BDBM50355501 INCB-018424::RUXOLITINIB::RUXOLITINIB PHOSPHATE::US10112907, Example 00016::US10766894, Compound TABLE 1.1::US10875847, Compound JAKAFI::US11203595, TABLE 1.1::US11279703, TABLE 6.147::US20240140952, Compound Ruxolitinib

SMILES N#CC[C@H](C1CCCC1)n1cc(cn1)-c1ncnc2[nH]ccc12

InChI Key InChIKey=HFNKQEVNSGCOJV-OAHLLOKOSA-N

Data  12 KI  141 IC50  447 Kd  6 EC50

PDB links: 5 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 606 hits for monomerid = 50355501   

TargetTyrosine-protein kinase JAK1(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  0.0900nMAssay Description:Inhibition of purified JAK1 incubated for 30 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank


TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of human JAK2 (828-1132) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank
PDB3D3D Structure (crystal)

TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of JAK2 kinase domain using N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank
PDB3D3D Structure (crystal)

TargetTyrosine-protein kinase JAK1(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of JAK1 kinase domain using N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank


TargetTyrosine-protein kinase JAK1(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of human JAK1 (837-1142) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank


TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  0.240nMAssay Description:Inhibition of purified JAK2 incubated for 30 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank
PDB3D3D Structure (crystal)

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  0.5nMAssay Description:Inhibition of TYK2 kinase domain using N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  0.550nMAssay Description:Inhibition of purified TYK2 incubated for 30 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase JAK3(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  3.20nMAssay Description:Inhibition of human JAK3 (781-1124) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase JAK3(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  3.20nMAssay Description:Inhibition of JAK3 kinase domain using N-terminal 5-carboxyfluorescein-tagged Leu-Pro-Leu-Asp-Lys-Asp-Tyr-Tyr-Val-Val-Arg as substrate after 30 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase JAK3(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  3.22nMAssay Description:Inhibition of purified JAK3 incubated for 30 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetOxysterols receptor LXR-beta(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKi:  4.50E+4nMAssay Description:Binding affinity to recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as inhibitory constant incubated for 30 mins by f...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase JAK1(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  6.40nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank


TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  8.80nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank
PDB3D3D Structure (crystal)

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  30nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  194nMAssay Description:Inhibition of JAK1/TYK2 in human whole blood assessed as inhibition of IFN-alpha-induced STAT-3 phosphorylation preincubated for 45 mins followed by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  298nMAssay Description:Inhibition of JAK1/JAK2/TYK2 in human whole blood assessed as inhibition of IL-6-induced STAT-1 phosphorylation preincubated for 45 mins followed by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetTyrosine-protein kinase JAK3(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  487nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  677nMAssay Description:Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincub...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank
PDB3D3D Structure (crystal)

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  818nMAssay Description:Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-23-induced STAT-3 phosphorylation preincubated for 45 mins followed by IL-2...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  1.09E+3nMAssay Description:Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-12-induced STAT-4 phosphorylation preincubated for 45 mins followed by IL-1...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetJAK3/JAK1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  1.85E+3nMAssay Description:Inhibition of JAK1/JAK3 in human whole blood assessed as inhibition of IL-15-induced STAT-5 phosphorylation preincubated for 45 mins followed by IL-1...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetcGMP-dependent protein kinase 1(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PRKG1 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for IKK-alpha kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetDeath-associated protein kinase 1(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd:  72nMAssay Description:Binding constant for DAPK1 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetInsulin receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for INSR kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCalcium/calmodulin-dependent protein kinase kinase 2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CAMKK2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMast/stem cell growth factor receptor Kit(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for KIT kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCyclin-dependent kinase 11A(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CDC2L2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEpidermal growth factor receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(S752-I759del) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for ABL1(T315I)-phosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMitogen-activated protein kinase kinase kinase 4(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MAP3K4 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd:  9.50E+3nMAssay Description:Binding constant for ABL1(F317L)-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetHepatocyte growth factor receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MET kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047Y) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEpidermal growth factor receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(L858R,T790M) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEpidermal growth factor receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for FLT3(K663Q) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEphrin type-A receptor 6(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EPHA6 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetRho-associated protein kinase 2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd:  52nMAssay Description:Binding constant for ROCK2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetLeucine-rich repeat serine/threonine-protein kinase 2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd:  290nMAssay Description:Binding constant for LRRK2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for FLT3(ITD) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase JAK1(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for JAK1(JH2domain-pseudokinase) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank


TargetMast/stem cell growth factor receptor Kit(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for KIT(V559D,V654A) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd:  190nMAssay Description:Binding constant for RET(V804M) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEpidermal growth factor receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(L747-E749del, A750P) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for FLT3(N841I) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

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