Z BioInf
Skocz do: nawigacja, szukaj
(Utworzył nową stronę „Lp inhibitor (inne hamowane kinazy) klasa chemiczna test enzym. test komórkowy literatura IC50 (mM) linia komórkowa GI50 (mM) 1 AG490 (EGFR, PDGFR) tyrphostin...”)
 
 
(Nie pokazano 119 pośrednich wersji utworzonych przez tego samego użytkownika)
Linia 1: Linia 1:
Lp
+
==Small molecule inhibitors of the tyrosine kinase JAK2==
inhibitor
 
(inne hamowane kinazy)
 
klasa chemiczna
 
test enzym.
 
test komórkowy
 
literatura
 
  
 
+
{|class="wikitable center" style="text-align:center; font-size:100%; border:1px"
 
+
! rowspan=2|Nb
IC50 (mM)
+
! rowspan=2|inhibitor<br>(other kinase targets)
linia komórkowa
+
! rowspan=2|chemical class
GI50 (mM)
+
! enzymatic test
 
+
! colspan=2|cell test
1
+
! rowspan=2|&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;references&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;
AG490
+
|-
(EGFR,
+
!scope="row"|IC<sub>50</sub> (&micro;M)
PDGFR)
+
!scope="row"|&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;cell&nbsp;line&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;
tyrphostin
+
!scope="row"|GI<sub>50</sub> (&micro;M)
36.4
+
|-
48
+
|1
145.3
+
!scope="row" style="background-color:LemonChiffon" |AG490<br>(EGFR, PDGFR)
B-precursor (KOCL-33,-45,-50,-69,KOPN-30bi,-55bi,-57bi,-72bi,KOPN-32,-62,-84,NALM 6)
+
|tyrphostin
T-precursor (KOPT-K1,-5,-11,Jurkat)
+
|36.4<br>48<br>145.3
Ba/F3:JAK2V617F
+
|B-precursor (KOCL-33,-45,<br>-50,-69,KOPN-30bi,-55bi,<br>-57bi,-72bi,KOPN-32,-62,<br>-84,NALM 6)<br>T-precursor (KOPT-K1,-5,<br>-11,Jurkat)<br>Ba/F3:JAK2<sup>V617F</sup><br>HEL (JAK2<sup>V617F</sup>)<br>SET-2 (JAK2<sup>V617F/wt</sup>)<br>XG-1<br>XG-2<br>U266<br>MDAH2774<br>Caov-3<br>MDA-MB-468
HEL (JAK2V617F)
+
|<nowiki>-</nowiki><br><br><br><br>-<br><br>1.0<br>>20.0<br>>20.0<br>14.8<br>12.9<br>26.0<br>-<br>-<br>-
SET-2 (JAK2V617F/wt)
+
|[http://dx.doi.org/10.1021/jm00130a020 Gazit et al. 1989]<br>[http://dx.doi.org/10.1021/jm00110a022 Gazit et al. 1991]<br>[http://dx.doi.org/10.1038/379645a0 Meydan et al. 1996]<br>[http://dx.doi.org/10.1046/j.1365-2141.2000.02127.x Vos et al. 2000]<br>[http://www.nature.com/leu/journal/v15/n11/full/2402260a.html Miyamoto et al. 2001]<br>[http://www.nature.com/onc/journal/v20/n55/full/1204990a.html Burke et al. 2001]<br>[http://dx.doi.org/10.1023/A%3A1016186907376 Duhé et al. 2002]<br>[http://www.sciencedirect.com/science/article/pii/S0968089610000829 Reddy et al. 2010]<br>[http://gan.sagepub.com/content/1/4/331.abstract Jatiani et al. 2010]
XG-1
+
|-
XG-2
+
|2
U266
+
!scope="row" style="background-color:LemonChiffon" |LS104<br>(BCR-ABL)
MDAH2774
+
|tyrphostin
Caov-3
+
|2.52<br>0.1-0.6
MDA-MB-468
+
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>Ba/F3:EpoR,JAK2<sup>wt</sup><br>HEL
-
+
|1.5<br>10.0
 
+
|[http://bloodjournal.hematologylibrary.org/content/102/12/4153.abstract Grunberger et al. 2003]<br>[http://mct.aacrjournals.org/content/7/5/1176.abstract Lipka et al. 2008]
 
+
|-
 
+
|3
 
+
!scope="row" style="background-color:LemonChiffon" |WP1066
-
+
|tyrphostin
 
+
|<nowiki>-</nowiki>
1.0
+
|HEL
>20.0
+
|2.3
>20.0
+
|[http://clincancerres.aacrjournals.org/content/14/3/788.abstract Verstovsek et al. 2008]
14.8
+
|-
12.9
+
|4
26.0
+
!scope="row" style="background-color:LemonChiffon" |ON044580<br>(BCR-ABL)
-
+
|&alpha;-benzoyl styryl benzyl sulfide
-
+
|0.9-1.2<br>4.2
-
+
|Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>SET-2
Gazit et al. 1989,1991
+
|0.25<br>0.90<br>3.00
Meydan et al. 1996
+
|[http://www.sciencedirect.com/science/article/pii/S0968089610000829 Reddy et al. 2010]<br>[http://gan.sagepub.com/content/1/4/331.abstract Jatiani et al. 2010]<br>[http://gan.sagepub.com/content/1/4/346.abstract Samanta et al. 2010]
Vos et al. 2000
+
|-
Miyamoto et al. 2001
+
|5
Burke et al. 2001
+
!scope="row" style="background-color:LemonChiffon" |lestaurtinib<br>(CEP701)<br>(FLT3,JAK3)
Duhé et al. 2002
+
|indolocarbazole
Reddy et al. 2010
+
|0.001
Jatiani et al. 2010
+
|HEL
2
+
|0.03-0.10
LS104
+
|[http://bloodjournal.hematologylibrary.org/content/111/12/5663.abstract Hexner et al. 2008]<br>[http://bloodjournal.hematologylibrary.org/content/115/6/1131.abstract Santos et al. 2010]
(BCR-ABL)
+
|-
tyrphostin
+
|6
2.52
+
!scope="row" style="background-color:LemonChiffon" |G&ouml;6976<br>(JAK3, FLT3, PKC&alpha;,&beta;1)
0.1-0.6
+
|indolocarbazole
Ba/F3:EpoR,JAK2V617F
+
|0.13
Ba/F3:EpoR,JAK2wt
+
|32D<br>32D:TEL-JAK2<br>FDCP1<br>TF-1<br>Mo7E<br>HEL
HEL
+
|0.093<br>0.242<br>-<br>-<br>-<br>-
1.5
+
|[http://dx.doi.org/10.1111/j.1365-2141.2006.06291.x Grandage et al. 2006]
 
+
|-
10.0
+
|7
Grunberger et al. 2003
+
!scope="row" style="background-color:LemonChiffon" |TG02<br>(CDKs, TYK2, FLT3, TYRO3, ERK5, p38&delta;, Fms, Lck, Fyn, JAK1)
Lipka et al. 2008
+
|pyrimidine
3
+
|<nowiki>-</nowiki>
WP1066
+
|HEL<br>SET-2<br>Ba/F3:JAK2<sup>wt</sup><br>Ba/F3:JAK2<sup>V617F</sup><br>Karpas-1106P<br>32D
tyrphostin
+
|0.202<br>0.231<br>0.156<br>0.099<br>0.068<br>0.098
-
+
|[http://dx.doi.org/10.1038/leu.2011.218 Goh et al. 2012]<br>[http://dx.doi.org/10.1111/bjh.12018 Pallis et al. 2012]
HEL
+
|-
2.3
+
|8
Verstovsek et al. 2008
+
!scope="row" style="background-color:LemonChiffon" |TG101209<br>(FLT3, RET, JAK3)
 
+
|pyrimidine
4
+
|0.006
ON044580
+
|Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>multiple myeloma cell lines (RPMI8226, MM1S, OPM2, NCI-H929, Dox40, MM1R, LR5)
(BCR-ABL)
+
|0.2<br>2-5<br>-
a-benzoyl styryl benzyl sulfide
+
|[http://dx.doi.org/10.1038/sj.leu.2404750 Pardanani et al. 2007]<br>[http://bloodjournal.hematologylibrary.org/content/114/24/5024.abstract Wang and Fiskus et al. 2009]<br>[http://dx.doi.org/10.1002/ajh.21785 Ramakrishnan et al. 2010]
0.9-1.2
+
|-
4.2
+
|9
Ba/F3:JAK2V617F
+
!scope="row" style="background-color:LemonChiffon" |TG101348<br>(FLT3, RET, JAK1, JAK3, TYK2)
HEL
+
|pyrimidine
SET-2
+
|0.003
0.25
+
|Ba/F3:JAK2<sup>V617F</sup><br>HEL
0.90
+
|0.270<br>0.305
3.00
+
|[http://www.sciencedirect.com/science/article/pii/S1535610808000457 Wernig et al. 2008]<br>[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;114/22/755 Pardanani et al. 2009]<br>[http://jco.ascopubs.org/content/29/7/789.abstract Pardanani et al. 2011]
Reddy et al. 2010
+
|-
Jatiani et al. 2010
+
|10
Samanta et al. 2010
+
!scope="row" style="background-color:LemonChiffon" |R723<br>(JAK3, TYK2, FLT3, PRKD2, TBK1, SYK, PAK4, DAPK3, PRKD1, MYLK2, PRKCN, STK22D, IKBKE)
5
+
|pyrimidine
CEP701
+
|0.002
(FLT3,JAK3)
+
|Ba/F3:JAK2<sup>V617F</sup>
indolocarbazole
+
|0.13-0.20
0.001
+
|[https://ash.confex.com/ash/2009/webprogram/Paper18988.html Shide et al. 2009]<br>[http://bloodjournal.hematologylibrary.org/content/117/25/6866.abstract Shide et al. 2011]
HEL
+
|-
0.03-0.10
+
|11
Hexner et al. 2008
+
!scope="row" style="background-color:LemonChiffon" |INCB018424<br>(JAK1, JAK3, TYK2)
Santos et al. 2010
+
|pyrrolopyrimidine
6
+
|0.0045
Go6976
+
|<nowiki>-</nowiki>
(JAK3,
+
|<nowiki>-</nowiki>
FLT3,
+
|[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;110/11/3538  Fridman et al. 2007]<br>[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;110/11/558 Verstovsek et al. 2007]<br>[https://ash.confex.com/ash/2008/webprogram/Paper8625.html Verstovsek et al. 2008]<br>[http://www.nejm.org/doi/full/10.1056/NEJMoa1002028 Verstovsek et al. 2010]<br>[http://bloodjournal.hematologylibrary.org/content/115/15/3109.abstract Quintás-Cardama et al. 2010]<br>[http://dx.doi.org/10.1002/cncr.26129 Mesa et al. 2011]
PKCa,b1)
+
|-
indolocarbazole
+
|12
0.13
+
!scope="row" style="background-color:LemonChiffon" |INCB16562<br>(JAK1, JAK3)
32D
+
|pyrrolopyrimidine
32D:TEL-JAK2
+
|0.0003
FDCP1
+
|Ba/F3:JAK2<sup>V617F</sup><br>Ba/F3:JAK2<sup>K539L</sup><br>Ba/F3:MPL<sup>W515L</sup><br>Ba/F3:TEL-JAK2<br>SET-2<br>UKE-1
TF-1
+
|0.177<br>0.406<br>0.600<br>0.168<br>0.046<br>0.573
Mo7E
+
|[http://bloodjournal.hematologylibrary.org/content/115/14/2919.abstract Koppikar et al. 2010]
HEL
+
|-
0.093
+
|13
0.242
+
!scope="row" style="background-color:LemonChiffon" |CP690550<br>(JAK1, JAK3, TYK2)
-
+
|pyrrolopyrimidine
-
+
|0.0041<br>0.011<br>0.012<br>0.020
-
+
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup>
-
+
|2.1<br>0.25
Grandage et al. 2006
+
|[http://search.ebscohost.com/login.aspx?direct=true&db=a9h&AN=11414503&lang=pl&site=eds-live&scope=site Changelian et al. 2003]<br>[http://www.sciencedirect.com/science/article/pii/S0960894X06009152 Chen et al. 2006]<br>[http://www.sciencedirect.com/science/article/pii/S0960894X06014053 Clark et al. 2007]<br>[http://dx.doi.org/10.1111/j.1349-7006.2008.00817.x Manshouri et al. 2008]<br>[http://www.journal-inflammation.com/content/7/1/41 Meyer et al. 2010]<br>[http://dx.doi.org/10.1021/jm101157q Thoma et al. 2011]
7
+
|-
TG02
+
|14
(CDKs,
+
!scope="row" style="background-color:LemonChiffon" |AZD1480<br>(JAK1, JAK3, TRKA, AuroraA, FLT4, FGFR1, ARK5)
FLT3)
+
|pyrazolopyrimidine
pyrimidine
+
|0.0004<br>|0.003
-
+
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1<br>HEL
HEL
+
|0.06<br>0.016<br>0.054<br>0.39
SET-2
+
|[http://www.cell.com/cancer-cell/abstract/S1535-6108(09)00384-5 Hedvat et al. 2009]<br>[http://dx.doi.org/10.1021/jm1011319 Ioannidis et al. 2011]
Ba/F3:JAK2wt
+
|-
Ba/F3:JAK2V617F
+
|15
Karpas-1106P
+
!scope="row" style="background-color:LemonChiffon" |CYT387<br>(JAK1, TYK2, CDK2/cyclinA, JNK1, PRKCN, PRKD1, ROCK2, TBK1)
32D
+
|aminopyrimidine
0.202
+
|0.018
0.231
+
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>32D:EpoR,JAK2<sup>V617F</sup><br>HEL<br>TF-1<br>U266<br>CHRF-288-11:JAK2<sup>T875N</sup><br>Ba/F3:TEL-JAK2
0.156
+
|0.5<br>1.5<br>1.5<br>1.25<br>0.75<br>0.001<br>0.724
0.099
+
|[http://dx.doi.org/10.1038/leu.2009.50 Pardanani et al. 2009]<br>[http://bloodjournal.hematologylibrary.org/content/115/25/5232.abstract Tyner et al. 2010]
0.068
+
|-
0.098
+
|16
Goh et al. 2011
+
!scope="row" style="background-color:LemonChiffon" |SGI1252<br>(JAK1, JAK3, TYK2, YES, FLT3, ABL, SRC, LCK)
8
+
|diaminopyrimidine
TG101209
+
|0.0054<br>0.002<br>0.0197
(FLT3,
+
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>UKE-1
RET,
+
|0.074<br>0.110<br>0.441<br>0.055<br>0.089
JAK3)
+
|[http://linkinghub.elsevier.com/retrieve/pii/S1359634908725059?showall=true Olsen et al. 2008]<br>[https://ash.confex.com/ash/2008/webprogram/Paper10062.html Riaz Ahmed et al. 2008]<br>[http://linkinghub.elsevier.com/retrieve/pii/S0301472X10004947?showall=true Riaz Ahmed et al. 2011]
pyrimidine
+
|-
0.006
+
|17
Ba/F3:JAK2V617F
+
!scope="row" style="background-color:LemonChiffon" |SB1518<br>(FLT3, JAK1, JAK3, TYK2)
HEL
+
|aminopyrimidine macrocycle
multiple myeloma cell lines (RPMI8226, MM1S, OPM2, NCI-H929, Dox40, MM1R, LR5)
+
|0.023<br>0.019
0.2
+
|Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>Karpas-1106P<br>U266
2-5
+
|0.16<br>1.726<br>0.217<br>0.348<br>1.350
-
+
|[http://dx.doi.org/10.1038/leu.2011.148 Hart et al. 2011]<br>[http://pubs.acs.org/doi/abs/10.1021/jm200326p William et al. 2011]
 
+
|-
 
+
|18
 
+
!scope="row" style="background-color:LemonChiffon" |"38"<br>(JAK1, TYK2, JAK3, MEKK2, MEKK3)
 
+
|8-oxo-pyridopyrimidine
Pardanani et al. 2007
+
|0.001
Wang and Fiskus et al. 2009
+
|TF-1-EPO (IC<sub>50</sub>)
Ramkrishnan et al. 2010
+
|0.115
9
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X13010226 Labadie et al. 2013]
TG101348
+
|-
(FLT3,RET,JAK1,
+
|19
JAK3,TYK2)
+
!scope="row" style="background-color:LemonChiffon" |Z3
pyrimidine
+
|pyridine
0.003
+
|15.0<br>28.0
Ba/F3:JAK2V617F
+
|HEL
HEL
+
|<nowiki>-</nowiki>
0.270
+
|[http://mct.aacrjournals.org/content/7/8/2308.abstract Sayyah et al. 2008]
0.305
+
|-
Wernig et al. 2008
+
|20
Animesh et al. 2009
+
!scope="row" style="background-color:LemonChiffon" |"25"<br>(JAK1, GAK, YSK4)
Pardanani et al. 2011
+
|thienopyridine
10
+
|0.002
R723
+
|Ba/F3:TEL-JAK2 (IC<sub>50</sub>)
(JAK3,TYK2,FLT3,
+
|1.62
PRKD2,TBK1,SYK,
+
|[http://dx.doi.org/10.1021/jm200911r Schenkel et al. 2011]
PAK4,DAPK3,PRKD1,MYLK2,PRKCN,
+
|-
STK22D,IKBKE)
+
|21
pyrimidine
+
!scope="row" style="background-color:LemonChiffon" |"65"<br>(JAK1, cSRC, TRKA, ACK1, FMS, FYN, FLT3, HCK, RET, BMX, LYN, FGR, LCK, ARK5, BTK, YES, PTK5, TRKB, CaMKII&delta;,&gamma;, PRK2, ARG, MLK1, ALK)
0.002
+
|pyridoindolcarboxamide
Ba/F3:JAK2V617F
+
|0.0008
0.13-0.20
+
|irf1-bla HEL (IC<sub>50</sub>)
Shide et al. 2009
+
|0.025
Shide et al. 2011
+
|[http://dx.doi.org/10.1021/jm200909u Lim et al. 2011]
11
+
|-
INCB018424
+
|22
(JAK1,JAK3,TYK2)
+
!scope="row" style="background-color:LemonChiffon" |AT9283<br>(AuroraK, JAK3, FLT3, ABL)
pyrrolopyrimidine
+
|pyrazole benzimidazole
0.0045
+
|0.0012
-
+
|HEL (JAK2<sup>V617F</sup>)<br>SET-2 (JAK2<sup>V617F/wt</sup>)<br>Ba/F3:ETV6-JAK2<br>Ba/F3-IL-3<br>TF-1-IL-3<br>CMK (JAK2<sup>A572V</sup>)
-
+
|0.110<br>0.057<br>0.016<br>0.017<br>0.040<br>0.026
Verstovsek et al. 2008, 2010
+
|[http://dx.doi.org/10.1021/jm800984v Howard et al. 2009]<br>[http://dx.doi.org/10.1111/j.1365-2141.2010.08175.x Dawson et al. 2010]
Mesa 2010
+
|-
12
+
|23
INCB16562
+
!scope="row" style="background-color:LemonChiffon" |AZ960<br>(TRKA, AuroraA, ARK5, ALK, CaMKII, FLT4, FGFR1, LIMK1, BrSK2, FAK)
(JAK1,JAK3)
+
|pyrazole nicotinonitrile
pyrrolopyrimidine
+
|0.003
0.0003
+
|SET-2 (JAK2<sup>V617F/wt</sup>)<br>Ba/F3:TEL-JAK2<br>HTLV-1 infected T cells (MT-1, MT-2)
Ba/F3:JAK2V617F
+
|0.033<br>0.025<br>-
Ba/F3:JAK2K539L
+
|[http://www.jbc.org/content/283/47/32334.abstract Gozgit et al. 2008]<br>[http://mct.aacrjournals.org/content/9/12/3386.abstract Yang et al. 2010]
Ba/F3:MPLW515L
+
|-
Ba/F3:TEL-JAK2
+
|24
SET-2
+
!scope="row" style="background-color:LemonChiffon" |CMP6<br>(JAK1, JAK3, TYK2)
UKE-1
+
|pyridone tetracycle
0.177
+
|0.001
0.406
+
|CTLL-2<br>B9<br>U266<br>KMS11
0.600
+
|0.052-0.1<br>0.25<br>-<br>-
0.168
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X02001063 Thompson et al. 2002]<br>[http://bloodjournal.hematologylibrary.org/content/107/1/176.abstract Lucet et al. 2006]<br>[http://cancerres.aacrjournals.org/content/66/19/9714.abstract Pedranzini et al. 2006]
0.046
+
|-
0.573
+
|25
Koppikar et al. 2010
+
!scope="row" style="background-color:LemonChiffon" |"13"
13
+
|sulfonamide aminoindazole
CP690550
+
|0.078
(JAK1,
+
|<nowiki>-</nowiki>
JAK3,
+
|<nowiki>-</nowiki>
TYK2)
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X08010007 Antonysamy et al. 2009]
pyrrolopyrimidine
+
|-
0.0041
+
|26
0.011
+
!scope="row" style="background-color:LemonChiffon" |comp 9<br>(JAK3, ALK, cKIT, GCK)
0.012
+
|polycyclic azaindole
0.020
+
|0.001
FDCP-EpoR,JAK2wt
+
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
FDCP-EpoR,JAK2V617F
+
|0.27<br>1.53
2.1
+
|[http://dx.doi.org/10.1021/jm901383u Wang et al. 2009]
0.25
+
|-
Changelian et al. 2003
+
|27
Chen et al. 2006
+
!scope="row" style="background-color:LemonChiffon" |"15a"
Clark et al. 2007
+
|polycyclic azaindole
Manshouri et al. 2008
+
|0.0008
Meyer et al. 2010
+
|TF-1-GMCSF (IC<sub>50</sub>)
Thoma et al. 2011
+
|0.16
14
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X09015911 Wang et al. 2010]
AZD1480
+
|-
(JAK1,JAK3,TRKA,
+
|28
AuroraA,FLT4,FGFR1,ARK5)
+
!scope="row" style="background-color:LemonChiffon" |"40"<br>(JAK3)
pyrazolopyrimidine
+
|aminopyrazolopyrimidine
0.0004
+
|0.0002
0.003
+
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
Ba/F3:TEL-JAK2
+
|0.16<br>3.2
SET-2
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X09014541 Ledeboer et al. 2009]
UKE1
+
|-
HEL
+
|29
0.06
+
!scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3)
0.016
+
|pyrrolotriazine aminopyrrazole
0.054
+
|0.0018
0.39
+
|SET-2
Hedvat et al. 2009
+
|0.11
Ioannidis et al. 2011
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X11000357 Harikrishnan et al. 2011]
15
+
|-
CYT387
+
|30
(JAK1,TYK2,
+
!scope="row" style="background-color:LemonChiffon" |atiprimod<br>(JAK3)
CDK2/cyclinA,
+
|azaspirane
JNK1,PRKCN,
+
|<nowiki>-</nowiki>
PRKD1,ROCK2,TBK1)
+
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>SET-2
aminopyrimidine
+
|0.69<br>0.42<br>0.53
0.018
+
|[http://bloodjournal.hematologylibrary.org/content/105/11/4470.abstract Hamasaki et al. 2005]<br>[http://dx.doi.org/10.1007/s10637-010-9429-z Quintás-Cardama et al. 2011]
Ba/F3:EpoR,JAK2V617F
+
|-
32D:EpoR,JAK2V617F
+
|31
HEL
+
!scope="row" style="background-color:LemonChiffon" |G6
TF-1
+
|stilbenoid<br>(diaryleten)
U266
+
|0.060
CHRF-288-11:JAK2T875N
+
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>HEL
Ba/F3:TEL-JAK2
+
|<nowiki>-</nowiki><br>4.0
0.5
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X09006477 Kiss et al. 2009]<br>[http://www.jbc.org/content/285/41/31399.abstract Majumder et al. 2010]<br>[http://www.jbc.org/content/286/6/4280.abstract Kirabo et al. 2011]
1.5
+
|-
1.5
+
|32
1.25
+
!scope="row" style="background-color:LemonChiffon" |NVP-BSK805<br>(JAK1, TYK2, ABL)
0.75
+
|diarylquinoxaline
0.001
+
|0.00048<br>0.00058<br>0.00056
 
+
|Ba/F3:JAK2<sup>V617F</sup><br>SET-2<br>MB-02<br>UKE-1<br>MUTZ-8
0.724
+
|0.039<br>0.051<br>0.064<br>0.071<br>0.331
Pardanani et al. 2009
+
|[http://mct.aacrjournals.org/content/9/7/1945.abstract Baffert et al. 2010]
Tyner et al. 2010
+
|-
16
+
|33
SGI1252
+
!scope="row" style="background-color:LemonChiffon" |"26"<br>(ABL)
(JAK1,JAK3,TYK2,
+
|diarylquinoxaline
YES,FLT3,ABL,SRC,
+
|0.0073
LCK)
+
|SET-2
diaminopyrimidine
+
|0.088
0.002
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X10002568 Pissot-Soldermann et al. 2010]
0.0197
+
|-
FDCP-EpoR,JAK2wt
+
|34
FDCP-EpoR,JAK2V617F
+
!scope="row" style="background-color:LemonChiffon" |hexabromo cyclohexane
HEL
+
|cyclohexane
SET-2
+
|low &micro;M
UKE-1
+
|&gamma;-2A
0.074
+
|<nowiki>-</nowiki>
0.110
+
|[http://dx.doi.org/10.1021/jm049470k Sandberg et al. 2005]
0.441
+
|-
0.055
+
|35
0.089
+
!scope="row" style="background-color:LemonChiffon" |XL019<br>(JAK1, JAK3, FLT3, PDGFRB, cKIT)
Olsen et al. 2008
+
|arylaminopyrimidine
Riaz Ahmed et al. 2011
+
|0.002
17
+
|HEL
SB1518
+
|<nowiki>-</nowiki>
(FLT3,JAK1,
+
|[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;112/11/2810 Paquette et al. 2008]<br>[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;112/11/98 Shah et al. 2008]<br>[http://www.sciencedirect.com/science/article/pii/S0960894X12012747 Forsyth et al. 2012]
JAK3,TYK2)
+
|-
aminopyrimidine macrocycle
+
|36
0.023
+
!scope="row" style="background-color:LemonChiffon" |CEP33779<br>(JAK1, JAK3)
0.019
+
|triazolopyridine
Ba/F3:JAK2V617F
+
|0.0018
HEL
+
|irf1-bla TF-1 (IC<sub>50</sub>)
SET-2
+
|0.061
Karpas-1106P
+
|[http://dx.doi.org/10.1021/jm300248q Dugan et al. 2012]
U266
+
|-
0.16
+
|37
1.726
+
!scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3, TYK2)
0.217
+
|triazolopyridine
0.348
+
|0.0017
1.350
+
|SET-2 (IC<sub>50</sub>)
Hart et al. 2011
+
|0.212
William et al. 2011
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X13007178 Siu et al. 2013]
18
+
|-
Z3
+
|38
pyridine
+
!scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK1, JAK3, TYK2)
15.0
+
|imidazopyrrolopyridine
28.0
+
|0.0021
HEL
+
|TF-1-EPO (IC<sub>50</sub>)
-
+
|0.097
Sayyah et al. 2008
+
|[http://dx.doi.org/10.1021/jm300628c Zak et al. 2012]
19
+
|-
25
+
|39
(JAK1,GAK,YSK4)
+
!scope="row" style="background-color:LemonChiffon" |"7"<br>(JAK1, JAK3, TYK2)
thienopyridine
+
|imidazopyrrolopyridine
0.002
+
|0.0012
Ba/F3:TEL-JAK2 (IC50)
+
|TF-1-EPO (IC<sub>50</sub>)
1.62
+
|0.86
Schenkel et al. 2011
+
|[http://dx.doi.org/10.1021/jm300438j Kulagowski et al. 2012]
20
+
|-
65
+
|40
(JAK1,cSRC,TRKA,
+
!scope="row" style="background-color:LemonChiffon" |"31"<br>(JAK1, JAK3, TYK2)
ACK1,FMS,FYN,FLT3,HCK,RET,BMX,LYN,
+
|imidazopyrrolopyridine
FGR,LCK,ARK5,BTK,YES,PTK5,TRKB,
+
|0.068
CaMKIId,g,PRK2,ARG,MLK1,ALK)
+
|TF-1-EPO (IC<sub>50</sub>)
pyridoindolcarboxamide
+
|7.68
0.0008
+
|[http://dx.doi.org/10.1021/jm4004895 Zak et al. 2013]
irf1-bla HEL (IC50)
+
|-
0.025
+
|41
Lim et al. 2011
+
!scope="row" style="background-color:LemonChiffon" |"46"<br>(JAK1, TYK2)
21
+
|pyridine amide
AT9283
+
|0.028
(AuroraK,JAK3, FLT3,ABL)
+
|TF-1-EPO (IC<sub>50</sub>)
pyrazole benzimidazole
+
|1.7
0.0012
+
|[http://www.sciencedirect.com/science/article/pii/S0223523413002304 Liang et al. 2013]
HEL (JAK2V617F)
+
|-
SET-2 (JAK2V617F/wt)
+
|42
Ba/F3:ETV6-JAK2
+
!scope="row" style="background-color:LemonChiffon" |"7j"<br>(JAK1, JAK3, TYK2)
Ba/F3-IL-3
+
|pyrazolopyrimidine
TF-1-IL-3
+
|0.0001
CMK (JAK2A572V)
+
|SET-2 (IC<sub>50</sub>)<br>TF-1-EPO (IC<sub>50</sub>)
0.110
+
|0.0039<br>0.0074
0.057
+
|[http://dx.doi.org/10.1021/jm3012239 Hanan et al. 2012]
0.016
+
|-
0.017
+
|43
0.040
+
!scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK3)
0.026
+
|pyrazolopyrimidine amine
Howard et al. 2009
+
|0.003
Dawson et al. 2010
+
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
22
+
|0.006<br>0.078<br>0.050
AZ960
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X13002989 Guan et al. 2013]
(TRKA,AuroraA,
+
|-
ARK5,ALK,CaMKII,
+
|44
FLT4,FGFR1,LIMK1,
+
!scope="row" style="background-color:LemonChiffon" |"19a"<br>(JAK1, JAK3, CK2&alpha;2, KDR, ABL, FGR, TRKA, FLT4, FLT3, RET, ALK, FGFR1, AuroraA, LIMK1)
BrSK2,FAK)
+
|methylimidazole
pyrazole nicotinonitrile
+
|0.002
0.003
+
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
SET-2 (JAK2V617F/wt)
+
|0.012<br>0.014<br>0.055
Ba/F3:TEL-JAK2
+
|[http://dx.doi.org/10.1021/jm401546n Su et al. 2014]
HTLV-1 infected T cells (MT-1, MT-2)
+
|-
0.033
+
|45
0.025
+
!scope="row" style="background-color:LemonChiffon" |NS-018<br>(JAK1, JAK3, TYK2, SRC, FYN, YES, LYNa, FGR, LCK, HCK, ABL, FLT3)
-
+
|pyrazinopyridine diamine
 
+
|0.00072
Gozgit et al. 2008
+
|Ba/F3:JAK2<sup>V617F</sup><br>Ba/F3:TEL-JAK2<br>Ba/F3:MPL<sup>W515L</sup><br>SET-2<br>Ba/F3:TEL-JAK3<br>MV4-11(FLT3-ITD)
Yang et al. 2010
+
|0.060 0.011 0.061 0.120 0.800 0.730
23
+
|[http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3255248/ Nakaya et al. 2011]<br>[http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3913942/ Nakaya et al. 2014]
CMP6
+
|}
(JAK1,
 
JAK3,
 
TYK2)
 
pyridone tetracycle
 
0.001
 
CTLL-2
 
B9
 
U266
 
KMS11
 
0.052-0.1
 
0.25
 
-
 
-
 
Thompson et al. 2002
 
Lucet et al. 2006
 
Pedranzini et al. 2008
 
24
 
13
 
sulfonamide aminoindazole
 
0.078
 
-
 
-
 
Antonysamy et al. 2009
 
25
 
comp 9
 
(JAK3,ALK,
 
cKIT,GCK)
 
polycyclic azaindole
 
0.001
 
TF-1-GMCSF (IC50)
 
HT2-IL2 (IC50)
 
0.27
 
1.53
 
Wang et al. 2009
 
26
 
15a
 
polycyclic azaindole
 
0.0008
 
TF-1-GMCSF (IC50)
 
0.16
 
Wang et al. 2010
 
27
 
40
 
(JAK3)
 
aminopyrazolopyrimidine
 
0.0002
 
TF-1-GMCSF (IC50)
 
HT2-IL2 (IC50)
 
0.16
 
3.2
 
Ledeboer et al. 2009
 
28
 
29
 
(JAK1,JAK3)
 
pyrrolotriazine aminopyrrazole
 
0.0018
 
SET-2
 
0.11
 
Harikrishnan et al. 2011
 
29
 
atiprimod
 
(JAK3)
 
azaspirane
 
-
 
FDCP-EpoR,JAK2wt
 
FDCP-EpoR,JAK2V617F
 
SET-2
 
0.69
 
0.42
 
0.53
 
Hamasaki et al. 2005
 
Quintás-Cardama et al. 2011
 
30
 
G6
 
stilbenoid
 
(diaryleten)
 
0.060
 
Ba/F3:EpoR,JAK2V617F
 
HEL
 
-
 
 
 
4.0
 
Kiss et al. 2009
 
Majumder et al. 2010
 
Kirabo et al. 2011
 
31
 
NVP-BSK805
 
(JAK1,TYK2,ABL)
 
diarylquinoxaline
 
0.00048
 
0.00058
 
0.00056
 
Ba/F3:JAK2V617F
 
SET-2
 
MB-02
 
UKE-1
 
MUTZ-8
 
0.039
 
0.051
 
0.064
 
0.071
 
0.331
 
Baffert et al. 2010
 
32
 
26
 
(ABL)
 
diarylquinoxaline
 
0.0073
 
SET-2
 
0.088
 
Pissot-Soldermann et al. 2010
 
33
 
hexabromo cyclohexane
 
hexabromo cyclohexane
 
low mM
 
g-2A
 
-
 
Sandberg et al. 2005
 
34
 
XL019
 
(JAK1,JAK3,FLT3,
 
PDGFRB,cKIT)
 
arylaminopyrimidine
 
0.002
 
HEL
 
-
 
Paquette et al. 2008
 
Shah et al. 2008
 
Forsyth et al. 2012
 
35
 
CEP33779
 
(JAK1,JAK3)
 
triazolopyridine
 
0.0018
 
irf1-bla TF-1 (IC50)
 
0.061
 
Dugan et al. 2012
 
36
 
29
 
(JAK1,JAK3,TYK2)
 
triazolopyridine
 
0.0017
 
SET-2 (IC50)
 
0.212
 
Siu et al. 2013
 
37
 
6
 
(JAK1,JAK3,TYK2)
 
imidazopyrrolopyridine
 
0.0021
 
TF-1-EPO (IC50)
 
0.097
 
Zak et al. 2012
 
38
 
7
 
(JAK1,JAK3,TYK2)
 
imidazopyrrolopyridine
 
0.0012
 
TF-1-EPO (IC50)
 
0.86
 
Kulagowski et al. 2012
 
39
 
31
 
(JAK1,JAK3,TYK2)
 
imidazopyrrolopyridine
 
0.068
 
TF-1-EPO (IC50)
 
7.68
 
Zak et al. 2013
 
40
 
46
 
(JAK1,TYK2)
 
pyridine amide
 
0.028
 
TF-1-EPO (IC50)
 
1.7
 
Liang et al. 2013
 
41
 
7j
 
(JAK1,JAK3,TYK2)
 
pyrazolopyrimidine
 
0.0001
 
SET-2 (IC50)
 
TF-1-EPO (IC50)
 
0.0039
 
0.0074
 
Hanan et al. 2012
 
42
 
6
 
(JAK3)
 
pyrazolopyrimidine amine
 
0.003
 
Ba/F3:TEL-JAK2
 
SET-2
 
UKE1
 
0.006
 
0.078
 
0.050
 
Guan et al. 2013
 
43
 
19a
 
(JAK1,JAK3,CK2a2,
 
KDR,ABL,FGR,TRKA,FLT4,FLT3,RET,ALK,
 
FGFR1,AuroraA,
 
LIMK1)
 
methylimidazole
 
0.002
 
Ba/F3:TEL-JAK2
 
SET-2
 
UKE1
 
0.012
 
0.014
 
0.055
 
Su et al. 2014
 

Aktualna wersja na dzień 16:07, 28 lis 2015

Small molecule inhibitors of the tyrosine kinase JAK2

Nb inhibitor
(other kinase targets)
chemical class enzymatic test cell test            references           
IC50 (µM)         cell line         GI50 (µM)
1 AG490
(EGFR, PDGFR)
tyrphostin 36.4
48
145.3
B-precursor (KOCL-33,-45,
-50,-69,KOPN-30bi,-55bi,
-57bi,-72bi,KOPN-32,-62,
-84,NALM 6)
T-precursor (KOPT-K1,-5,
-11,Jurkat)
Ba/F3:JAK2V617F
HEL (JAK2V617F)
SET-2 (JAK2V617F/wt)
XG-1
XG-2
U266
MDAH2774
Caov-3
MDA-MB-468
-



-

1.0
>20.0
>20.0
14.8
12.9
26.0
-
-
-
Gazit et al. 1989
Gazit et al. 1991
Meydan et al. 1996
Vos et al. 2000
Miyamoto et al. 2001
Burke et al. 2001
Duhé et al. 2002
Reddy et al. 2010
Jatiani et al. 2010
2 LS104
(BCR-ABL)
tyrphostin 2.52
0.1-0.6
Ba/F3:EpoR,JAK2V617F
Ba/F3:EpoR,JAK2wt
HEL
1.5
10.0
Grunberger et al. 2003
Lipka et al. 2008
3 WP1066 tyrphostin - HEL 2.3 Verstovsek et al. 2008
4 ON044580
(BCR-ABL)
α-benzoyl styryl benzyl sulfide 0.9-1.2
4.2
Ba/F3:JAK2V617F
HEL
SET-2
0.25
0.90
3.00
Reddy et al. 2010
Jatiani et al. 2010
Samanta et al. 2010
5 lestaurtinib
(CEP701)
(FLT3,JAK3)
indolocarbazole 0.001 HEL 0.03-0.10 Hexner et al. 2008
Santos et al. 2010
6 Gö6976
(JAK3, FLT3, PKCα,β1)
indolocarbazole 0.13 32D
32D:TEL-JAK2
FDCP1
TF-1
Mo7E
HEL
0.093
0.242
-
-
-
-
Grandage et al. 2006
7 TG02
(CDKs, TYK2, FLT3, TYRO3, ERK5, p38δ, Fms, Lck, Fyn, JAK1)
pyrimidine - HEL
SET-2
Ba/F3:JAK2wt
Ba/F3:JAK2V617F
Karpas-1106P
32D
0.202
0.231
0.156
0.099
0.068
0.098
Goh et al. 2012
Pallis et al. 2012
8 TG101209
(FLT3, RET, JAK3)
pyrimidine 0.006 Ba/F3:JAK2V617F
HEL
multiple myeloma cell lines (RPMI8226, MM1S, OPM2, NCI-H929, Dox40, MM1R, LR5)
0.2
2-5
-
Pardanani et al. 2007
Wang and Fiskus et al. 2009
Ramakrishnan et al. 2010
9 TG101348
(FLT3, RET, JAK1, JAK3, TYK2)
pyrimidine 0.003 Ba/F3:JAK2V617F
HEL
0.270
0.305
Wernig et al. 2008
Pardanani et al. 2009
Pardanani et al. 2011
10 R723
(JAK3, TYK2, FLT3, PRKD2, TBK1, SYK, PAK4, DAPK3, PRKD1, MYLK2, PRKCN, STK22D, IKBKE)
pyrimidine 0.002 Ba/F3:JAK2V617F 0.13-0.20 Shide et al. 2009
Shide et al. 2011
11 INCB018424
(JAK1, JAK3, TYK2)
pyrrolopyrimidine 0.0045 - - Fridman et al. 2007
Verstovsek et al. 2007
Verstovsek et al. 2008
Verstovsek et al. 2010
Quintás-Cardama et al. 2010
Mesa et al. 2011
12 INCB16562
(JAK1, JAK3)
pyrrolopyrimidine 0.0003 Ba/F3:JAK2V617F
Ba/F3:JAK2K539L
Ba/F3:MPLW515L
Ba/F3:TEL-JAK2
SET-2
UKE-1
0.177
0.406
0.600
0.168
0.046
0.573
Koppikar et al. 2010
13 CP690550
(JAK1, JAK3, TYK2)
pyrrolopyrimidine 0.0041
0.011
0.012
0.020
FDCP-EpoR,JAK2wt
FDCP-EpoR,JAK2V617F
2.1
0.25
Changelian et al. 2003
Chen et al. 2006
Clark et al. 2007
Manshouri et al. 2008
Meyer et al. 2010
Thoma et al. 2011
14 AZD1480
(JAK1, JAK3, TRKA, AuroraA, FLT4, FGFR1, ARK5)
pyrazolopyrimidine 0.003 Ba/F3:TEL-JAK2
SET-2
UKE1
HEL
0.06
0.016
0.054
0.39
Hedvat et al. 2009
Ioannidis et al. 2011
15 CYT387
(JAK1, TYK2, CDK2/cyclinA, JNK1, PRKCN, PRKD1, ROCK2, TBK1)
aminopyrimidine 0.018 Ba/F3:EpoR,JAK2V617F
32D:EpoR,JAK2V617F
HEL
TF-1
U266
CHRF-288-11:JAK2T875N
Ba/F3:TEL-JAK2
0.5
1.5
1.5
1.25
0.75
0.001
0.724
Pardanani et al. 2009
Tyner et al. 2010
16 SGI1252
(JAK1, JAK3, TYK2, YES, FLT3, ABL, SRC, LCK)
diaminopyrimidine 0.0054
0.002
0.0197
FDCP-EpoR,JAK2wt
FDCP-EpoR,JAK2V617F
HEL
SET-2
UKE-1
0.074
0.110
0.441
0.055
0.089
Olsen et al. 2008
Riaz Ahmed et al. 2008
Riaz Ahmed et al. 2011
17 SB1518
(FLT3, JAK1, JAK3, TYK2)
aminopyrimidine macrocycle 0.023
0.019
Ba/F3:JAK2V617F
HEL
SET-2
Karpas-1106P
U266
0.16
1.726
0.217
0.348
1.350
Hart et al. 2011
William et al. 2011
18 "38"
(JAK1, TYK2, JAK3, MEKK2, MEKK3)
8-oxo-pyridopyrimidine 0.001 TF-1-EPO (IC50) 0.115 Labadie et al. 2013
19 Z3 pyridine 15.0
28.0
HEL - Sayyah et al. 2008
20 "25"
(JAK1, GAK, YSK4)
thienopyridine 0.002 Ba/F3:TEL-JAK2 (IC50) 1.62 Schenkel et al. 2011
21 "65"
(JAK1, cSRC, TRKA, ACK1, FMS, FYN, FLT3, HCK, RET, BMX, LYN, FGR, LCK, ARK5, BTK, YES, PTK5, TRKB, CaMKIIδ,γ, PRK2, ARG, MLK1, ALK)
pyridoindolcarboxamide 0.0008 irf1-bla HEL (IC50) 0.025 Lim et al. 2011
22 AT9283
(AuroraK, JAK3, FLT3, ABL)
pyrazole benzimidazole 0.0012 HEL (JAK2V617F)
SET-2 (JAK2V617F/wt)
Ba/F3:ETV6-JAK2
Ba/F3-IL-3
TF-1-IL-3
CMK (JAK2A572V)
0.110
0.057
0.016
0.017
0.040
0.026
Howard et al. 2009
Dawson et al. 2010
23 AZ960
(TRKA, AuroraA, ARK5, ALK, CaMKII, FLT4, FGFR1, LIMK1, BrSK2, FAK)
pyrazole nicotinonitrile 0.003 SET-2 (JAK2V617F/wt)
Ba/F3:TEL-JAK2
HTLV-1 infected T cells (MT-1, MT-2)
0.033
0.025
-
Gozgit et al. 2008
Yang et al. 2010
24 CMP6
(JAK1, JAK3, TYK2)
pyridone tetracycle 0.001 CTLL-2
B9
U266
KMS11
0.052-0.1
0.25
-
-
Thompson et al. 2002
Lucet et al. 2006
Pedranzini et al. 2006
25 "13" sulfonamide aminoindazole 0.078 - - Antonysamy et al. 2009
26 comp 9
(JAK3, ALK, cKIT, GCK)
polycyclic azaindole 0.001 TF-1-GMCSF (IC50)
HT2-IL2 (IC50)
0.27
1.53
Wang et al. 2009
27 "15a" polycyclic azaindole 0.0008 TF-1-GMCSF (IC50) 0.16 Wang et al. 2010
28 "40"
(JAK3)
aminopyrazolopyrimidine 0.0002 TF-1-GMCSF (IC50)
HT2-IL2 (IC50)
0.16
3.2
Ledeboer et al. 2009
29 "29"
(JAK1, JAK3)
pyrrolotriazine aminopyrrazole 0.0018 SET-2 0.11 Harikrishnan et al. 2011
30 atiprimod
(JAK3)
azaspirane - FDCP-EpoR,JAK2wt
FDCP-EpoR,JAK2V617F
SET-2
0.69
0.42
0.53
Hamasaki et al. 2005
Quintás-Cardama et al. 2011
31 G6 stilbenoid
(diaryleten)
0.060 Ba/F3:EpoR,JAK2V617F
HEL
-
4.0
Kiss et al. 2009
Majumder et al. 2010
Kirabo et al. 2011
32 NVP-BSK805
(JAK1, TYK2, ABL)
diarylquinoxaline 0.00048
0.00058
0.00056
Ba/F3:JAK2V617F
SET-2
MB-02
UKE-1
MUTZ-8
0.039
0.051
0.064
0.071
0.331
Baffert et al. 2010
33 "26"
(ABL)
diarylquinoxaline 0.0073 SET-2 0.088 Pissot-Soldermann et al. 2010
34 hexabromo cyclohexane cyclohexane low µM γ-2A - Sandberg et al. 2005
35 XL019
(JAK1, JAK3, FLT3, PDGFRB, cKIT)
arylaminopyrimidine 0.002 HEL - Paquette et al. 2008
Shah et al. 2008
Forsyth et al. 2012
36 CEP33779
(JAK1, JAK3)
triazolopyridine 0.0018 irf1-bla TF-1 (IC50) 0.061 Dugan et al. 2012
37 "29"
(JAK1, JAK3, TYK2)
triazolopyridine 0.0017 SET-2 (IC50) 0.212 Siu et al. 2013
38 "6"
(JAK1, JAK3, TYK2)
imidazopyrrolopyridine 0.0021 TF-1-EPO (IC50) 0.097 Zak et al. 2012
39 "7"
(JAK1, JAK3, TYK2)
imidazopyrrolopyridine 0.0012 TF-1-EPO (IC50) 0.86 Kulagowski et al. 2012
40 "31"
(JAK1, JAK3, TYK2)
imidazopyrrolopyridine 0.068 TF-1-EPO (IC50) 7.68 Zak et al. 2013
41 "46"
(JAK1, TYK2)
pyridine amide 0.028 TF-1-EPO (IC50) 1.7 Liang et al. 2013
42 "7j"
(JAK1, JAK3, TYK2)
pyrazolopyrimidine 0.0001 SET-2 (IC50)
TF-1-EPO (IC50)
0.0039
0.0074
Hanan et al. 2012
43 "6"
(JAK3)
pyrazolopyrimidine amine 0.003 Ba/F3:TEL-JAK2
SET-2
UKE1
0.006
0.078
0.050
Guan et al. 2013
44 "19a"
(JAK1, JAK3, CK2α2, KDR, ABL, FGR, TRKA, FLT4, FLT3, RET, ALK, FGFR1, AuroraA, LIMK1)
methylimidazole 0.002 Ba/F3:TEL-JAK2
SET-2
UKE1
0.012
0.014
0.055
Su et al. 2014
45 NS-018
(JAK1, JAK3, TYK2, SRC, FYN, YES, LYNa, FGR, LCK, HCK, ABL, FLT3)
pyrazinopyridine diamine 0.00072 Ba/F3:JAK2V617F
Ba/F3:TEL-JAK2
Ba/F3:MPLW515L
SET-2
Ba/F3:TEL-JAK3
MV4-11(FLT3-ITD)
0.060 0.011 0.061 0.120 0.800 0.730 Nakaya et al. 2011
Nakaya et al. 2014