BDBM246868 US10053465, 7::US10065963, Compound 7::US10125150, Example 7::US10336759, # 7::US10479803, Example 7::US10519163, Example 7::US10675284, Example 7::US10875847, Compound INCB39110::US11084822, Example 7::US11130767, # 7::US11136326, Example 7::US11285140, Example 364::US11304949, Compound 1::US11324749, Comp. No. 1::US11406640, Comp. No. 1::US11596632, Comp. No. 1::US11918581, Compound 1::US11957661, Compound 4::US11992490, Compound 1::US12226418, Example 7::US12268667, Compound 4::US20240058343, Compound 1::US20240307353, Compound 4::US9732097, Example 7::US9999619, Example 364::{1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl] piperidin-4- yl}-3-[4-(7H- pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1- yl]azetidin-3- yl}acetonitrile

SMILES Fc1c(ccnc1C(F)(F)F)C(=O)N1CCC(CC1)N1CC(CC#N)(C1)n1cc(cn1)-c1ncnc2[nH]ccc12

InChI Key InChIKey=KTBSXLIQKWEBRB-UHFFFAOYSA-N

Data  75 IC50  5 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 80 hits for monomerid = 246868   

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 5nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders were tested for inhibitory activity of JAK targe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2024
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders were tested for inhibitory activity of JAK targe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/16/2025
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK target...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2023
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:JAK1 inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK targets accord...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2024
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 2nMAssay 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 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:Selective JAK1 inhibitors that can be used in combination with an immunomodulatory agent and steroid for the treatment of hematological diseases or d...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:JAK1 pathway inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK target...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/28/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:JAK1 inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK targets accord...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/31/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2 [828-1132](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 75nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:Selective JAK1 inhibitors that can be used in combination with a ROCK inhibitor as described herein are tested for inhibitory activity of JAK targets...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2024
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2 [828-1132](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 75nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 5nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2 [828-1132](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 75nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 5nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2 [828-1132](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 100nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 5nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase receptor TYRO3(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 3.00E+3nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase receptor UFO(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 500nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase Mer(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 500nMAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataKd:  26nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 488nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataKd:  11nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 4.10E+3nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 1.08E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 54nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 3.40nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataKd:  385nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataKd:  324nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:The IC50s obtained by the method of Assay A at 1 mM ATP as described in the US Patent Publications.More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataKd:  51nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2025
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 1.00E+3nMAssay Description:The catalytic activity of JAK1, JAK2 or JAK3 was assayed by measuring the phosphorylation of a biotinylated peptide. The phosphorylated peptide was d...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/17/2025
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:JAK1 inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK targets accord...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/16/2025
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:JAK1 inhibitors that can be used for the treatment of cytokine-related diseases or disorders are tested for inhibitory activity of JAK targets accord...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2024
Entry Details
Go to US Patent

TargetNon-receptor tyrosine-protein kinase TYK2(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 795nMAssay Description:Inhibition of TYK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 2nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Tampere University

Curated by ChEMBL
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 63nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetTyrosine-protein kinase Mer(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 500nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2 [828-1132](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 25nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/11/2020
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/11/2020
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2 [828-1132](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 25nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/11/2020
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/11/2020
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK2 [828-1132](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 25nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/11/2020
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1 [837-1142](Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:Compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., Analytical Bi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/11/2020
Entry Details
Go to US Patent

TargetTyrosine-protein kinase JAK1(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 10nMAssay Description:The kinase reaction was conducted in clear-bottom 96-well plate from Thermo Fisher Scientific in a final volume of 24 μL. Inhibitors were first ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase receptor TYRO3(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 3.00E+3nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
Go to US Patent

TargetTyrosine-protein kinase receptor UFO(Human)
Incyte

US Patent
LigandPNGBDBM246868({1-{1-[3-Fluoro-2- (trifluoromethyl) isonicotinoyl...)
Affinity DataIC50: 500nMT: 2°CAssay Description:The kinase assay buffer contained 50 mM HEPES, pH7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% NP-40 and 2 mM DTT. 0.1 ul test compounds dissolved in DMSO were ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
Go to US Patent

Displayed 1 to 50 (of 80 total ) | Next | Last >>