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(→‎Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2)
(→‎Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2)
Linia 147: Linia 147:
 
|Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>Karpas-1106P<br>U266
 
|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
 
|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
 
|18
Linia 155: Linia 155:
 
|HEL
 
|HEL
 
|<nowiki>-</nowiki>
 
|<nowiki>-</nowiki>
−
|[Sayyah et al. 2008]
+
|[http://mct.aacrjournals.org/content/7/8/2308.abstract Sayyah et al. 2008]
 
|-
 
|-
 
|19
 
|19
Linia 163: Linia 163:
 
|Ba/F3:TEL-JAK2 (IC<sub>50</sub>)
 
|Ba/F3:TEL-JAK2 (IC<sub>50</sub>)
 
|1.62
 
|1.62
−
|[Schenkel et al. 2011]
+
|[http://dx.doi.org/10.1021/jm200911r Schenkel et al. 2011]
 
|-
 
|-
 
|20
 
|20
Linia 171: Linia 171:
 
|irf1-bla HEL (IC<sub>50</sub>)
 
|irf1-bla HEL (IC<sub>50</sub>)
 
|0.025
 
|0.025
−
|[Lim et al. 2011]
+
|[http://dx.doi.org/10.1021/jm200909u Lim et al. 2011]
 
|-
 
|-
 
|21
 
|21
Linia 179: Linia 179:
 
|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>)
 
|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
 
|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
 
|22
Linia 187: Linia 187:
 
|SET-2 (JAK2<sup>V617F/wt</sup>)<br>Ba/F3:TEL-JAK2<br>HTLV-1 infected T cells (MT-1, MT-2)
 
|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>-
 
|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
 
|23
Linia 195: Linia 195:
 
|CTLL-2<br>B9<br>U266<br>KMS11
 
|CTLL-2<br>B9<br>U266<br>KMS11
 
|0.052-0.1<br>0.25<br>-<br>-
 
|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
 
|24
Linia 203: Linia 203:
 
|<nowiki>-</nowiki>
 
|<nowiki>-</nowiki>
 
|<nowiki>-</nowiki>
 
|<nowiki>-</nowiki>
−
|[Antonysamy et al. 2009]
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X08010007 Antonysamy et al. 2009]
 
|-
 
|-
 
|25
 
|25
Linia 211: Linia 211:
 
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
 
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
 
|0.27<br>1.53
 
|0.27<br>1.53
−
|[Wang et al. 2009]
+
|[http://dx.doi.org/10.1021/jm901383u Wang et al. 2009]
 
|-
 
|-
 
|26
 
|26
Linia 219: Linia 219:
 
|TF-1-GMCSF (IC<sub>50</sub>)
 
|TF-1-GMCSF (IC<sub>50</sub>)
 
|0.16
 
|0.16
−
|[Wang et al. 2010]
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X09015911 Wang et al. 2010]
 
|-
 
|-
 
|27
 
|27
Linia 227: Linia 227:
 
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
 
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
 
|0.16<br>3.2
 
|0.16<br>3.2
−
|[Ledeboer et al. 2009]
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X09014541 Ledeboer et al. 2009]
 
|-
 
|-
 
|28
 
|28
Linia 235: Linia 235:
 
|SET-2
 
|SET-2
 
|0.11
 
|0.11
−
|[Harikrishnan et al. 2011]
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X11000357 Harikrishnan et al. 2011]
 
|-
 
|-
 
|29
 
|29
Linia 243: Linia 243:
 
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>SET-2
 
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>SET-2
 
|0.69<br>0.42<br>0.53
 
|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
 
|30
Linia 251: Linia 251:
 
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>HEL
 
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>HEL
 
|<nowiki>-</nowiki><br>4.0
 
|<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
 
|31
Linia 259: Linia 259:
 
|Ba/F3:JAK2<sup>V617F</sup><br>SET-2<br>MB-02<br>UKE-1<br>MUTZ-8
 
|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
 
|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
 
|32
Linia 267: Linia 267:
 
|SET-2
 
|SET-2
 
|0.088
 
|0.088
−
|[Pissot-Soldermann et al. 2010]
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X10002568 Pissot-Soldermann et al. 2010]
 
|-
 
|-
 
|33
 
|33
Linia 275: Linia 275:
 
|g-2A
 
|g-2A
 
|<nowiki>-</nowiki>
 
|<nowiki>-</nowiki>
−
|[Sandberg et al. 2005]
+
|[http://dx.doi.org/10.1021/jm049470k Sandberg et al. 2005]
 
|-
 
|-
 
|34
 
|34
Linia 283: Linia 283:
 
|HEL
 
|HEL
 
|<nowiki>-</nowiki>
 
|<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
 
|35
Linia 291: Linia 291:
 
|irf1-bla TF-1 (IC<sub>50</sub>)
 
|irf1-bla TF-1 (IC<sub>50</sub>)
 
|0.061
 
|0.061
−
|[Dugan et al. 2012]
+
|[http://dx.doi.org/10.1021/jm300248q Dugan et al. 2012]
 
|-
 
|-
 
|36
 
|36
Linia 299: Linia 299:
 
|SET-2 (IC<sub>50</sub>)
 
|SET-2 (IC<sub>50</sub>)
 
|0.212
 
|0.212
−
|[Siu et al. 2013]
+
|[http://www.sciencedirect.com/science/article/pii/S0960894X13007178 Siu et al. 2013]
 
|-
 
|-
 
|37
 
|37
Linia 307: Linia 307:
 
|TF-1-EPO (IC<sub>50</sub>)
 
|TF-1-EPO (IC<sub>50</sub>)
 
|0.097
 
|0.097
−
|[Zak et al. 2012]
+
|[http://dx.doi.org/10.1021/jm300628c Zak et al. 2012]
 
|-
 
|-
 
|38
 
|38
Linia 315: Linia 315:
 
|TF-1-EPO (IC<sub>50</sub>)
 
|TF-1-EPO (IC<sub>50</sub>)
 
|0.86
 
|0.86
−
|[Kulagowski et al. 2012]
+
|[http://dx.doi.org/10.1021/jm300438j Kulagowski et al. 2012]
 
|-
 
|-
 
|39
 
|39
Linia 323: Linia 323:
 
|TF-1-EPO (IC<sub>50</sub>)
 
|TF-1-EPO (IC<sub>50</sub>)
 
|7.68
 
|7.68
−
|[Zak et al. 2013]
+
|[http://dx.doi.org/10.1021/jm4004895 Zak et al. 2013]
 
|-
 
|-
 
|40
 
|40
Linia 331: Linia 331:
 
|TF-1-EPO (IC<sub>50</sub>)
 
|TF-1-EPO (IC<sub>50</sub>)
 
|1.7
 
|1.7
−
|[Liang et al. 2013]
+
|[http://www.sciencedirect.com/science/article/pii/S0223523413002304 Liang et al. 2013]
 
|-
 
|-
 
|41
 
|41
Linia 339: Linia 339:
 
|SET-2 (IC<sub>50</sub>)<br>TF-1-EPO (IC<sub>50</sub>)
 
|SET-2 (IC<sub>50</sub>)<br>TF-1-EPO (IC<sub>50</sub>)
 
|0.0039<br>0.0074
 
|0.0039<br>0.0074
−
|[Hanan et al. 2012]
+
|[http://dx.doi.org/10.1021/jm3012239 Hanan et al. 2012]
 
|-
 
|-
 
|42
 
|42
Linia 347: Linia 347:
 
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
 
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
 
|0.006<br>0.078<br>0.050
 
|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
 
|43
Linia 355: Linia 355:
 
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
 
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
 
|0.012<br>0.014<br>0.055
 
|0.012<br>0.014<br>0.055
−
|[Su et al. 2014]
+
|[http://dx.doi.org/10.1021/jm401546n Su et al. 2014]
 
|}
 
|}

Wersja z 19:47, 19 maj 2014

Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2

Lp. inhibitor
(inne hamowane kinazy) 		klasa chemiczna test enzym. test komórkowy            literatura           
IC50 (µM)         linia komórkowa         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 - - {http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;110/11/3538 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 Z3 pyridine 15.0
28.0 		HEL - Sayyah et al. 2008
19 "25"
(JAK1, GAK, YSK4) 		thienopyridine 0.002 Ba/F3:TEL-JAK2 (IC50) 1.62 Schenkel et al. 2011
20 "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
21 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
22 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
23 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
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 cyclohexane low µM g-2A - Sandberg et al. 2005
34 XL019
(JAK1, JAK3, FLT3, PDGFRB, cKIT) 		arylaminopyrimidine 0.002 HEL - Paquette et al. 2008
[ http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;112/11/98 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, 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
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