JAK2 inhibitor: Różnice pomiędzy wersjami

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
Nb	inhibitor (other kinase targets)	chemical class	IC₅₀ (µM)	cell line	GI₅₀ (µM)	references
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:JAK2^V617F HEL (JAK2^V617F) SET-2 (JAK2^V617F/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,JAK2^V617F Ba/F3:EpoR,JAK2^wt 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:JAK2^V617F 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:JAK2^wt Ba/F3:JAK2^V617F 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:JAK2^V617F 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:JAK2^V617F 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:JAK2^V617F	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:JAK2^V617F Ba/F3:JAK2^K539L Ba/F3:MPL^W515L 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,JAK2^wt FDCP-EpoR,JAK2^V617F	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,JAK2^V617F 32D:EpoR,JAK2^V617F HEL TF-1 U266 CHRF-288-11:JAK2^T875N 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,JAK2^wt FDCP-EpoR,JAK2^V617F 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:JAK2^V617F 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 (JAK2^V617F) SET-2 (JAK2^V617F/wt) Ba/F3:ETV6-JAK2 Ba/F3-IL-3 TF-1-IL-3 CMK (JAK2^A572V)	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 (JAK2^V617F/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,JAK2^wt FDCP-EpoR,JAK2^V617F 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,JAK2^V617F 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:JAK2^V617F 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:JAK2^V617F Ba/F3:TEL-JAK2 Ba/F3:MPL^W515L 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

JAK2 inhibitor: Różnice pomiędzy wersjami

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Aktualna wersja na dzień 16:07, 28 lis 2015

Small molecule inhibitors of the tyrosine kinase JAK2

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@@ Linia 1: / Linia 1: @@
-==Niskocząsteczkowe inhibitory domeny kinazowej JAK2==
+==Small molecule inhibitors of the tyrosine kinase JAK2==
 {|class="wikitable center" style="text-align:center; font-size:100%; border:1px"
-! rowspan=2|Lp.
+! rowspan=2|Nb
-! rowspan=2|inhibitor<br>(inne hamowane kinazy)
+! rowspan=2|inhibitor<br>(other kinase targets)
-! rowspan=2|klasa chemiczna
+! rowspan=2|chemical class
-! test enzym.
+! enzymatic test
-! colspan=2|test komórkowy
+! colspan=2|cell test
-! rowspan=2|literatura
+! 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;
 |-
 !scope="row"|IC<sub>50</sub> (&micro;M)
-!scope="row"|linia komórkowa
+!scope="row"|&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;cell&nbsp;line&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;
 !scope="row"|GI<sub>50</sub> (&micro;M)
 |-
@@ Linia 17: / Linia 17: @@
 |tyrphostin
 |36.4<br>48<br>145.3
-|B-precursor (KOCL-33,-45,-50,-69,KOPN-30bi,-55bi,-57bi,-72bi,KOPN-32,-62,-84,NALM 6)<br>T-precursor (KOPT-K1,-5,-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
+|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
-|<br><br><nowiki>-</nowiki><br>-<br>1.0<br>>20.0<br>>20.0<br>14.8<br>12.9<br>26.0<br>-<br>-<br>-
+|<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>-
-|Gazit&nbsp;et&nbsp;al.&nbsp;1989<br>Gazit et al. 1991<br>Meydan et al. 1996<br>Vos et al. 2000<br>Miyamoto et al. 2001<br>Burke et al. 2001<br>Duhé et al. 2002<br>Reddy et al. 2010<br>Jatiani et al. 2010
+|[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]
 |-
 |2
-|LS104<br>(BCR-ABL)
+!scope="row" style="background-color:LemonChiffon" |LS104<br>(BCR-ABL)
 |tyrphostin
 |2.52<br>0.1-0.6
-|Ba/F3:EpoR,JAK2<sup>V617F</sup>Ba/F3:EpoR,JAK2<sup>wt</sup><br>HEL
+|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>Ba/F3:EpoR,JAK2<sup>wt</sup><br>HEL
 |1.5<br>10.0
-|Grunberger et al. 2003<br>Lipka et al. 2008
+|[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
-|WP1066
+!scope="row" style="background-color:LemonChiffon" |WP1066
 |tyrphostin
 |<nowiki>-</nowiki>
 |HEL
 |2.3
-|Verstovsek et al. 2008
+|[http://clincancerres.aacrjournals.org/content/14/3/788.abstract Verstovsek et al. 2008]
 |-
 |4
-|ON044580<br>(BCR-ABL)
+!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
 |0.25<br>0.90<br>3.00
-|Reddy et al. 2010<br>Jatiani et al. 2010<br>Samanta et al. 2010
+|[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]
 |-
 |5
-|CEP701<br>(FLT3,JAK3)
+!scope="row" style="background-color:LemonChiffon" |lestaurtinib<br>(CEP701)<br>(FLT3,JAK3)
 |indolocarbazole
 |0.001
 |HEL
 |0.03-0.10
-|Hexner et al. 2008<br>Santos et al. 2010
+|[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]
 |-
 |6
-|Go6976<br>(JAK3, FLT3, PKC&alpha;,&beta;1)
+!scope="row" style="background-color:LemonChiffon" |G&ouml;6976<br>(JAK3, FLT3, PKC&alpha;,&beta;1)
 |indolocarbazole
 |0.13
 |32D<br>32D:TEL-JAK2<br>FDCP1<br>TF-1<br>Mo7E<br>HEL
 |0.093<br>0.242<br>-<br>-<br>-<br>-
-|Grandage et al. 2006
+|[http://dx.doi.org/10.1111/j.1365-2141.2006.06291.x Grandage et al. 2006]
 |-
 |7
-|TG02<br>(CDKs, FLT3)
+!scope="row" style="background-color:LemonChiffon" |TG02<br>(CDKs, TYK2, FLT3, TYRO3, ERK5, p38&delta;, Fms, Lck, Fyn, JAK1)
 |pyrimidine
 |<nowiki>-</nowiki>
 |HEL<br>SET-2<br>Ba/F3:JAK2<sup>wt</sup><br>Ba/F3:JAK2<sup>V617F</sup><br>Karpas-1106P<br>32D
 |0.202<br>0.231<br>0.156<br>0.099<br>0.068<br>0.098
-|Goh et al. 2011
+|[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]
 |-
 |8
-|TG101209<br>(FLT3, RET, JAK3)
+!scope="row" style="background-color:LemonChiffon" |TG101209<br>(FLT3, RET, JAK3)
 |pyrimidine
 |0.006
 |Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>multiple myeloma cell lines (RPMI8226, MM1S, OPM2, NCI-H929, Dox40, MM1R, LR5)
 |0.2<br>2-5<br>-
-|Pardanani et al. 2007<br>Wang and Fiskus et al. 2009<br>Ramkrishnan et al. 2010
+|[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]
 |-
 |9
-|TG101348<br>(FLT3, RET, JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |TG101348<br>(FLT3, RET, JAK1, JAK3, TYK2)
 |pyrimidine
 |0.003
 |Ba/F3:JAK2<sup>V617F</sup><br>HEL
 |0.270<br>0.305
-|Wernig et al. 2008<br>Animesh et al. 2009<br>Pardanani et al. 2011
+|[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]
 |-
 |10
-|R723<br>(JAK3, TYK2, FLT3, PRKD2, TBK1, SYK, PAK4, DAPK3, PRKD1, MYLK2, PRKCN, STK22D, IKBKE)
+!scope="row" style="background-color:LemonChiffon" |R723<br>(JAK3, TYK2, FLT3, PRKD2, TBK1, SYK, PAK4, DAPK3, PRKD1, MYLK2, PRKCN, STK22D, IKBKE)
 |pyrimidine
 |0.002
 |Ba/F3:JAK2<sup>V617F</sup>
 |0.13-0.20
-|Shide et al. 2009<br>Shide et al. 2011
+|[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]
 |-
 |11
-|INCB018424<br>(JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |INCB018424<br>(JAK1, JAK3, TYK2)
 |pyrrolopyrimidine
 |0.0045
 |<nowiki>-</nowiki>
 |<nowiki>-</nowiki>
-|Verstovsek et al. 2008<br>Verstovsek et al. 2010<br>Mesa 2010
+|[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]
 |-
 |12
-|INCB16562<br>(JAK1, JAK3)
+!scope="row" style="background-color:LemonChiffon" |INCB16562<br>(JAK1, JAK3)
 |pyrrolopyrimidine
 |0.0003
 |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
 |0.177<br>0.406<br>0.600<br>0.168<br>0.046<br>0.573
-|Koppikar et al. 2010
+|[http://bloodjournal.hematologylibrary.org/content/115/14/2919.abstract Koppikar et al. 2010]
 |-
 |13
-|CP690550<br>(JAK1, JAK3, TYK2)
+!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
-|Changelian et al. 2003<br>Chen et al. 2006<br>Clark et al. 2007<br>Manshouri et al. 2008<br>Meyer et al. 2010<br>Thoma et al. 2011
+|[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]
 |-
 |14
-|AZD1480<br>(JAK1, JAK3, TRKA, AuroraA, FLT4, FGFR1, ARK5)
+!scope="row" style="background-color:LemonChiffon" |AZD1480<br>(JAK1, JAK3, TRKA, AuroraA, FLT4, FGFR1, ARK5)
 |pyrazolopyrimidine
 |0.0004<br>|0.003
 |Ba/F3:TEL-JAK2<br>SET-2<br>UKE1<br>HEL
 |0.06<br>0.016<br>0.054<br>0.39
-|Hedvat et al. 2009<br>Ioannidis et al. 2011
+|[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]
 |-
 |15
-|CYT387<br>(JAK1, TYK2, CDK2/cyclinA, JNK1, PRKCN, PRKD1, ROCK2, TBK1)
+!scope="row" style="background-color:LemonChiffon" |CYT387<br>(JAK1, TYK2, CDK2/cyclinA, JNK1, PRKCN, PRKD1, ROCK2, TBK1)
 |aminopyrimidine
 |0.018
 |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
 |0.5<br>1.5<br>1.5<br>1.25<br>0.75<br>0.001<br>0.724
-|Pardanani et al. 2009<br>Tyner et al. 2010
+|[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]
 |-
 |16
-|SGI1252<br>(JAK1, JAK3, TYK2, YES, FLT3, ABL, SRC, LCK)
+!scope="row" style="background-color:LemonChiffon" |SGI1252<br>(JAK1, JAK3, TYK2, YES, FLT3, ABL, SRC, LCK)
 |diaminopyrimidine
-|0.002<br>0.0197
+|0.0054<br>0.002<br>0.0197
 |FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>UKE-1
 |0.074<br>0.110<br>0.441<br>0.055<br>0.089
-|Olsen et al. 2008<br>Riaz Ahmed et al. 2011
+|[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]
 |-
 |17
-|SB1518<br>(FLT3, JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |SB1518<br>(FLT3, JAK1, JAK3, TYK2)
 |aminopyrimidine macrocycle
 |0.023<br>0.019
 |Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>Karpas-1106P<br>U266
 |0.16<br>1.726<br>0.217<br>0.348<br>1.350
-|Hart et al. 2011<br>William et al. 2011
+|[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
-|Z3
+!scope="row" style="background-color:LemonChiffon" |"38"<br>(JAK1, TYK2, JAK3, MEKK2, MEKK3)
+|8-oxo-pyridopyrimidine
+|0.001
+|TF-1-EPO (IC<sub>50</sub>)
+|0.115
+|[http://www.sciencedirect.com/science/article/pii/S0960894X13010226 Labadie et al. 2013]
+|-
+|19
+!scope="row" style="background-color:LemonChiffon" |Z3
 |pyridine
 |15.0<br>28.0
 |HEL
-|Sayyah et al. 2008
+|<nowiki>-</nowiki>
+|[http://mct.aacrjournals.org/content/7/8/2308.abstract Sayyah et al. 2008]
 |-
-|19
+|20
-|"25"<br>(JAK1, GAK, YSK4)
+!scope="row" style="background-color:LemonChiffon" |"25"<br>(JAK1, GAK, YSK4)
 |thienopyridine
 |0.002
 |Ba/F3:TEL-JAK2 (IC<sub>50</sub>)
 |1.62
-|Schenkel et al. 2011
+|[http://dx.doi.org/10.1021/jm200911r Schenkel et al. 2011]
 |-
-|20
+|21
-|"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)
+!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)
 |pyridoindolcarboxamide
 |0.0008
 |irf1-bla HEL (IC<sub>50</sub>)
 |0.025
-|Lim et al. 2011
+|[http://dx.doi.org/10.1021/jm200909u Lim et al. 2011]
 |-
-|21
+|22
-|AT9283<br>(AuroraK, JAK3, FLT3, ABL)
+!scope="row" style="background-color:LemonChiffon" |AT9283<br>(AuroraK, JAK3, FLT3, ABL)
 |pyrazole benzimidazole
 |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
-|Howard et al. 2009<br>Dawson et al. 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]
 |-
-|22
+|23
-|AZ960<br>(TRKA, AuroraA, ARK5, ALK, CaMKII, FLT4, FGFR1, LIMK1, BrSK2, FAK)
+!scope="row" style="background-color:LemonChiffon" |AZ960<br>(TRKA, AuroraA, ARK5, ALK, CaMKII, FLT4, FGFR1, LIMK1, BrSK2, FAK)
 |pyrazole nicotinonitrile
 |0.003
 |SET-2 (JAK2<sup>V617F/wt</sup>)<br>Ba/F3:TEL-JAK2<br>HTLV-1 infected T cells (MT-1, MT-2)
 |0.033<br>0.025<br>-
-|Gozgit et al. 2008<br>Yang et al. 2010
+|[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]
 |-
-|23
+|24
-|CMP6<br>(JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |CMP6<br>(JAK1, JAK3, TYK2)
 |pyridone tetracycle
 |0.001
 |CTLL-2<br>B9<br>U266<br>KMS11
 |0.052-0.1<br>0.25<br>-<br>-
-|Thompson et al. 2002<br>Lucet et al. 2006<br>Pedranzini et al. 2008
+|[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]
 |-
-|24
+|25
-|"13"
+!scope="row" style="background-color:LemonChiffon" |"13"
 |sulfonamide aminoindazole
 |0.078
 |<nowiki>-</nowiki>
 |<nowiki>-</nowiki>
-|Antonysamy et al. 2009
+|[http://www.sciencedirect.com/science/article/pii/S0960894X08010007 Antonysamy et al. 2009]
 |-
-|25
+|26
-|comp 9<br>(JAK3, ALK, cKIT, GCK)
+!scope="row" style="background-color:LemonChiffon" |comp 9<br>(JAK3, ALK, cKIT, GCK)
 |polycyclic azaindole
 |0.001
 |TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
 |0.27<br>1.53
-|Wang et al. 2009
+|[http://dx.doi.org/10.1021/jm901383u Wang et al. 2009]
 |-
-|26
+|27
-|"15a"
+!scope="row" style="background-color:LemonChiffon" |"15a"
 |polycyclic azaindole
 |0.0008
 |TF-1-GMCSF (IC<sub>50</sub>)
 |0.16
-|Wang et al. 2010
+|[http://www.sciencedirect.com/science/article/pii/S0960894X09015911 Wang et al. 2010]
 |-
-|27
+|28
-|"40"<br>(JAK3)
+!scope="row" style="background-color:LemonChiffon" |"40"<br>(JAK3)
 |aminopyrazolopyrimidine
 |0.0002
 |TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
 |0.16<br>3.2
-|Ledeboer et al. 2009
+|[http://www.sciencedirect.com/science/article/pii/S0960894X09014541 Ledeboer et al. 2009]
 |-
-|28
+|29
-|"29"<br>(JAK1, JAK3)
+!scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3)
 |pyrrolotriazine aminopyrrazole
 |0.0018
 |SET-2
 |0.11
-|Harikrishnan et al. 2011
+|[http://www.sciencedirect.com/science/article/pii/S0960894X11000357 Harikrishnan et al. 2011]
 |-
-|29
+|30
-|atiprimod<br>(JAK3)
+!scope="row" style="background-color:LemonChiffon" |atiprimod<br>(JAK3)
 |azaspirane
 |<nowiki>-</nowiki>
 |FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>SET-2
 |0.69<br>0.42<br>0.53
-|Hamasaki et al. 2005<br>Quintás-Cardama et al. 2011
+|[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]
 |-
-|30
+|31
-|G6
+!scope="row" style="background-color:LemonChiffon" |G6
 |stilbenoid<br>(diaryleten)
 |0.060
 |Ba/F3:EpoR,JAK2<sup>V617F</sup><br>HEL
 |<nowiki>-</nowiki><br>4.0
-|Kiss et al. 2009<br>Majumder et al. 2010<br>Kirabo et al. 2011
+|[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]
 |-
-|31
+|32
-|NVP-BSK805<br>(JAK1, TYK2, ABL)
+!scope="row" style="background-color:LemonChiffon" |NVP-BSK805<br>(JAK1, TYK2, ABL)
 |diarylquinoxaline
 |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
 |0.039<br>0.051<br>0.064<br>0.071<br>0.331
-|Baffert et al. 2010
+|[http://mct.aacrjournals.org/content/9/7/1945.abstract Baffert et al. 2010]
 |-
-|32
+|33
-|"26"<br>(ABL)
+!scope="row" style="background-color:LemonChiffon" |"26"<br>(ABL)
 |diarylquinoxaline
 |0.0073
 |SET-2
 |0.088
-|Pissot-Soldermann et al. 2010
+|[http://www.sciencedirect.com/science/article/pii/S0960894X10002568 Pissot-Soldermann et al. 2010]
 |-
-|33
+|34
-|hexabromo cyclohexane
+!scope="row" style="background-color:LemonChiffon" |hexabromo cyclohexane
 |cyclohexane
 |low &micro;M
-|g-2A
+|&gamma;-2A
 |<nowiki>-</nowiki>
-|Sandberg et al. 2005
+|[http://dx.doi.org/10.1021/jm049470k Sandberg et al. 2005]
 |-
-|34
+|35
-|XL019<br>(JAK1, JAK3, FLT3, PDGFRB, cKIT)
+!scope="row" style="background-color:LemonChiffon" |XL019<br>(JAK1, JAK3, FLT3, PDGFRB, cKIT)
 |arylaminopyrimidine
 |0.002
 |HEL
 |<nowiki>-</nowiki>
-|Paquette et al. 2008<br>Shah et al. 2008<br>Forsyth et al. 2012
+|[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]
 |-
-|35
+|36
-|CEP33779<br>(JAK1, JAK3)
+!scope="row" style="background-color:LemonChiffon" |CEP33779<br>(JAK1, JAK3)
 |triazolopyridine
 |0.0018
 |irf1-bla TF-1 (IC<sub>50</sub>)
 |0.061
-|Dugan et al. 2012
+|[http://dx.doi.org/10.1021/jm300248q Dugan et al. 2012]
 |-
-|36
+|37
-|"29"<br>(JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3, TYK2)
 |triazolopyridine
 |0.0017
 |SET-2 (IC<sub>50</sub>)
 |0.212
-|Siu et al. 2013
+|[http://www.sciencedirect.com/science/article/pii/S0960894X13007178 Siu et al. 2013]
 |-
-|37
+|38
-|"6"<br>(JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK1, JAK3, TYK2)
 |imidazopyrrolopyridine
 |0.0021
 |TF-1-EPO (IC<sub>50</sub>)
 |0.097
-|Zak et al. 2012
+|[http://dx.doi.org/10.1021/jm300628c Zak et al. 2012]
 |-
-|38
+|39
-|"7"<br>(JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |"7"<br>(JAK1, JAK3, TYK2)
 |imidazopyrrolopyridine
 |0.0012
 |TF-1-EPO (IC<sub>50</sub>)
 |0.86
-|Kulagowski et al. 2012
+|[http://dx.doi.org/10.1021/jm300438j Kulagowski et al. 2012]
 |-
-|39
+|40
-|"31"<br>(JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |"31"<br>(JAK1, JAK3, TYK2)
 |imidazopyrrolopyridine
 |0.068
 |TF-1-EPO (IC<sub>50</sub>)
 |7.68
-|Zak et al. 2013
+|[http://dx.doi.org/10.1021/jm4004895 Zak et al. 2013]
 |-
-|40
+|41
-|"46"<br>(JAK1, TYK2)
+!scope="row" style="background-color:LemonChiffon" |"46"<br>(JAK1, TYK2)
 |pyridine amide
 |0.028
 |TF-1-EPO (IC<sub>50</sub>)
 |1.7
-|Liang et al. 2013
+|[http://www.sciencedirect.com/science/article/pii/S0223523413002304 Liang et al. 2013]
 |-
-|41
+|42
-|"7j"<br>(JAK1, JAK3, TYK2)
+!scope="row" style="background-color:LemonChiffon" |"7j"<br>(JAK1, JAK3, TYK2)
 |pyrazolopyrimidine
 |0.0001
 |SET-2 (IC<sub>50</sub>)<br>TF-1-EPO (IC<sub>50</sub>)
 |0.0039<br>0.0074
-|Hanan et al. 2012
+|[http://dx.doi.org/10.1021/jm3012239 Hanan et al. 2012]
 |-
-|42
+|43
-|"6"<br>(JAK3)
+!scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK3)
 |pyrazolopyrimidine amine
 |0.003
 |Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
 |0.006<br>0.078<br>0.050
-|Guan et al. 2013
+|[http://www.sciencedirect.com/science/article/pii/S0960894X13002989 Guan et al. 2013]
 |-
-|43
+|44
-|"19a"<br>(JAK1, JAK3, CK2&alpha;2, KDR, ABL, FGR, TRKA, FLT4, FLT3, RET, ALK, FGFR1, AuroraA, 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)
 |methylimidazole
 |0.002
 |Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
 |0.012<br>0.014<br>0.055
-|Su et al. 2014
+|[http://dx.doi.org/10.1021/jm401546n Su et al. 2014]
+|-
+|45
+!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
+|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)
+|0.060 0.011 0.061 0.120 0.800 0.730
+|[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]
 |}