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

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

InChI Key InChIKey=HFNKQEVNSGCOJV-OAHLLOKOSA-N

Data  12 KI  118 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
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 16 hits for monomerid = 50355501   

TargetTyrosine-protein kinase JAK1(Homo sapiens (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(Homo sapiens (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
TargetTyrosine-protein kinase JAK2(Homo sapiens (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
TargetTyrosine-protein kinase JAK1(Homo sapiens (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(Homo sapiens (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(Homo sapiens (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
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (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(Homo sapiens (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(Homo sapiens (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(Homo sapiens (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(Homo sapiens (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
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataEC50:  12nMAssay Description:Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins prior to EPO-induction measur...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataEC50:  24nMAssay Description:Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measur...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataEC50:  12nMAssay Description:Inhibition of JAK2 (unknown origin) assessed as inhibition of STAT5 phosphorylation by cell-based assayMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataEC50:  24nMAssay Description:Inhibition of JAK1 (unknown origin) assessed as inhibition of STAT3 phosphorylation by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  6.85nMAssay Description:Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPOMore data for this Ligand-Target Pair