Z BioInf
(→Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2) |
(→Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2) |
||
| Linia 157: | Linia 157: | ||
|[http://www.sciencedirect.com/science/article/pii/S0960894X13010226 Labadie et al. 2013] | |[http://www.sciencedirect.com/science/article/pii/S0960894X13010226 Labadie et al. 2013] | ||
|- | |- | ||
| − | | | + | |19 |
!scope="row" style="background-color:LemonChiffon" |Z3 | !scope="row" style="background-color:LemonChiffon" |Z3 | ||
|pyridine | |pyridine | ||
| Linia 165: | Linia 165: | ||
|[http://mct.aacrjournals.org/content/7/8/2308.abstract Sayyah et al. 2008] | |[http://mct.aacrjournals.org/content/7/8/2308.abstract Sayyah et al. 2008] | ||
|- | |- | ||
| − | | | + | |20 |
!scope="row" style="background-color:LemonChiffon" |"25"<br>(JAK1, GAK, YSK4) | !scope="row" style="background-color:LemonChiffon" |"25"<br>(JAK1, GAK, YSK4) | ||
|thienopyridine | |thienopyridine | ||
| Linia 173: | Linia 173: | ||
|[http://dx.doi.org/10.1021/jm200911r Schenkel et al. 2011] | |[http://dx.doi.org/10.1021/jm200911r Schenkel et al. 2011] | ||
|- | |- | ||
| − | | | + | |21 |
!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, CaMKIIδ,γ, 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, CaMKIIδ,γ, PRK2, ARG, MLK1, ALK) | ||
|pyridoindolcarboxamide | |pyridoindolcarboxamide | ||
| Linia 181: | Linia 181: | ||
|[http://dx.doi.org/10.1021/jm200909u Lim et al. 2011] | |[http://dx.doi.org/10.1021/jm200909u Lim et al. 2011] | ||
|- | |- | ||
| − | | | + | |22 |
!scope="row" style="background-color:LemonChiffon" |AT9283<br>(AuroraK, JAK3, FLT3, ABL) | !scope="row" style="background-color:LemonChiffon" |AT9283<br>(AuroraK, JAK3, FLT3, ABL) | ||
|pyrazole benzimidazole | |pyrazole benzimidazole | ||
| Linia 189: | Linia 189: | ||
|[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] | |[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] | ||
|- | |- | ||
| − | | | + | |23 |
!scope="row" style="background-color:LemonChiffon" |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 | |pyrazole nicotinonitrile | ||
| Linia 197: | Linia 197: | ||
|[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] | |[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] | ||
|- | |- | ||
| − | | | + | |24 |
!scope="row" style="background-color:LemonChiffon" |CMP6<br>(JAK1, JAK3, TYK2) | !scope="row" style="background-color:LemonChiffon" |CMP6<br>(JAK1, JAK3, TYK2) | ||
|pyridone tetracycle | |pyridone tetracycle | ||
| Linia 205: | Linia 205: | ||
|[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] | |[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] | ||
|- | |- | ||
| − | | | + | |25 |
!scope="row" style="background-color:LemonChiffon" |"13" | !scope="row" style="background-color:LemonChiffon" |"13" | ||
|sulfonamide aminoindazole | |sulfonamide aminoindazole | ||
| Linia 213: | Linia 213: | ||
|[http://www.sciencedirect.com/science/article/pii/S0960894X08010007 Antonysamy et al. 2009] | |[http://www.sciencedirect.com/science/article/pii/S0960894X08010007 Antonysamy et al. 2009] | ||
|- | |- | ||
| − | | | + | |26 |
!scope="row" style="background-color:LemonChiffon" |comp 9<br>(JAK3, ALK, cKIT, GCK) | !scope="row" style="background-color:LemonChiffon" |comp 9<br>(JAK3, ALK, cKIT, GCK) | ||
|polycyclic azaindole | |polycyclic azaindole | ||
| Linia 221: | Linia 221: | ||
|[http://dx.doi.org/10.1021/jm901383u Wang et al. 2009] | |[http://dx.doi.org/10.1021/jm901383u Wang et al. 2009] | ||
|- | |- | ||
| − | | | + | |27 |
!scope="row" style="background-color:LemonChiffon" |"15a" | !scope="row" style="background-color:LemonChiffon" |"15a" | ||
|polycyclic azaindole | |polycyclic azaindole | ||
| Linia 229: | Linia 229: | ||
|[http://www.sciencedirect.com/science/article/pii/S0960894X09015911 Wang et al. 2010] | |[http://www.sciencedirect.com/science/article/pii/S0960894X09015911 Wang et al. 2010] | ||
|- | |- | ||
| − | | | + | |28 |
!scope="row" style="background-color:LemonChiffon" |"40"<br>(JAK3) | !scope="row" style="background-color:LemonChiffon" |"40"<br>(JAK3) | ||
|aminopyrazolopyrimidine | |aminopyrazolopyrimidine | ||
| Linia 237: | Linia 237: | ||
|[http://www.sciencedirect.com/science/article/pii/S0960894X09014541 Ledeboer et al. 2009] | |[http://www.sciencedirect.com/science/article/pii/S0960894X09014541 Ledeboer et al. 2009] | ||
|- | |- | ||
| − | | | + | |29 |
!scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3) | !scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3) | ||
|pyrrolotriazine aminopyrrazole | |pyrrolotriazine aminopyrrazole | ||
| Linia 245: | Linia 245: | ||
|[http://www.sciencedirect.com/science/article/pii/S0960894X11000357 Harikrishnan et al. 2011] | |[http://www.sciencedirect.com/science/article/pii/S0960894X11000357 Harikrishnan et al. 2011] | ||
|- | |- | ||
| − | | | + | |30 |
!scope="row" style="background-color:LemonChiffon" |atiprimod<br>(JAK3) | !scope="row" style="background-color:LemonChiffon" |atiprimod<br>(JAK3) | ||
|azaspirane | |azaspirane | ||
| Linia 253: | Linia 253: | ||
|[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] | |[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] | ||
|- | |- | ||
| − | | | + | |31 |
!scope="row" style="background-color:LemonChiffon" |G6 | !scope="row" style="background-color:LemonChiffon" |G6 | ||
|stilbenoid<br>(diaryleten) | |stilbenoid<br>(diaryleten) | ||
| Linia 261: | Linia 261: | ||
|[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] | |[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] | ||
|- | |- | ||
| − | | | + | |32 |
!scope="row" style="background-color:LemonChiffon" |NVP-BSK805<br>(JAK1, TYK2, ABL) | !scope="row" style="background-color:LemonChiffon" |NVP-BSK805<br>(JAK1, TYK2, ABL) | ||
|diarylquinoxaline | |diarylquinoxaline | ||
| Linia 269: | Linia 269: | ||
|[http://mct.aacrjournals.org/content/9/7/1945.abstract Baffert et al. 2010] | |[http://mct.aacrjournals.org/content/9/7/1945.abstract Baffert et al. 2010] | ||
|- | |- | ||
| − | | | + | |33 |
!scope="row" style="background-color:LemonChiffon" |"26"<br>(ABL) | !scope="row" style="background-color:LemonChiffon" |"26"<br>(ABL) | ||
|diarylquinoxaline | |diarylquinoxaline | ||
| Linia 277: | Linia 277: | ||
|[http://www.sciencedirect.com/science/article/pii/S0960894X10002568 Pissot-Soldermann et al. 2010] | |[http://www.sciencedirect.com/science/article/pii/S0960894X10002568 Pissot-Soldermann et al. 2010] | ||
|- | |- | ||
| − | | | + | |34 |
!scope="row" style="background-color:LemonChiffon" |hexabromo cyclohexane | !scope="row" style="background-color:LemonChiffon" |hexabromo cyclohexane | ||
|cyclohexane | |cyclohexane | ||
| Linia 285: | Linia 285: | ||
|[http://dx.doi.org/10.1021/jm049470k Sandberg et al. 2005] | |[http://dx.doi.org/10.1021/jm049470k Sandberg et al. 2005] | ||
|- | |- | ||
| − | | | + | |35 |
!scope="row" style="background-color:LemonChiffon" |XL019<br>(JAK1, JAK3, FLT3, PDGFRB, cKIT) | !scope="row" style="background-color:LemonChiffon" |XL019<br>(JAK1, JAK3, FLT3, PDGFRB, cKIT) | ||
|arylaminopyrimidine | |arylaminopyrimidine | ||
| Linia 293: | Linia 293: | ||
|[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] | |[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] | ||
|- | |- | ||
| − | | | + | |36 |
!scope="row" style="background-color:LemonChiffon" |CEP33779<br>(JAK1, JAK3) | !scope="row" style="background-color:LemonChiffon" |CEP33779<br>(JAK1, JAK3) | ||
|triazolopyridine | |triazolopyridine | ||
| Linia 301: | Linia 301: | ||
|[http://dx.doi.org/10.1021/jm300248q Dugan et al. 2012] | |[http://dx.doi.org/10.1021/jm300248q Dugan et al. 2012] | ||
|- | |- | ||
| − | | | + | |37 |
!scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3, TYK2) | !scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3, TYK2) | ||
|triazolopyridine | |triazolopyridine | ||
| Linia 309: | Linia 309: | ||
|[http://www.sciencedirect.com/science/article/pii/S0960894X13007178 Siu et al. 2013] | |[http://www.sciencedirect.com/science/article/pii/S0960894X13007178 Siu et al. 2013] | ||
|- | |- | ||
| − | | | + | |38 |
!scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK1, JAK3, TYK2) | !scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK1, JAK3, TYK2) | ||
|imidazopyrrolopyridine | |imidazopyrrolopyridine | ||
| Linia 317: | Linia 317: | ||
|[http://dx.doi.org/10.1021/jm300628c Zak et al. 2012] | |[http://dx.doi.org/10.1021/jm300628c Zak et al. 2012] | ||
|- | |- | ||
| − | | | + | |39 |
!scope="row" style="background-color:LemonChiffon" |"7"<br>(JAK1, JAK3, TYK2) | !scope="row" style="background-color:LemonChiffon" |"7"<br>(JAK1, JAK3, TYK2) | ||
|imidazopyrrolopyridine | |imidazopyrrolopyridine | ||
| Linia 325: | Linia 325: | ||
|[http://dx.doi.org/10.1021/jm300438j Kulagowski et al. 2012] | |[http://dx.doi.org/10.1021/jm300438j Kulagowski et al. 2012] | ||
|- | |- | ||
| − | | | + | |40 |
!scope="row" style="background-color:LemonChiffon" |"31"<br>(JAK1, JAK3, TYK2) | !scope="row" style="background-color:LemonChiffon" |"31"<br>(JAK1, JAK3, TYK2) | ||
|imidazopyrrolopyridine | |imidazopyrrolopyridine | ||
| Linia 333: | Linia 333: | ||
|[http://dx.doi.org/10.1021/jm4004895 Zak et al. 2013] | |[http://dx.doi.org/10.1021/jm4004895 Zak et al. 2013] | ||
|- | |- | ||
| − | | | + | |41 |
!scope="row" style="background-color:LemonChiffon" |"46"<br>(JAK1, TYK2) | !scope="row" style="background-color:LemonChiffon" |"46"<br>(JAK1, TYK2) | ||
|pyridine amide | |pyridine amide | ||
| Linia 341: | Linia 341: | ||
|[http://www.sciencedirect.com/science/article/pii/S0223523413002304 Liang et al. 2013] | |[http://www.sciencedirect.com/science/article/pii/S0223523413002304 Liang et al. 2013] | ||
|- | |- | ||
| − | | | + | |42 |
!scope="row" style="background-color:LemonChiffon" |"7j"<br>(JAK1, JAK3, TYK2) | !scope="row" style="background-color:LemonChiffon" |"7j"<br>(JAK1, JAK3, TYK2) | ||
|pyrazolopyrimidine | |pyrazolopyrimidine | ||
| Linia 349: | Linia 349: | ||
|[http://dx.doi.org/10.1021/jm3012239 Hanan et al. 2012] | |[http://dx.doi.org/10.1021/jm3012239 Hanan et al. 2012] | ||
|- | |- | ||
| − | | | + | |43 |
!scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK3) | !scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK3) | ||
|pyrazolopyrimidine amine | |pyrazolopyrimidine amine | ||
| Linia 357: | Linia 357: | ||
|[http://www.sciencedirect.com/science/article/pii/S0960894X13002989 Guan et al. 2013] | |[http://www.sciencedirect.com/science/article/pii/S0960894X13002989 Guan et al. 2013] | ||
|- | |- | ||
| − | | | + | |44 |
!scope="row" style="background-color:LemonChiffon" |"19a"<br>(JAK1, JAK3, CK2α2, KDR, ABL, FGR, TRKA, FLT4, FLT3, RET, ALK, FGFR1, AuroraA, LIMK1) | !scope="row" style="background-color:LemonChiffon" |"19a"<br>(JAK1, JAK3, CK2α2, KDR, ABL, FGR, TRKA, FLT4, FLT3, RET, ALK, FGFR1, AuroraA, LIMK1) | ||
|methylimidazole | |methylimidazole | ||
| Linia 365: | Linia 365: | ||
|[http://dx.doi.org/10.1021/jm401546n 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) | !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 | |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) | |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) | ||
Wersja z 10:49, 20 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 | - | - | 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 | g-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 |