General
Preferred name
RUXOLITINIB
Synonyms
RUXOLITINIB PHOSPHATE ()
INCB-18424 ()
Ruxolitinib (sulfate) ()
INCB018424 sulfate ()
INCB-018424, Jakafi, Ruxolitinib Phosphate, INCB-018424 Salt ()
INCB018424 phosphate ()
INCB018424 ()
INC424 ()
INC 424 phosphate ()
(R)-Ruxolitinib ()
Ruxolitinib (INCB-18424) phosphate ()
INCB 018424 phosphate ()
INCB018424(R)-Ruxolitinib ()
INCB018424 (Ruxolitinib) ()
INCB18424 ()
Jakafi ()
CTP-543 ()
Ruxolitinib (INCB018424) ()
Ruxolitinib (phosphate) ()
INC-424 ()
INCB-018424 ()
JAKAVI ()
Ruxolitinib sulfate ()
INCB018424, INC424 ()
INCB-018424 PHOSPHATE ()
Ruxolitinib monophosphate ()
INCB018424 PHOSPHATE ()
Opzelura ()
Ruxolitinib (as phosphate) ()
INCB018424 SALT ()
INCB-018424 Salt ()
INCB-18424 PHOSPHATE ()
DEURUXOLITINIB ()
D8-ruxolitinib ()
C-21543 ()
CTP-543 phosphate ()
D8- ruxolitinib phosphate ()
D8-ruxolitinib phosphate ()
C-21543 phosphate ()
DEURUXOLITINIB PHOSPHATE ()
P&D ID
PD003424
CAS
941678-49-5
1092939-17-7
1092939-15-5
1513883-39-0
1092939-16-6
Tags
available
covalent binder
drug
drug candidate
probe
Approved by
FDA
EMA
First approval
2011
Drug indication
Alopecia
Nasopharyngeal carcinoma
Coronavirus Disease 2019 (COVID-19)
Atopic dermatitis
Essential thrombocythemia
Pancreatic cancer
High-risk myelofibrosis
Vitiligo
Drug Status
approved
investigational
Max Phase
4.0
3.0
1.0
Probe info
Probe type
experimental probe
calculated probe
Probe targets
JAK2
JAK1
JAK1,JAK2
Probe control
Probe control not defined
Orthogonal probes
41
Similar probes
2
Structure
RUXOLITINIB
JAK2, JAK1, J...
high-quality probe approved
RO5
MW
306.16
HBA
5
HBD
1
RB
4
LOGP
3.47
4
45
0
140
60
Probe scores
P&D probe-likeness score
20%
0%
20%
0%
0%
10%
10%
60%
P&D probe-likeness JAK1
67%
Probe Miner Score CAMK2A
100%
Cells score
Chemical Probes.org
100%
Organisms score
Chemical Probes.org
Structure formats
SMILES
N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1
InChI
InChI=1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/m1/s1
InChIkey
HFNKQEVNSGCOJV-OAHLLOKOSA-N
MOL
RUXOLITINIB RDKit 2D 23 26 0 0 0 0 0 0 0 0999 V2000 -10.5923 4.1480 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0 -9.1657 3.6844 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -7.7391 3.2209 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -7.4272 1.7537 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -8.5419 0.7500 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -8.3851 -0.7418 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -9.7555 -1.3519 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -10.7592 -0.2372 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -10.0092 1.0619 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -6.0006 1.2902 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0 -4.7871 2.1718 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -3.5736 1.2902 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -2.1470 1.7537 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -1.8351 3.2209 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0 -0.4086 3.6844 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 0.7062 2.6807 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0 0.3943 1.2135 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 1.2760 0.0000 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0 0.3943 -1.2135 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -1.0323 -0.7500 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -1.0323 0.7500 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -4.0371 -0.1364 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0 -5.5371 -0.1364 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0 1 2 3 0 2 3 1 0 4 3 1 1 4 5 1 0 5 6 1 0 6 7 1 0 7 8 1 0 8 9 1 0 4 10 1 0 10 11 1 0 11 12 2 0 12 13 1 0 13 14 2 0 14 15 1 0 15 16 2 0 16 17 1 0 17 18 1 0 18 19 1 0 19 20 2 0 20 21 1 0 12 22 1 0 22 23 2 0 9 5 1 0 23 10 1 0 21 13 1 0 21 17 2 0 M END > <ID> PD003424 > <Name> RUXOLITINIB
Description
(extracted from source data)
ABSORPTION Absorption is rapid and is not affected by food. ; Cmax, 15 mg, healthy subject = 649 nmol/L; ; Tmax, 15 mg, healthy subject = 1.5 hours;; Ruxolitinib does not accumulate significantly. ;
DESCPRITION a kinase inhibitor, inhibits Janus Associated Kinases (JAKs) JAK1 and JAK2 which mediate the signaling of a number of cytokines and growth factors that are important for hematopoiesis and immune function
COMMENT This compound inhibits JAK1 IC50 7 nM (1 mM ATP) and JAK2 IC50 9 nM (1 mM ATP) equally well. Because either JAK1 or JAK2 can be a part of any receptor pairing in any in vitro or in vivo setting, this probe evaluates the effect of pan-JAK inhibition. Jun 16 2016 - 5:22pm; Jun 16 2016 - 5:24pm; Validation for this compound is high. No significant inhibtion was observed in a panel of 26 kinases when tested at a concentration 100-fold higher than the IC50 observed for JAK1/2, though the modest selectivity against TYK2 is worth noting. Aug 29 2016 - 10:45am
DESCRIPTION Ruxolitinib is a Type-1 kinase inhibitor and was first approved by the US FDA in 2011. Ruxolitinib has high potency against Janus kinases 1 and 2 (JAK1, JAK2), as well as against the related family member, tyrosine kinase 2 (TYK2) . Inhibitory activity against JAK3 is only slightly reduced compared to the other three family kinases.
Marketed formulations may contain ruxolitinib phosphate (PubChem CID 25127112). (GtoPdb)
DESCRIPTION Deuruxolitinib (CTP-543) is a deuterium-modified analogue of the JAK inhibitor . It is an oral inhibitor that inhibits JAK1/2. The chemical structure, and its use in hair loss disorders are claimed in patent WO2017192905A1 . (GtoPdb)
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION inhibitor of Janus kinases 1 and 2 (Informer Set)
DESCRIPTION Treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera (post-PV) myelofibrosis and post-essential thrombocythemia (post-ET) myelofibrosis. [Lexicomp] Myeolofibrosis is the proliferation of abnormal bone marrow stem cells which cause fibrosis (the excessive formation of connective tissue). (PKIDB)
DESCRIPTION Potent and selective beta-secretase (BACE) inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Potent VEGFR, PDGFR and FGFR inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Ruxolitinib sulfate (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. (BOC Sciences Bioactive Compounds)
Protein targets
140
8.55
8.1
JAK2 Tyrosine-protein kinase JAK2 inhibitor BIOCHEM 1.2x CELL-BASED 1.1x
38
37
8.48
8.05
JAK1 Tyrosine-protein kinase JAK1 inhibitor
29
35
8.39
8
TYK2 Non-receptor tyrosine-protein kinase TYK2 inhibitor
20
17
7.82
HDAC6 Histone deacetylase 6
11
1
7.51
JAK1,JAK2 JAK2/JAK1
0
1
7.4
7.29
JAK3 Tyrosine-protein kinase JAK3 inhibitor
11
23
7.39
MAP3K2 Mitogen-activated protein kinase kinase kinase 2
0
1
7.34
CAMK2A Calcium/calmodulin-dependent protein kinase type II subunit alpha
21
1
7.17
DCLK1 Serine/threonine-protein kinase DCLK1
0
1
7.14
DAPK1 Death-associated protein kinase 1
1
1
7.05
DAPK3 Death-associated protein kinase 3
1
1
7.01
DAPK2 Death-associated protein kinase 2
1
1
6.92
GAK Cyclin-G-associated kinase
2
2
6.92
CAMK1D Calcium/calmodulin-dependent protein kinase type 1D
0
1
6.85
RPS6KA5 Ribosomal protein S6 kinase alpha-5
5
1
6.82
MAP3K3 Mitogen-activated protein kinase kinase kinase 3
1
1
6.82
RPS6KA2 Ribosomal protein S6 kinase alpha-2
7
1
6.8
LRRK2 Leucine-rich repeat serine/threonine-protein kinase 2
1
1
6.8
CAMK2G Calcium/calmodulin-dependent protein kinase type II subunit gamma
21
2
6.78
CAMK2D Calcium/calmodulin-dependent protein kinase type II subunit delta
20
2
6.72
ULK2 Serine/threonine-protein kinase ULK2
0
1
6.71
CAMK4 Calcium/calmodulin-dependent protein kinase type IV
6
1
6.71
Uncharacterized protein FLJ45252
0
1
6.71
7.19
JAK1,TYK2 JAK1/TYK2
0
4
6.7
MKNK2 MAP kinase-interacting serine/threonine-protein kinase 2
0
1
6.7
PLK4 Serine/threonine-protein kinase PLK4
7
1
6.65
ROCK1 Rho-associated protein kinase 1
15
2
6.58
DCLK3 Serine/threonine-protein kinase DCLK3
0
1
6.57
MAP3K19 Mitogen-activated protein kinase kinase kinase 19
0
1
6.54
IRAK1 Interleukin-1 receptor-associated kinase 1
18
1
6.53
JAK1,JAK2,TYK2 JAK1/JAK2/TYK2
0
1
6.52
ULK1 Serine/threonine-protein kinase ULK1
5
1
6.51
CAMK2B Calcium/calmodulin-dependent protein kinase type II subunit beta
21
1
6.5
NUAK2 NUAK family SNF1-like kinase 2
0
1
6.48
NTRK3 NT-3 growth factor receptor
10
1
6.48
7.7
JAK1,JAK3 JAK3/JAK1
0
4
6.47
RPS6KA4 Ribosomal protein S6 kinase alpha-4
1
1
6.44
NTRK2 BDNF/NT-3 growth factors receptor
14
1
6.44
MYLK Myosin light chain kinase, smooth muscle
2
1
6.41
PLK1 Serine/threonine-protein kinase PLK1
25
2
6.41
ANKK1 Ankyrin repeat and protein kinase domain-containing protein 1
0
1
6.4
AAK1 AP2-associated protein kinase 1
2
3
6.36
LTK Leukocyte tyrosine kinase receptor
1
1
6.34
CLK2 Dual specificity protein kinase CLK2
0
3
6.34
RPS6KA6 Ribosomal protein S6 kinase alpha-6
3
1
6.33
CAMK1 Calcium/calmodulin-dependent protein kinase type 1
2
1
6.33
MAP2K3 Dual specificity mitogen-activated protein kinase kinase 3
3
1
6.32
TTK Dual specificity protein kinase TTK
0
1
6.31
STK16 Serine/threonine-protein kinase 16
0
1
6.28
PRKCE Protein kinase C epsilon type
5
1
6.28
MAST1 Microtubule-associated serine/threonine-protein kinase 1
0
1
6.27
GRK7 Rhodopsin kinase GRK7
1
1
6.26
ROCK2 Rho-associated protein kinase 2
12
2
6.23
TAOK3 Serine/threonine-protein kinase TAO3
3
1
6.2
RET Proto-oncogene tyrosine-protein kinase receptor Ret
5
2
6.16
PRKG2 cGMP-dependent protein kinase 2
4
1
6.15
PLK3 Serine/threonine-protein kinase PLK3
2
1
6.14
MAP3K7 Mitogen-activated protein kinase kinase kinase 7
18
1
6.14
GRK1 Rhodopsin kinase GRK1
1
1
6.12
DCLK2 Serine/threonine-protein kinase DCLK2
0
1
6.07
CSNK1G1 Casein kinase I isoform gamma-1
0
1
6.03
BMPR2 Bone morphogenetic protein receptor type-2
1
1
6.02
JAK2,TYK2 JAK2/TYK2
0
1
6
RPS6KA1 Ribosomal protein S6 kinase alpha-1
8
2
6
HIPK2 Homeodomain-interacting protein kinase 2
6
1
5.96
MAP3K15 Mitogen-activated protein kinase kinase kinase 15
0
1
5.96
BMP2K BMP-2-inducible protein kinase
0
2
5.92
HIPK1 Homeodomain-interacting protein kinase 1
3
1
5.92
RIOK2 Serine/threonine-protein kinase RIO2
1
1
5.92
HIPK3 Homeodomain-interacting protein kinase 3
0
1
5.92
IKBKE Inhibitor of nuclear factor kappa-B kinase subunit epsilon
13
1
5.89
PAK5 Serine/threonine-protein kinase PAK 5
5
1
5.89
SBK1 Serine/threonine-protein kinase SBK1
0
1
5.89
SIK3 Serine/threonine-protein kinase SIK3
0
1
5.82
ALK ALK tyrosine kinase receptor
11
1
5.82
PLK2 Serine/threonine-protein kinase PLK2
3
1
5.82
CASK Peripheral plasma membrane protein CASK
7
1
5.82
NTRK1 High affinity nerve growth factor receptor
10
1
5.8
PAK4 Serine/threonine-protein kinase PAK 4
11
1
5.79
DYRK1A Dual specificity tyrosine-phosphorylation-regulated kinase 1A
1
2
5.77
TBK1 Serine/threonine-protein kinase TBK1
19
1
5.77
CLK4 Dual specificity protein kinase CLK4
0
2
5.75
CSNK1A1 Casein kinase I isoform alpha
15
1
5.75
MAP2K4 Dual specificity mitogen-activated protein kinase kinase 4
5
1
5.75
BMPR1B Bone morphogenetic protein receptor type-1B
1
1
5.72
STK39 STE20/SPS1-related proline-alanine-rich protein kinase
0
1
5.72
MAP2K1 Dual specificity mitogen-activated protein kinase kinase 1
15
1
5.72
MAP3K11 Mitogen-activated protein kinase kinase kinase 11
7
1
5.7
MAP4K2 Mitogen-activated protein kinase kinase kinase kinase 2
0
1
5.7
TAOK2 Serine/threonine-protein kinase TAO2
0
2
5.7
RIOK3 Serine/threonine-protein kinase RIO3
1
2
5.69
TNK2 Activated CDC42 kinase 1
1
2
5.68
RIPK4 Receptor-interacting serine/threonine-protein kinase 4
0
1
5.68
PHKG2 Phosphorylase b kinase gamma catalytic chain, liver/testis isoform
1
2
5.68
SRPK1 SRSF protein kinase 1
2
1
5.66
MELK Maternal embryonic leucine zipper kinase
0
1
5.66
CAMK1G Calcium/calmodulin-dependent protein kinase type 1G
0
1
5.64
IKBKB Inhibitor of nuclear factor kappa-B kinase subunit beta
29
1
5.62
ULK3 Serine/threonine-protein kinase ULK3
1
1
5.6
RIOK1 Serine/threonine-protein kinase RIO1
1
1
5.6
ERN1 Serine/threonine-protein kinase/endoribonuclease IRE1
1
1
5.57
MARK2 Serine/threonine-protein kinase MARK2
0
2
5.57
OXSR1 Serine/threonine-protein kinase OSR1
0
1
5.54
PAK6 Serine/threonine-protein kinase PAK 6
6
1
5.52
PKN1 Serine/threonine-protein kinase N1
6
1
5.52
BRAF Serine/threonine-protein kinase B-raf
16
1
5.51
EPHB6 Ephrin type-B receptor 6
4
1
5.51
MAPKAPK5 MAP kinase-activated protein kinase 5
3
1
5.51
STK26 Serine/threonine-protein kinase 26
1
1
5.49
CLK1 Dual specificity protein kinase CLK1
0
1
5.48
CDK7 Cyclin-dependent kinase 7
34
1
5.48
SRPK3 SRSF protein kinase 3
0
1
5.47
PI4KB Phosphatidylinositol 4-kinase beta
1
1
5.46
STK17B Serine/threonine-protein kinase 17B
0
1
5.46
ABL1 Tyrosine-protein kinase ABL1
13
1
5.46
DMPK Myotonin-protein kinase
1
1
5.45
TAOK1 Serine/threonine-protein kinase TAO1
6
2
5.45
CSNK2A2 Casein kinase II subunit alpha'
11
2
5.43
STRADA STE20-related kinase adapter protein alpha
1
1
5.43
DYRK2 Dual specificity tyrosine-phosphorylation-regulated kinase 2
1
1
5.4
MAP2K2 Dual specificity mitogen-activated protein kinase kinase 2
14
1
5.4
VRK2 Serine/threonine-protein kinase VRK2
7
1
5.38
CSNK2A1 Casein kinase II subunit alpha
11
1
5.38
MAP3K1 Mitogen-activated protein kinase kinase kinase 1
5
1
5.38
PKNB Serine/threonine-protein kinase PknB
0
1
5.32
MAPK8 Mitogen-activated protein kinase 8
12
1
5.31
NEK7 Serine/threonine-protein kinase Nek7
3
1
5.24
SBK3 Uncharacterized serine/threonine-protein kinase SBK3
0
1
5.24
NEK3 Serine/threonine-protein kinase Nek3
0
2
5.24
PHKG1 Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform
1
1
5.21
STK17A Serine/threonine-protein kinase 17A
0
1
5.21
EPHA3 Ephrin type-A receptor 3
3
1
5.21
GRK4 G protein-coupled receptor kinase 4
1
1
5.2
STK25 Serine/threonine-protein kinase 25
0
1
5.18
KIT Mast/stem cell growth factor receptor Kit
20
1
5.06
AURKC Aurora kinase C
0
1
4.83
MARK3 MAP/microtubule affinity-regulating kinase 3
10
1
4.8
CIT Citron Rho-interacting kinase
5
1
4.78
PRKCA Protein kinase C alpha type
20
1
4.35
NR1H2 Oxysterols receptor LXR-beta
9
1
Target pathways
410
Acetylcholine regulates insulin secretion
PRKCA
Activated NTRK2 signals through CDK5
NTRK2
Activated NTRK2 signals through FRS2 and FRS3
NTRK2
Activated NTRK2 signals through FYN
NTRK2
Activated NTRK2 signals through PI3K
NTRK2
Activated NTRK2 signals through PLCG1
NTRK2
Activated NTRK2 signals through RAS
NTRK2
Activated NTRK3 signals through PI3K
NTRK3
Activated NTRK3 signals through PLCG1
NTRK3
Activated NTRK3 signals through RAS
NTRK3
Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3
PKN1
activated TAK1 mediates p38 MAPK activation
MAP2K3
MAP3K7
IRAK1
Activation of BIM and translocation to mitochondria
MAPK8
Activation of BMF and translocation to mitochondria
MAPK8
Activation of IRF3, IRF7 mediated by TBK1, IKKε (IKBKE)
TBK1
IKBKE
Activation of NF-kappaB in B cells
IKBKB
MAP3K7
Activation of NIMA Kinases NEK9, NEK6, NEK7
NEK7
PLK1
Activation of RAC1
PAK4
PAK6
PAK5
Activation of RAC1 downstream of NMDARs
CAMK1
Activation of SMO
CSNK1A1
Activation of the AP-1 family of transcription factors
MAPK8
Aggrephagy
HDAC6
alectinib-resistant ALK mutants
ALK
ALK mutants bind TKIs
ALK
Alpha-protein kinase 1 signaling pathway
MAP3K7
Amplification of signal from unattached kinetochores via a MAD2 inhibitory signal
TAOK1
PLK1
Anchoring of the basal body to the plasma membrane
PLK4
PLK1
APC truncation mutants have impaired AXIN binding
CSNK1A1
APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1
PLK1
Apoptotic cleavage of cellular proteins
STK26
ROCK1
ARMS-mediated activation
BRAF
NTRK1
ASP-3026-resistant ALK mutants
ALK
Assembly and cell surface presentation of NMDA receptors
CAMK2A
CASK
CAMK2G
CAMK2B
CAMK2D
AURKA Activation by TPX2
PLK4
PLK1
AXIN missense mutants destabilize the destruction complex
CSNK1A1
BDNF activates NTRK2 (TRKB) signaling
NTRK2
Beta-catenin phosphorylation cascade
CSNK1A1
brigatinib-resistant ALK mutants
ALK
Ca2+ pathway
CAMK2A
PRKCA
PRKG2
MAP3K7
Calmodulin induced events
PRKCA
CaMK IV-mediated phosphorylation of CREB
CAMK2A
CAMK2G
CAMK2B
CAMK2D
CAMK4
Cargo recognition for clathrin-mediated endocytosis
AAK1
Caspase activation via Dependence Receptors in the absence of ligand
DAPK1
DAPK2
DAPK3
CD163 mediating an anti-inflammatory response
PLK2
CD209 (DC-SIGN) signaling
RPS6KA5
CDC42 GTPase cycle
PAK4
MAP3K11
PAK6
PAK5
ceritinib-resistant ALK mutants
ALK
cGMP effects
PRKG2
Chaperone Mediated Autophagy
HDAC6
Cilium Assembly
HDAC6
Clathrin-mediated endocytosis
AAK1
GAK
CLEC7A (Dectin-1) signaling
IKBKB
MAP3K7
Condensation of Prometaphase Chromosomes
CSNK2A2
CSNK2A1
Condensation of Prophase Chromosomes
PLK1
Constitutive Signaling by Aberrant PI3K in Cancer
NTRK2
KIT
NTRK3
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
HDAC6
Constitutive Signaling by NOTCH1 PEST Domain Mutants
HDAC6
Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding
CSNK2A2
CSNK2A1
CREB phosphorylation
RPS6KA1
RPS6KA2
RPS6KA5
CREB1 phosphorylation through NMDA receptor-mediated activation of RAS signaling
RPS6KA6
RPS6KA1
RPS6KA2
CREB1 phosphorylation through the activation of CaMKII/CaMKK/CaMKIV cascasde
CAMK2G
CAMK2B
CAMK4
crizotinib-resistant ALK mutants
ALK
CTNNB1 S33 mutants aren't phosphorylated
CSNK1A1
CTNNB1 S37 mutants aren't phosphorylated
CSNK1A1
CTNNB1 S45 mutants aren't phosphorylated
CSNK1A1
CTNNB1 T41 mutants aren't phosphorylated
CSNK1A1
Cyclin A/B1/B2 associated events during G2/M transition
CDK7
PLK1
Cyclin A:Cdk2-associated events at S phase entry
CDK7
Cyclin D associated events in G1
CDK7
JAK2
ABL1
Cyclin E associated events during G1/S transition
CDK7
DAG and IP3 signaling
PRKCE
Dasatinib-resistant KIT mutants
KIT
DDX58/IFIH1-mediated induction of interferon-alpha/beta
TBK1
Degradation of beta-catenin by the destruction complex
CSNK1A1
Degradation of GLI2 by the proteasome
CSNK1A1
Depolymerization of the Nuclear Lamina
PRKCA
Disassembly of the destruction complex and recruitment of AXIN to the membrane
CSNK1A1
Disinhibition of SNARE formation
PRKCA
Dopamine Neurotransmitter Release Cycle
CASK
Downstream TCR signaling
IKBKB
MAP3K7
Dual incision in TC-NER
CDK7
Effects of PIP2 hydrolysis
PRKCE
EGFR Transactivation by Gastrin
PRKCA
EML4 and NUDC in mitotic spindle formation
NEK7
TAOK1
PLK1
Energy dependent regulation of mTOR by LKB1-AMPK
STRADA
EPH-ephrin mediated repulsion of cells
EPHA3
EPHB6
EPH-Ephrin signaling
EPHA3
EPHB6
EPHA-mediated growth cone collapse
EPHA3
ROCK1
ROCK2
EPHB-mediated forward signaling
ROCK1
EPHB6
ROCK2
Ephrin signaling
EPHB6
ER-Phagosome pathway
IKBKB
ERK/MAPK targets
RPS6KA1
RPS6KA2
RPS6KA5
Erythropoietin activates Phosphoinositide-3-kinase (PI3K)
JAK2
Erythropoietin activates Phospholipase C gamma (PLCG)
JAK2
Erythropoietin activates RAS
JAK2
Erythropoietin activates STAT5
JAK2
Evasion by RSV of host interferon responses
JAK1
TYK2
Factors involved in megakaryocyte development and platelet production
JAK2
ABL1
FCERI mediated MAPK activation
MAPK8
MAP3K1
MAP2K4
FCERI mediated NF-kB activation
IKBKB
MAP3K7
FCGR3A-mediated phagocytosis
ABL1
Formation of HIV elongation complex in the absence of HIV Tat
CDK7
Formation of HIV-1 elongation complex containing HIV-1 Tat
CDK7
Formation of Incision Complex in GG-NER
CDK7
Formation of RNA Pol II elongation complex
CDK7
Formation of TC-NER Pre-Incision Complex
CDK7
Formation of the Early Elongation Complex
CDK7
Formation of the HIV-1 Early Elongation Complex
CDK7
Formation of the nephric duct
RET
Formation of the ureteric bud
RET
Frs2-mediated activation
BRAF
NTRK1
MAP2K2
MAP2K1
G alpha (12/13) signalling events
ROCK1
ROCK2
G alpha (z) signalling events
PRKCA
PRKCE
G0 and Early G1
DYRK1A
Gain-of-function MRAS complexes activate RAF signaling
BRAF
Gap-filling DNA repair synthesis and ligation in TC-NER
CDK7
Gastrin-CREB signalling pathway via PKC and MAPK
RPS6KA1
RPS6KA2
GLI3 is processed to GLI3R by the proteasome
CSNK1A1
Glycogen breakdown (glycogenolysis)
PHKG1
PHKG2
Golgi Associated Vesicle Biogenesis
GAK
Golgi Cisternae Pericentriolar Stack Reorganization
PLK1
Growth hormone receptor signaling
JAK2
HDR through Single Strand Annealing (SSA)
ABL1
Hedgehog 'on' state
ULK3
HIV Transcription Initiation
CDK7
HSF1 activation
HDAC6
HSF1-dependent transactivation
CAMK2A
CAMK2G
CAMK2B
CAMK2D
HuR (ELAVL1) binds and stabilizes mRNA
PRKCA
IFNG signaling activates MAPKs
JAK1
JAK2
IkBA variant leads to EDA-ID
IKBKB
IKBKB deficiency causes SCID
IKBKB
IKBKG deficiency causes anhidrotic ectodermal dysplasia with immunodeficiency (EDA-ID) (via TLR)
IKBKB
IKK complex recruitment mediated by RIP1
IKBKB
IL-6-type cytokine receptor ligand interactions
JAK1
TYK2
JAK2
Imatinib-resistant KIT mutants
KIT
Inactivation of CSF3 (G-CSF) signaling
JAK1
TYK2
JAK2
Inactivation, recovery and regulation of the phototransduction cascade
PRKCA
GRK1
GRK4
GRK7
Initiation of Nuclear Envelope (NE) Reformation
VRK2
Interferon alpha/beta signaling
JAK1
TYK2
Interferon gamma signaling
CAMK2A
CAMK2G
JAK1
CAMK2B
CAMK2D
JAK2
Interleukin receptor SHC signaling
JAK1
JAK2
JAK3
Interleukin-1 signaling
IKBKB
MAP3K7
MAP3K3
IRAK1
Interleukin-10 signaling
JAK1
TYK2
Interleukin-12 signaling
JAK1
TYK2
JAK2
Interleukin-15 signaling
JAK1
JAK3
Interleukin-2 signaling
JAK1
JAK3
Interleukin-20 family signaling
JAK1
TYK2
JAK2
JAK3
Interleukin-21 signaling
JAK1
JAK3
Interleukin-23 signaling
TYK2
JAK2
Interleukin-27 signaling
JAK1
TYK2
JAK2
Interleukin-3, Interleukin-5 and GM-CSF signaling
JAK2
Interleukin-35 Signalling
JAK1
TYK2
JAK2
Interleukin-37 signaling
TBK1
Interleukin-38 signaling
MAPK8
Interleukin-4 and Interleukin-13 signaling
JAK1
TYK2
JAK2
JAK3
Interleukin-6 signaling
JAK1
TYK2
JAK2
Interleukin-7 signaling
JAK1
JAK3
Interleukin-9 signaling
JAK1
JAK3
Ion homeostasis
CAMK2A
CAMK2G
DMPK
CAMK2B
CAMK2D
Ion transport by P-type ATPases
CAMK2A
CAMK2G
CAMK2B
CAMK2D
IRAK1 recruits IKK complex
IKBKB
IRAK1
IRAK1 recruits IKK complex upon TLR7/8 or 9 stimulation
IKBKB
IRAK1
IRAK2 mediated activation of TAK1 complex
MAP3K7
IRAK2 mediated activation of TAK1 complex upon TLR7/8 or 9 stimulation
MAP3K7
IRE1alpha activates chaperones
ERN1
IRF3 mediated activation of type 1 IFN
TBK1
IRF3-mediated induction of type I IFN
TBK1
ISG15 antiviral mechanism
JAK1
JNK (c-Jun kinases) phosphorylation and activation mediated by activated human TAK1
MAPK8
MAP3K7
MAP2K4
IRAK1
KEAP1-NFE2L2 pathway
CSNK2A2
CSNK2A1
KIT mutants bind TKIs
KIT
Late endosomal microautophagy
HDAC6
Long-term potentiation
CAMK2A
CAMK2G
CAMK2B
CAMK2D
lorlatinib-resistant ALK mutants
ALK
Loss of Nlp from mitotic centrosomes
PLK4
PLK1
Loss of phosphorylation of MECP2 at T308
CAMK4
Loss of proteins required for interphase microtubule organization from the centrosome
PLK4
PLK1
Macroautophagy
ULK1
Major pathway of rRNA processing in the nucleolus and cytosol
RIOK3
RIOK2
RIOK1
MAP2K and MAPK activation
BRAF
MAP2K2
MAP2K1
MARK3
MAP3K8 (TPL2)-dependent MAPK1/3 activation
IKBKB
MAP2K1
MAP2K4
MAPK1 (ERK2) activation
JAK1
MAP2K2
TYK2
JAK2
MAPK3 (ERK1) activation
JAK1
TYK2
MAP2K1
JAK2
MAPK6/MAPK4 signaling
MAPKAPK5
Masitinib-resistant KIT mutants
KIT
Maturation of hRSV A proteins
CSNK2A2
CSNK2A1
Maturation of nucleoprotein
SRPK1
CSNK1A1
MDK and PTN in ALK signaling
ALK
Mitotic Metaphase/Anaphase Transition
PLK1
Mitotic Prometaphase
TAOK1
PLK1
Mitotic Telophase/Cytokinesis
PLK1
MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis
ABL1
Modulation of host responses by IFN-stimulated genes
IKBKB
mRNA Capping
CDK7
MyD88 cascade initiated on plasma membrane
MAP3K1
IRAK1
MyD88 dependent cascade initiated on endosome
IRAK1
MyD88:MAL(TIRAP) cascade initiated on plasma membrane
MAP3K1
IRAK1
Myogenesis
ABL1
NCAM signaling for neurite out-growth
RPS6KA5
Negative feedback regulation of MAPK pathway
BRAF
MAP2K2
MAP2K1
Negative regulation of MAPK pathway
BRAF
MARK3
Negative regulation of NMDA receptor-mediated neuronal transmission
CAMK2A
CAMK2G
CAMK2B
CAMK2D
CAMK4
CAMK1
Negative regulators of DDX58/IFIH1 signaling
TBK1
IKBKE
Nephrin family interactions
CASK
Neurexins and neuroligins
CASK
Neutrophil degranulation
ROCK1
NF-kB activation through FADD/RIP-1 pathway mediated by caspase-8 and -10
IKBKB
NF-kB is activated and signals survival
IKBKB
IRAK1
NGF-independant TRKA activation
NTRK2
NTRK1
Nilotinib-resistant KIT mutants
KIT
NOD1/2 Signaling Pathway
IKBKB
MAP3K7
IRAK1
NoRC negatively regulates rRNA expression
CDK7
Notch-HLH transcription pathway
HDAC6
NOTCH1 Intracellular Domain Regulates Transcription
HDAC6
NPAS4 regulates expression of target genes
RET
PLK2
NR1H2 & NR1H3 regulate gene expression linked to lipogenesis
NR1H2
NR1H2 & NR1H3 regulate gene expression linked to triglyceride lipolysis in adipose
NR1H2
NR1H2 & NR1H3 regulate gene expression to control bile acid homeostasis
NR1H2
NR1H2 & NR1H3 regulate gene expression to limit cholesterol uptake
NR1H2
NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux
NR1H2
NRAGE signals death through JNK
MAPK8
NRIF signals cell death from the nucleus
MAPK8
NTF3 activates NTRK2 (TRKB) signaling
NTRK2
NTF3 activates NTRK3 signaling
NTRK3
NTF4 activates NTRK2 (TRKB) signaling
NTRK2
NTRK2 activates RAC1
NTRK2
NTRK3 as a dependence receptor
NTRK3
Nuclear Envelope Breakdown
VRK2
Nuclear Pore Complex (NPC) Disassembly
NEK7
Nuclear Receptor transcription pathway
NR1H2
NVP-TAE684-resistant ALK mutants
ALK
Other interleukin signaling
JAK1
TYK2
Oxidative Stress Induced Senescence
MAP2K3
MAPK8
MAPKAPK5
MAP2K4
p75NTR recruits signalling complexes
IKBKB
IRAK1
Paradoxical activation of RAF signaling by kinase inactive BRAF
CAMK2A
BRAF
CAMK2G
CAMK2B
MAP2K2
MAP3K11
CAMK2D
MAP2K1
JAK2
MARK3
Phase 0 - rapid depolarisation
CAMK2A
CAMK2G
CAMK2B
CAMK2D
Phosphorylation of Emi1
PLK1
Phosphorylation of the APC/C
PLK1
Physiological factors
HIPK2
HIPK1
PI3K/AKT activation
NTRK1
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling
NTRK2
KIT
NTRK3
IRAK1
PINK1-PRKN Mediated Mitophagy
TBK1
PIP3 activates AKT signaling
NTRK2
KIT
NTRK3
IRAK1
PKR-mediated signaling
IKBKB
PLC-gamma1 signalling
NTRK1
Polo-like kinase mediated events
PLK1
Potential therapeutics for SARS
TBK1
JAK1
TYK2
ROCK1
JAK2
JAK3
ROCK2
PPARA activates gene expression
NR1H2
Prolactin receptor signaling
JAK2
PTK6 promotes HIF1A stabilization
LRRK2
RAB GEFs exchange GTP for GDP on RABs
ULK1
RAC1 GTPase cycle
CIT
PAK4
VRK2
PKN1
PAK6
TAOK3
PAK5
RAC2 GTPase cycle
PAK4
VRK2
TAOK3
RAC3 GTPase cycle
PAK4
VRK2
TAOK3
RAF activation
CAMK2A
BRAF
CAMK2G
CAMK2B
MAP2K2
MAP3K11
CAMK2D
MAP2K1
JAK2
MARK3
RAF/MAP kinase cascade
CAMK2A
KIT
CAMK2G
JAK1
CAMK2B
CAMK2D
RET
JAK2
JAK3
Ras activation upon Ca2+ influx through NMDA receptor
CAMK2A
CAMK2G
CAMK2B
CAMK2D
RAS processing
PRKG2
Receptor Mediated Mitophagy
CSNK2A2
ULK1
CSNK2A1
Receptor-type tyrosine-protein phosphatases
NTRK3
Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks
MAPK8
ABL1
Recruitment of mitotic centrosome proteins and complexes
PLK4
PLK1
Recruitment of NuMA to mitotic centrosomes
PLK4
PLK1
Recycling pathway of L1
RPS6KA4
RPS6KA6
RPS6KA1
RPS6KA2
RPS6KA5
Regorafenib-resistant KIT mutants
KIT
Regulation of actin dynamics for phagocytic cup formation
ABL1
Regulation of IFNA/IFNB signaling
JAK1
TYK2
Regulation of IFNG signaling
JAK1
JAK2
Regulation of innate immune responses to cytosolic DNA
TBK1
Regulation of KIT signaling
KIT
PRKCA
Regulation of MECP2 expression and activity
CAMK2A
CAMK2G
HIPK2
CAMK2B
CAMK2D
CAMK4
Regulation of MITF-M-dependent genes involved in cell cycle and proliferation
PLK1
Regulation of NF-kappa B signaling
IKBKB
Regulation of PLK1 Activity at G2/M Transition
PLK4
PLK1
Regulation of PTEN stability and activity
CSNK2A2
CSNK2A1
Regulation of TBK1, IKKε (IKBKE)-mediated activation of IRF3, IRF7
TBK1
IKBKE
Regulation of TBK1, IKKε-mediated activation of IRF3, IRF7 upon TLR3 ligation
TBK1
IKBKE
Regulation of TNFR1 signaling
IKBKB
TBK1
ULK1
IKBKE
Regulation of TP53 Activity through Phosphorylation
HIPK2
CSNK2A2
CSNK2A1
HIPK1
DYRK2
MAPKAPK5
PLK3
Replacement of protamines by nucleosomes in the male pronucleus
SRPK1
Resolution of Sister Chromatid Cohesion
TAOK1
PLK1
Response to elevated platelet cytosolic Ca2+
PRKCA
RET signaling
PRKCA
RET
Retrograde neurotrophin signalling
NTRK1
RHO GTPases activate CIT
CIT
RHO GTPases Activate Formins
TAOK1
PLK1
RHO GTPases Activate NADPH Oxidases
PRKCA
RHO GTPases activate PAKs
MYLK
RHO GTPases activate PKNs
PKN1
RHO GTPases Activate ROCKs
ROCK1
ROCK2
RHO GTPases Activate WASPs and WAVEs
ABL1
RHOA GTPase cycle
CIT
PKN1
ROCK1
ROCK2
RHOB GTPase cycle
CIT
PKN1
ROCK1
ROCK2
RHOBTB1 GTPase cycle
ROCK1
ROCK2
RHOC GTPase cycle
CIT
PKN1
ROCK1
ROCK2
RHOD GTPase cycle
VRK2
PAK6
PAK5
RHOG GTPase cycle
PAK4
VRK2
MAP3K11
RHOH GTPase cycle
PAK4
ROCK1
PAK6
ROCK2
PAK5
RHOJ GTPase cycle
PAK4
RHOQ GTPase cycle
PAK4
RHOU GTPase cycle
PAK4
RHOV GTPase cycle
PAK4
MAP3K11
PAK6
RIP-mediated NFkB activation via ZBP1
IKBKB
RMTs methylate histone arginines
JAK2
RNA Pol II CTD phosphorylation and interaction with CE
CDK7
RNA Pol II CTD phosphorylation and interaction with CE during HIV infection
CDK7
RNA Polymerase I Promoter Escape
CDK7
RNA Polymerase I Transcription Initiation
CDK7
RNA Polymerase I Transcription Termination
CDK7
RNA Polymerase II HIV Promoter Escape
CDK7
RNA Polymerase II Pre-transcription Events
CDK7
RNA Polymerase II Promoter Escape
CDK7
RNA polymerase II transcribes snRNA genes
CDK7
RNA Polymerase II Transcription Elongation
CDK7
RNA Polymerase II Transcription Initiation
CDK7
RNA Polymerase II Transcription Initiation And Promoter Clearance
CDK7
RNA Polymerase II Transcription Pre-Initiation And Promoter Opening
CDK7
RND3 GTPase cycle
ROCK1
ROBO receptors bind AKAP5
PRKCA
Role of ABL in ROBO-SLIT signaling
ABL1
Role of phospholipids in phagocytosis
PRKCE
RSK activation
RPS6KA6
RPS6KA1
RPS6KA2
RUNX1 interacts with co-factors whose precise effect on RUNX1 targets is not known
HIPK2
CSNK2A2
CSNK2A1
RUNX1 regulates transcription of genes involved in differentiation of HSCs
CDK7
ABL1
RUNX2 regulates osteoblast differentiation
ABL1
HDAC6
SARS-CoV-1 activates/modulates innate immune responses
TBK1
IKBKE
SARS-CoV-2 activates/modulates innate and adaptive immune responses
IKBKB
TBK1
JAK1
IKBKE
TYK2
MAP3K7
IRAK1
Sema4D induced cell migration and growth-cone collapse
ROCK1
ROCK2
Senescence-Associated Secretory Phenotype (SASP)
RPS6KA1
RPS6KA2
Sensory processing of sound by inner hair cells of the cochlea
CASK
Sensory processing of sound by outer hair cells of the cochlea
CASK
Separation of Sister Chromatids
TAOK1
PLK1
SHC1 events in ERBB2 signaling
PRKCA
PRKCE
SHOC2 M1731 mutant abolishes MRAS complex function
BRAF
Signal transduction by L1
CSNK2A2
MAP2K2
CSNK2A1
MAP2K1
Signaling by ALK
JAK3
ALK
Signaling by ALK fusions and activated point mutants
MAPK8
TYK2
ALK
Signaling by BMP
BMPR1B
BMPR2
Signaling by BRAF and RAF1 fusions
CAMK2A
BRAF
CAMK2G
CAMK2B
MAP2K2
CAMK2D
MAP2K1
JAK2
MARK3
Signaling by CSF3 (G-CSF)
JAK1
TYK2
JAK2
Signaling by Erythropoietin
JAK2
Signaling by extracellular domain mutants of KIT
KIT
Signaling by GSK3beta mutants
CSNK1A1
Signaling by high-kinase activity BRAF mutants
BRAF
MAP2K2
MAP2K1
MARK3
Signaling by juxtamembrane domain KIT mutants
KIT
Signaling by kinase domain mutants of KIT
KIT
Signaling by Leptin
JAK2
Signaling by LTK
LTK
TNK2
Signaling by MAP2K mutants
MAP2K2
MAP2K1
Signaling by moderate kinase activity BRAF mutants
CAMK2A
BRAF
CAMK2G
CAMK2B
MAP2K2
MAP3K11
CAMK2D
MAP2K1
JAK2
MARK3
Signaling by NTRK3 (TRKC)
NTRK3
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants
KIT
JAK2
Signaling by RAF1 mutants
CAMK2A
BRAF
CAMK2G
CAMK2B
MAP2K2
CAMK2D
MAP2K1
JAK2
MARK3
Signaling by SCF-KIT
KIT
PRKCA
JAK2
Signaling downstream of RAS mutants
CAMK2A
BRAF
CAMK2G
CAMK2B
MAP2K2
MAP3K11
CAMK2D
MAP2K1
JAK2
MARK3
Signalling to p38 via RIT and RIN
BRAF
NTRK1
Signalling to RAS
NTRK1
Signalling to STAT3
NTRK1
SLC15A4:TASL-dependent IRF5 activation
IKBKB
Smooth Muscle Contraction
MYLK
Sorafenib-resistant KIT mutants
KIT
Spry regulation of FGF signaling
BRAF
STAT6-mediated induction of chemokines
TBK1
SUMOylation of immune response proteins
IKBKE
SUMOylation of intracellular receptors
NR1H2
SUMOylation of transcription cofactors
HIPK2
Sunitinib-resistant KIT mutants
KIT
Syndecan interactions
CASK
PRKCA
Synthesis of PC
CSNK2A2
CSNK2A1
Synthesis of PIPs at the Golgi membrane
PI4KB
TAK1-dependent IKK and NF-kappa-B activation
IKBKB
MAP3K7
IRAK1
Tat-mediated elongation of the HIV-1 transcript
CDK7
TBC/RABGAPs
ULK1
Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation
PRKG2
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors
KIT
The role of GTSE1 in G2/M progression after G2 checkpoint
PLK1
TICAM1, RIP1-mediated IKK complex recruitment
IKBKB
TICAM1,TRAF6-dependent induction of TAK1 complex
MAP3K7
TICAM1-dependent activation of IRF3/IRF7
TBK1
IKBKE
TNFR1-induced NF-kappa-B signaling pathway
IKBKB
MAP3K7
TNFR1-induced proapoptotic signaling
TBK1
IKBKE
TP53 regulates transcription of additional cell cycle genes whose exact role in the p53 pathway remain uncertain
PLK3
PLK2
TP53 Regulates Transcription of DNA Repair Genes
CDK7
TRAF3-dependent IRF activation pathway
TBK1
IKBKE
TRAF6 mediated induction of NFkB and MAP kinases upon TLR7/8 or 9 activation
MAP3K1
IRAK1
TRAF6 mediated IRF7 activation
TBK1
IKBKE
TRAF6 mediated IRF7 activation in TLR7/8 or 9 signaling
IRAK1
TRAF6 mediated NF-kB activation
IKBKB
MAP3K1
TRAF6-mediated induction of TAK1 complex within TLR4 complex
MAP3K7
Trafficking of AMPA receptors
CAMK2A
CAMK2G
CAMK2B
CAMK2D
Trafficking of GluR2-containing AMPA receptors
PRKCA
Transcription of the HIV genome
CDK7
Transcription-Coupled Nucleotide Excision Repair (TC-NER)
CDK7
Transcriptional activation of mitochondrial biogenesis
CAMK4
Transcriptional and post-translational regulation of MITF-M expression and activity
KIT
RPS6KA1
MARK3
Transcriptional Regulation by MECP2
IRAK1
Transcriptional regulation by RUNX2
HDAC6
TRKA activation by NGF
NTRK1
Truncations of AMER1 destabilize the destruction complex
CSNK1A1
Turbulent (oscillatory, disturbed) flow shear stress activates signaling by PIEZO1 and integrins in endothelial cells
IKBKB
IKBKE
ABL1
Ub-specific processing proteases
MAP3K7
Unblocking of NMDA receptors, glutamate binding and activation
CAMK2A
CAMK2G
CAMK2B
CAMK2D
Uptake and function of anthrax toxins
MAP2K3
MAP2K2
MAP2K1
MAP2K4
VEGFA-VEGFR2 Pathway
ROCK1
ROCK2
VEGFR2 mediated cell proliferation
PRKCA
VLDLR internalisation and degradation
NR1H2
WNT mediated activation of DVL
CSNK2A2
CSNK2A1
WNT5:FZD7-mediated leishmania damping
MAPK8
WNT5A-dependent internalization of FZD4
PRKCA
YAP1- and WWTR1 (TAZ)-stimulated gene expression
HIPK2
HIPK1
References
56
2023 Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
Thoma G, Duthaler RO et al. J Med Chem
2023 Discovery of C-5 Pyrazole-Substituted Pyrrolopyridine Derivatives as Potent and Selective Inhibitors for Janus Kinase 1.
Lang JJ, Lv Y et al. J Med Chem
2023 Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers.
Qiu Q, Chi F et al. J Med Chem
2023 Novel Concept for Super-Soft Topical Drugs: Deactivation by an Enzyme-Induced Switch into an Inactive Conformation.
Thoma G, Vangrevelinghe E et al. ACS Med Chem Lett
2023 A JAK tyrosine kinase and pseudokinase Co-inhibition strategy combines enhanced potency and on-demand activation.
Chen X, Zhang L et al. Eur J Med Chem
2022 Discovery of Novel Pyrrolo[2,3-<i>d</i>]pyrimidine-based Derivatives as Potent JAK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors.
Liang X, Tang S et al. J Med Chem
2022 Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
Raghuvanshi R, Bharate SB. J Med Chem
2022 A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
Gu J, Wu Q et al. Eur J Med Chem
2022 Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases.
Shen P, Wang Y et al. Eur J Med Chem
2022 Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
Liosi ME, Ippolito JA et al. J Med Chem
2022 Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.
Li G, Cheng Y et al. RSC Med Chem
2021 Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.
Liao M, Zhang J et al. J Med Chem
2021 Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.
Davis RR,Li B et al. J Med Chem
2021 Discovery of novel JAK2 and EGFR inhibitors from a series of thiazole-based chalcone derivatives
Sanachai, Kamonpan et al. RSC Med Chem
2021 Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors.
Gao D, Jin N et al. Eur J Med Chem
Screening of ~5500 FDA-approved drugs and clinical candidates for anti-SARS-CoV-2 activity (dataset)
2020 The Exploration of Chirality for Improved Druggability within the Human Kinome.
Saha D, Kharbanda A et al. J Med Chem
2020 Discovery of (2R)-N-[3-[2-[(3-methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a potent and selective Janus Kinase 1 (JAK1) inhibitor.
Su Q, Banks E et al. J. Med. Chem.
2020 Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.
Shu L,Chen C et al. Eur J Med Chem
2019 Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.
Wang W, Diao Y et al. Bioorg Med Chem Lett
2019 Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.
Gehringer M, Laufer SA. J Med Chem
2019 The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors.
Egyed A, Bajusz D et al. Bioorg Med Chem
2019 Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
Liang X, Zang J et al. J Med Chem
2019 Identify liver X receptor β modulator building blocks by developing a fluorescence polarization-based competition assay.
Zhang Z, Chen H et al. Eur J Med Chem
2018 Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Vazquez ML, Kaila N et al. J. Med. Chem.
2018 Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.
Grimster NP, Anderson E et al. J Med Chem
2018 Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90).
Yao L, Ohlson S et al. Bioorg Med Chem Lett
2018 Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).
Yao L, Ramanujulu PM et al. Bioorg Med Chem Lett
2017 The target landscape of clinical kinase drugs.
Klaeger S, Heinzlmeir S and Wilhelm M et al Science
2017 Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
Yao L, Mustafa N et al. J Med Chem
2017 Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.
Murár M, Dobia¿ J et al. Eur J Med Chem
2017 Treatment of hair loss disorders with deuterated jak inhibitors
Wagner AT, Cassella JV et al. PATENT: WO2017192905A1
2016 Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.
Simov V, Deshmukh SV et al. Bioorg. Med. Chem. Lett.
2016 Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.
Liang X, Huang Y et al. Bioorg. Med. Chem.
2016 The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3.
Lee SM, Yoon KB et al. Bioorg Med Chem
2016 Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1<i>H</i>)-pyrazole Derivatives as JAKs Inhibitors.
Liang X, Zang J et al. ACS Med Chem Lett
2014 Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Clark JD, Flanagan ME et al. J. Med. Chem.
2014 Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.
McDonnell ME; Bian H et al.
2014 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Menet CJ; Fletcher SR et al.
2013 Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.
Lynch SM; DeVicente J et al.
2013 Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.
Liang J; van Abbema A et al.
2012 Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Hanan EJ, van Abbema A et al. J. Med. Chem.
2012 Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.
Kulagowski JJ; Blair W et al.
2012 Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Zak M; Mendonca R et al.
2012 Inhibitors of Stat5 protein signalling
Cumaraswamy AA, Todic A et al. MedChemComm
2011 Comprehensive analysis of kinase inhibitor selectivity.
Davis MI, Hunt JP et al. Nat. Biotechnol.
2010 Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms.
Quintás-Cardama A, Vaddi K et al. Blood
2010 Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.
Malerich JP; Lam JS et al.
Compositions and methods for treating beta-globinopathies
PATENT: US-20200216545-A1
Bursulaya, B; Fisch, A et al. PATENT: US10112907
Bursulaya, B; Fisch, A et al. PATENT: US10766894
Fuller, PH; Brubaker, J et al. PATENT: US10875847
Bursulaya, B; Fisch, A et al. PATENT: US11203595
CovalentInDB (dataset)
PKIDB (dataset)
Chemical Probes.org (dataset)
Cell lines
7
6.9
BaF3
6.35
PBMC
5.13
HEL
4.99
K562
4.84
TF-1
4.8
MOLT-4
4.74
HEL 92.1.7
Organisms
2
6.7
Human immunodeficiency virus 2
6.52
Human immunodeficiency virus 1
Compound Sets
45
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
Chemical Probes.org
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CovalentInDB
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
Informer Set
JUMP-MOA Compound Set
JUMP-Target 1 Compound Set
Kinase Inhibitors (best-in-class)
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tool Compound Set
Welcome Trust Cancer Drugs
ZINC Tool Compounds
Available from
11
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Properties
(calculated by RDKit )
Molecular Weight
306.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
3.47
TPSA
83.18
Fraction CSP3
0.41
Chiral centers
1.0
Largest ring
6.0
QED
0.8
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
JAK1
JAK2
Tyrosine-protein kinase JAK2
JAK1, JAK2, TYK2
JAK
Autophagy
Tyrosine-protein kinase JAK1
TYK2
JAK1, JAK2, JAK3, TYK2
JAK1/2 inhibitor
Mitophagy
Apoptosis related,Autophagy,JAK,Mitophagy
JAK1, JAK2
Compound status
FDA
Kinase group
TK
Pathway
Epigenetics
Stem Cell/Wnt
JAK/STAT Signaling
Angiogenesis
Chromatin/Epigenetic
Stem Cells
Tyrosine Kinase/Adaptors
Apoptosis
Protein Tyrosine Kinase/RTK
Targets
JAK1,JAK2
Primary Target
JAK Kinase
MOA
Inhibitor
JAK tyrosine kinase inhibitor
JAK inhibitor
Member status
virtual
Indication
myelofibrosis, polycythemia vera
Disease Area
hematologic malignancy, hematology
Target class
Protein kinase
Kinase, Kinase
Orthogonal probe
Baricitinib
Therapeutic Class
Antiviral Agents
Target subclass
TK, TK
Recommended Cell Concentration
None
Source data