BDBM103727 US10112907, Example 00033::US10206907, Compound 200::US10708263, Compound 1::US10766894, Compound TABLE 1.18::US10919890, Compound 1::US10961228, Example Filgotinib::US11000528, Cpd # 1::US11203595, TABLE 1.18::US11279699, Compound Filgotinib::US8563545, 1

SMILES O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1

InChI Key InChIKey=RIJLVEAXPNLDTC-UHFFFAOYSA-N

Data  117 IC50  1 Kd

  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 180 hits for monomerid = 103727   

LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD4+ T cells preincubated with compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 10nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 10nMAssay Description:Inhibition of recombinant JAK1 (unknown origin) in the presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 10nMAssay Description:Inhibition of JAK 1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 10nMAssay Description:Inhibition of recombinant human JAK1 using ULight-JAK-1(Tyr1023) peptide as substrate assessed as incorporation of phosphate into the substrate prein...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 10nMAssay Description:Inhibition of human recombinant JAK1 incubated for 60 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 10nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 10nMAssay Description:Inhibition of human recombinant JAK1More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/12/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataKd:  11nMAssay Description:Binding affinity to human recombinant JAK1 assessed as dissociation constant by Cheng-Prusoff equation analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 17nMAssay Description:Inhibition of recombinant JAK1 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr by TR-FRET Lanthascreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 25nMAssay Description:Inhibition of human recombinant JAK2 incubated for 60 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 25nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 26nMAssay Description:Inhibition of recombinant JAK1 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measure...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 28nMAssay Description:Inhibition of recombinant JAK2 (unknown origin) in the presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 28nMAssay Description:Inhibition of recombinant human JAK2 using ULight-JAK-1(Tyr1023) peptide as substrate assessed as incorporation of phosphate into the substrate prein...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 28nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 28nMAssay Description:Inhibition of JAK 2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetJak1 protein(Rat)
Galapagos

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 29nMAssay Description:Inhibition of rat JAK1More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/12/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 31.4nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetTyrosine-protein kinase JAK2 [808-1132](Human)
Alfasigma

US Patent
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 31.4nMAssay Description:Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) is purchased from Invitrogen. 0.025 mU of JAK2 is incubated wit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2026
Entry Details
US Patent

TargetTyrosine-protein kinase JAK2 [808-1132](Human)
Alfasigma

US Patent
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 31.4nMAssay Description:Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) was purchased from Invitrogen. 0.025 mU of JAK2 was incubated w...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/8/2021
Entry Details
US Patent

TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataKd:  32nMAssay Description:Binding affinity to human recombinant JAK2 assessed as dissociation constant by Cheng-Prusoff equation analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 33nMAssay Description:Inhibition of recombinant human JAK1 using MGEEPLYWSFPAKKK as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 41.2nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 46nMAssay Description:The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/10/2022
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 47.1nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1 [850-1154]()
Alfasigma

US Patent
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 47.1nMAssay Description:Recombinant human JAK1 catalytic domain (amino acids 850-1154; catalog number 08-144) is purchased from Carna Biosciences. 10 ng of JAK1 is incubated...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2026
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1 [850-1154]()
Alfasigma

US Patent
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 47.1nMAssay Description:Recombinant human JAK1 catalytic domain (amino acids 850-1154; catalog number 08-144) was purchased from Carna Biosciences. 10 ng of JAK1 was incubat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/8/2021
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 48.3nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1 [866-1154](Human)
Novartis

US Patent
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 50nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/29/2022
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1 [866-1154](Human)
Novartis

US Patent
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 50nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2019
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 50nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/26/2021
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1 [850-1154](Human)
Galapagos

US Patent
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 50nMAssay Description:JAK1 (IC50): Recombinant human JAK1 catalytic domain (amino acids 850-1154; catalog number 08-144) is purchased from Carna Biosciences. 10 ng of JAK1...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/8/2021
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 50.1nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 50.3nMAssay Description:Recombinant human JAK1 catalytic domain (amino acids 850-1154; catalog number 08-144) is purchased from Carna Biosciences. 10 ng of JAK1 is incubated...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2021
Entry Details
US Patent

TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 55nMAssay Description:The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/10/2022
Entry Details
US Patent

TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 55.5nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetTyrosine-protein kinase JAK1(Human)
Konkuk University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 55.7nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 65nMAssay Description:Inhibition of recombinant TYK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measure...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 72.7nMAssay Description:Recombinant human TYK2 catalytic domain (amino acids 871-1187; catalog number 08-147) was purchased from Carna biosciences. 5 ng of TYK2 was incubate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/8/2021
Entry Details
US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 72.7nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 72.7nMAssay Description:Recombinant human TYK2 catalytic domain (amino acids 871-1187; catalog number 08-147) is purchased from Carna biosciences. 5 ng of TYK2 is incubated ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2026
Entry Details
US Patent

TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 73.4nMAssay Description:Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) is purchased from Invitrogen. 0.025 mU of JAK2 is incubated wit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2021
Entry Details
US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 73.8nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetTyrosine-protein kinase JAK2(Human)
Galapagos NV

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 74nMAssay Description:Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2 [808-1132](Human)
Galapagos

US Patent
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 74nMAssay Description:JAK1 (KI): For the determination of Ki, different amounts of compound are mixed with the enzyme and the enzymatic reaction is followed as a function ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/8/2021
Entry Details
US Patent

LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 78nMAssay Description:JAK2 (Kd): JAK2 (Invitrogen, PV4210) is used at a final concentration of 5 nM. The binding experiment is performed in 50 mM Hepes pH 7.5, 0.01% Brij-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/8/2021
Entry Details
US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 78nMAssay Description:Recombinant human TYK2 catalytic domain (amino acids 871-1187; catalog number 08-147) is purchased from Carna biosciences. 5 ng of TYK2 is incubated ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2021
Entry Details
US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 79.1nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM103727(US8563545, 1 | US10112907, Example 00033 | US10206...)
Affinity DataIC50: 86.8nMAssay Description:In vitro inhibition assay using various enzyme.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/14/2014
Entry Details
US Patent

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