKα1β1γ2)S/T
336PRKAA1-B1-G3 (AMPKα1β1γ3)S/T
337PRKAA1‐B2‐G1 (AMPKα1β2γ1)S/T
338PRKAA1-B2-G2 (AMPKα1β2γ2)S/T
339PRKAA1-B2-G3 (AMPKα1β2γ3)S/T
340PRKAA2‐B1‐G1 (AMPKα2β1γ1)S/T
341PRKAA2-B1-G2 (AMPKα2β1γ2)S/T
342PRKAA2-B1-G3 (AMPKα2β1γ3)S/T
343PRKAA2‐B2‐G1 (AMPKα2β2γ1)S/T
344PRKAA2-B2-G2 (AMPKα2β2γ2)S/T
345PRKAA2-B2-G3 (AMPKα2β2γ3)S/T
346PRKACA (PKACα)S/T
347PRKACB (PKACβ)S/T
348PRKACG (PKACG, PKACg)S/T
349PRKCA (PKCα)S/T
350PRKCB1 (PKCβ1)S/T
351PRKCB2 (PKCβ2)S/T
352PRKCD (PKCδ)S/T
353PRKCE (PKCe)S/T
354PRKCG (PKCγ)S/T
355PRKCH (PKCη)S/T
356PRKCI (PKCι)S/T
357PRKCQ (PKCᶿ)S/T
358PRKCZ (PKCζ)S/T
359PRKD1 (PKD1)S/T
360PRKD2 (PKD2)S/T
361PRKD3 (PKD3)S/T
362PRKDC (DNA‐PK)S/T
363PRKG1 (PKG1, PGK)S/T
364PRKG2 (PKG2, PGK2, CGK2)S/T
365PRKXS/T
366PTK2 (FAK)Y
367PTK2B (PYK2)Y
368PTK6 (BRK)Y
369RAF1 [Y340E/Y341E]S/T
370RAF1 [Y340E/Y341E]S/T
371RETY
372RET [G691S]Y
373RET [M918T]Y
374RET [S891A]Y
375RET [Y791F]Y
376RET:CCDC6 (CCDC6‐RET)Y
377RIPK1S/T
378RIPK2S/T
379RIPK3S/T
380RIPK4 (ANKRD3)S/T
381ROCK1S/T
382ROCK2S/T
383ROS1 (ROS)Y
384ROS1 [G2032R]Y
385RPS6KA1 (RSK1)S/T
386RPS6KA2 (RSK3)S/T
387RPS6KA3 (RSK2)S/T
388RPS6KA4 (MSK2)S/T
389RPS6KA5 (MSK1)S/T
390RPS6KA6 (RSK4)S/T
391RPS6KB1 (p70S6K)S/T
392RPS6KB2 (p70S6KB)S/T
393SBK1 (SBK)S/T
394SGK1 (SGK)S/T
395SGK2S/T
396SGK3S/T
397SIK1 (SIK)S/T
398SIK2 (QIK)S/T
399SIK3 (QSK)S/T
400SLKS/T
401SNRKS/T
402SRCY
403SRMS (SRM)Y
404SRPK1S/T
405SRPK2S/T
406SRPK3 (MSSK1)S/T
407STK3 (CLIK1, MST2)S/T
408STK4 (MST1)S/T
409STK10 (LOK)S/T
410STK11 (LKB1, AMPKK)S/T
411STK17A (DRAK1)S/T
412STK17B (DRAK2)S/T
413STK24 (MST3)S/T
414STK25 (YSK1)S/T
415STK26 (MST4)S/T
416STK33S/T
417STK38 (NDR1)S/T
418STK38L (NDR2)S/T
419SYKY
420TAOK1 (TAO1)S/T
421TAOK2 (TAO2)S/T
422TAOK3 (TAO3)S/T
423TBK1S/T
424TECY
425TEK (TIE2)Y
426TESK2S/T
427TLK1S/T
428TLK2S/T
429TNIK (ZC2)S/T
430TNK1Y
431TNK2 (ACK)Y
432TRPM7 (CHAK1)S/T
433TSSK1B (TSSK1)S/T
434TSSK2S/T
435TSSK3S/T
436TSSK6 (SSTK)S/T
437TTBK1S/T
438TTBK2S/T
439TTKS/T
440TXKY
441TYK2 [JH1]Y
442TYRO3Y
443ULK1S/T
444ULK2S/T
445ULK3S/T
446VRK1S/T
447VRK2S/T
448WEE1S/T
449YES1 (YES)Y
450ZAP70Y