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Found 1227 hits Enz. Inhib. hit(s) with Target = 'Non-receptor tyrosine-protein kinase TYK2'   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146027
PNG
(CHEMBL3763213)
Show SMILES CC(C)[C@H](C)n1cc(-c2cc(N3CCOCC3)n(C)n2)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C19H27N7O2/c1-11(2)12(3)26-10-13(17-16(19(26)27)18(20)22-21-17)14-9-15(24(4)23-14)25-5-7-28-8-6-25/h9-12H,5-8H2,1-4H3,(H3,20,21,22)/t12-/s2
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n/an/a 0.550n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a 0.600n/an/an/an/an/an/a



Southeast University

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin) incubated for 1 hr by spectrophotometric analysis


Bioorg Med Chem 24: 3483-93 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50355501
PNG
(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE)
Show SMILES N#CC[C@H](C1CCCC1)n1cc(cn1)-c1ncnc2[nH]ccc12
Show 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
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n/an/a 0.720n/an/an/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin)


Bioorg Med Chem Lett 26: 1803-8 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146030
PNG
(CHEMBL3763991)
Show SMILES CC(C)[C@H](C)n1cc(-c2ccc(cn2)N2CCOCC2)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C20H26N6O2/c1-12(2)13(3)26-11-15(18-17(20(26)27)19(21)24-23-18)16-5-4-14(10-22-16)25-6-8-28-9-7-25/h4-5,10-13H,6-9H2,1-3H3,(H3,21,23,24)/t13-/s2
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n/an/a 0.920n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146026
PNG
(CHEMBL3764277)
Show SMILES CC(C)[C@H](C)n1cc(-c2cc(C3CCOCC3)n(C)n2)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C20H28N6O2/c1-11(2)12(3)26-10-14(18-17(20(26)27)19(21)23-22-18)15-9-16(25(4)24-15)13-5-7-28-8-6-13/h9-13H,5-8H2,1-4H3,(H3,21,22,23)/t12-/s2
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n/an/a 0.980n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM26198
PNG
(4-tert-butyl-15-fluoro-3,5,10-triazatetracyclo[11....)
Show SMILES CC(C)(C)c1nc2c([nH]1)c1ccc(F)cc1c1c2cc[nH]c1=O
Show InChI InChI=1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
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n/an/a 1n/an/an/an/an/an/a



University of Oxford

Curated by ChEMBL


Assay Description
Inhibition of Tyk2


Citation and Details
Checked by Author
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
JAK2/TYK2


(Homo sapiens (Human))
BDBM26198
PNG
(4-tert-butyl-15-fluoro-3,5,10-triazatetracyclo[11....)
Show SMILES CC(C)(C)c1nc2c([nH]1)c1ccc(F)cc1c1c2cc[nH]c1=O
Show InChI InChI=1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
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n/an/a 1n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Inhibition of Tyrosine kinase 2 kinase


Bioorg Med Chem Lett 12: 1219-23 (2002)

More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
JAK2/TYK2


(Homo sapiens (Human))
BDBM239955
PNG
(US9403801, 14A | US9403801, 14B)
Show SMILES Cn1cc(Nc2ncc(Cl)c(NC3CCC4(CCN(C4)C(=O)CC#N)CC3)n2)cn1
Show InChI InChI=1S/C20H25ClN8O/c1-28-12-15(10-24-28)26-19-23-11-16(21)18(27-19)25-14-2-5-20(6-3-14)7-9-29(13-20)17(30)4-8-22/h10-12,14H,2-7,9,13H2,1H3,(H2,23,25,26,27)
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n/an/a 1n/an/an/an/an/an/a



CALITOR SCIENCES, LLC; SUNSHINE LAKE PHARMA CO., LTD.

US Patent


Assay Description
TYK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM GGMEDIYFEFMGGKKK, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx...


US Patent US9403801 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146025
PNG
(CHEMBL3765517)
Show SMILES CC(C)[C@H](C)n1cc(-c2cc(N3CCS(=O)(=O)CC3)n(C)n2)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C19H27N7O3S/c1-11(2)12(3)26-10-13(17-16(19(26)27)18(20)22-21-17)14-9-15(24(4)23-14)25-5-7-30(28,29)8-6-25/h9-12H,5-8H2,1-4H3,(H3,20,21,22)/t12-/s2
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n/an/a 1.20n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198268
PNG
(US9216999, 75)
Show SMILES ClC[C@H]1CC[C@@H](CC1)c1nnn2cnc3[nH]ccc3c12
Show InChI InChI=1/C14H16ClN5/c15-7-9-1-3-10(4-2-9)12-13-11-5-6-16-14(11)17-8-20(13)19-18-12/h5-6,8-10,16H,1-4,7H2/t9-,10-
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n/an/a 1.20n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50152595
PNG
(CHEMBL3780091)
Show SMILES N[C@H]1CC[C@H](CC1)Nc1cc[nH]c(=O)c1-c1nc2ccccc2[nH]1
Show InChI InChI=1/C18H21N5O/c19-11-5-7-12(8-6-11)21-15-9-10-20-18(24)16(15)17-22-13-3-1-2-4-14(13)23-17/h1-4,9-12H,5-8,19H2,(H,22,23)(H2,20,21,24)/t11-,12+
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n/an/a 1.5n/an/an/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin)


Bioorg Med Chem Lett 26: 1803-8 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146031
PNG
(CHEMBL3763252)
Show SMILES CC(C)C(C)n1cc(-c2ccc(cn2)N2CCOCC2)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C20H26N6O2/c1-12(2)13(3)26-11-15(18-17(20(26)27)19(21)24-23-18)16-5-4-14(10-22-16)25-6-8-28-9-7-25/h4-5,10-13H,6-9H2,1-3H3,(H3,21,23,24)
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n/an/a 1.5n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50122319
PNG
(CHEMBL3622150)
Show SMILES CCn1c(cc2c1nc(Nc1cc(C)[nH]n1)c1ncn(C)c21)C(=O)N(C1CC1)C1CC1
Show InChI InChI=1S/C22H26N8O/c1-4-29-16(22(31)30(13-5-6-13)14-7-8-14)10-15-19-18(23-11-28(19)3)20(25-21(15)29)24-17-9-12(2)26-27-17/h9-11,13-14H,4-8H2,1-3H3,(H2,24,25,26,27)
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n/an/a 1.90n/an/an/an/an/an/a



Bristol-Myers Squibb R&D

Curated by ChEMBL


Assay Description
Inhibition of recombinant TYK2 (unknown origin) by scintillation counting method


ACS Med Chem Lett 6: 850-5 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50035810
PNG
(CHEMBL3359927)
Show SMILES C[C@]1(F)CCC[C@H]1Nc1c(cnn2cccc12)C(N)=O
Show InChI InChI=1/C14H17FN4O/c1-14(15)6-2-5-11(14)18-12-9(13(16)20)8-17-19-7-3-4-10(12)19/h3-4,7-8,11,18H,2,5-6H2,1H3,(H2,16,20)/t11-,14+/s2
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n/an/a 2n/an/an/an/an/an/a



Bristol-Myers Squibb Company

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin) by caliper assay


Citation and Details
More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146024
PNG
(CHEMBL3765822)
Show SMILES CC(C)[C@@H](C)n1cc(-c2cc(n(C)n2)C(C)(C)O)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C18H26N6O2/c1-9(2)10(3)24-8-11(15-14(17(24)25)16(19)21-20-15)12-7-13(18(4,5)26)23(6)22-12/h7-10,26H,1-6H3,(H3,19,20,21)/t10-/s2
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n/an/a 2.10n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198294
PNG
(US9216999, 101)
Show SMILES Fc1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)cc1
Show InChI InChI=1/C21H23FN6/c22-17-7-3-15(4-8-17)12-23-11-14-1-5-16(6-2-14)19-20-18-9-10-24-21(18)25-13-28(20)27-26-19/h3-4,7-10,13-14,16,23-24H,1-2,5-6,11-12H2/t14-,16-
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n/an/a 2.30n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198267
PNG
(US9216999, 74)
Show SMILES BrC[C@H]1CC[C@@H](CC1)c1nnn2cnc3[nH]ccc3c12
Show InChI InChI=1/C14H16BrN5/c15-7-9-1-3-10(4-2-9)12-13-11-5-6-16-14(11)17-8-20(13)19-18-12/h5-6,8-10,16H,1-4,7H2/t9-,10-
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n/an/a 2.60n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198291
PNG
(US9216999, 98)
Show SMILES FC(F)(F)c1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)cc1
Show InChI InChI=1/C22H23F3N6/c23-22(24,25)17-7-3-15(4-8-17)12-26-11-14-1-5-16(6-2-14)19-20-18-9-10-27-21(18)28-13-31(20)30-29-19/h3-4,7-10,13-14,16,26-27H,1-2,5-6,11-12H2/t14-,16-
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n/an/a 2.60n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198376
PNG
(US9216999, 177)
Show SMILES Clc1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)cc1
Show InChI InChI=1/C21H23ClN6/c22-17-7-3-15(4-8-17)12-23-11-14-1-5-16(6-2-14)19-20-18-9-10-24-21(18)25-13-28(20)27-26-19/h3-4,7-10,13-14,16,23-24H,1-2,5-6,11-12H2/t14-,16-
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n/an/a 2.80n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM130257
PNG
(US8815840, 17)
Show SMILES CN1CCN(CC1)C(=O)c1ccc2[nH]c3c(cc(cc3c2c1)-c1ccc(Cl)cc1)C(N)=O
Show InChI InChI=1S/C25H23ClN4O2/c1-29-8-10-30(11-9-29)25(32)16-4-7-22-19(12-16)20-13-17(15-2-5-18(26)6-3-15)14-21(24(27)31)23(20)28-22/h2-7,12-14,28H,8-11H2,1H3,(H2,27,31)
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n/an/a 2.80n/an/an/an/an/an/a



Bristol-Myers Squibb Co.

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198643
PNG
(US9216999, 435b)
Show SMILES N#CC[C@H]1CC[C@@H](CC1)c1nnn2cnc3[nH]ccc3c12
Show InChI InChI=1/C15H16N6/c16-7-5-10-1-3-11(4-2-10)13-14-12-6-8-17-15(12)18-9-21(14)20-19-13/h6,8-11,17H,1-5H2/t10-,11-
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n/an/a 2.90n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198305
PNG
(US9216999, 112)
Show SMILES Fc1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)cc1C(F)(F)F
Show InChI InChI=1/C22H22F4N6/c23-18-6-3-14(9-17(18)22(24,25)26)11-27-10-13-1-4-15(5-2-13)19-20-16-7-8-28-21(16)29-12-32(20)31-30-19/h3,6-9,12-13,15,27-28H,1-2,4-5,10-11H2/t13-,15-
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n/an/a 3.30n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198299
PNG
(US9216999, 106)
Show SMILES Cc1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)s1
Show InChI InChI=1/C20H24N6S/c1-13-2-7-16(27-13)11-21-10-14-3-5-15(6-4-14)18-19-17-8-9-22-20(17)23-12-26(19)25-24-18/h2,7-9,12,14-15,21-22H,3-6,10-11H2,1H3/t14-,15-
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n/an/a 3.60n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM239963
PNG
(US9403801, 28)
Show SMILES CC(=O)N1CCC2(CCC(CC2)Nc2nc(Nc3cnn(C)c3)ncc2Cl)CC1
Show InChI InChI=1S/C20H28ClN7O/c1-14(29)28-9-7-20(8-10-28)5-3-15(4-6-20)24-18-17(21)12-22-19(26-18)25-16-11-23-27(2)13-16/h11-13,15H,3-10H2,1-2H3,(H2,22,24,25,26)
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n/an/a 4n/an/an/an/an/an/a



CALITOR SCIENCES, LLC; SUNSHINE LAKE PHARMA CO., LTD.

US Patent


Assay Description
TYK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM GGMEDIYFEFMGGKKK, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx...


US Patent US9403801 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198473
PNG
(US9216999, 270)
Show SMILES COc1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)cc1
Show InChI InChI=1/C22H26N6O/c1-29-18-8-4-16(5-9-18)13-23-12-15-2-6-17(7-3-15)20-21-19-10-11-24-22(19)25-14-28(21)27-26-20/h4-5,8-11,14-15,17,23-24H,2-3,6-7,12-13H2,1H3/t15-,17-
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n/an/a 4.80n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50124208
PNG
(ASP-015K | ASP015K | PEFICITINIB | Peficitinib)
Show SMILES NC(=O)c1cnc2[nH]ccc2c1N[C@H]1[C@H]2CC3C[C@@H]1C[C@](O)(C3)C2
Show InChI InChI=1/C18H22N4O2/c19-16(23)13-8-21-17-12(1-2-20-17)15(13)22-14-10-3-9-4-11(14)7-18(24,5-9)6-10/h1-2,8-11,14,24H,3-7H2,(H2,19,23)(H2,20,21,22)/t9?,10-,11+,14-,18-
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n/an/a 4.80n/an/an/an/an/an/a



Konkuk University

Curated by ChEMBL


Assay Description
Inhibition of Tyk2 (unknown origin)


J Med Chem 58: 7596-602 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198303
PNG
(US9216999, 110)
Show SMILES FC(F)(F)Oc1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)cc1
Show InChI InChI=1/C22H23F3N6O/c23-22(24,25)32-17-7-3-15(4-8-17)12-26-11-14-1-5-16(6-2-14)19-20-18-9-10-27-21(18)28-13-31(20)30-29-19/h3-4,7-10,13-14,16,26-27H,1-2,5-6,11-12H2/t14-,16-
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n/an/a 4.90n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50084464
PNG
(CHEMBL3426891)
Show SMILES CN1CCN(CC1)c1ccc(Nc2ncc(Cl)c(NC[C@H]3CCCO3)n2)cc1
Show InChI InChI=1/C20H27ClN6O/c1-26-8-10-27(11-9-26)16-6-4-15(5-7-16)24-20-23-14-18(21)19(25-20)22-13-17-3-2-12-28-17/h4-7,14,17H,2-3,8-13H2,1H3,(H2,22,23,24,25)/t17-/s2
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n/an/a 5n/an/an/an/an/an/a



University of South Florida

Curated by ChEMBL


Assay Description
Inhibition of human TYK2 using KKSRGDYMTMQIG peptide substrate by 33P Hotspot assay


Citation and Details
More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50109821
PNG
(CHEBI:87103 | CHEMBL21156)
Show SMILES CC(C)(C)c1nc2c([nH]1)c1cc[nH]c(=O)c1c1cc(F)ccc21
Show InChI InChI=1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
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n/an/a 5n/an/an/an/an/an/a



Konkuk University

Curated by ChEMBL


Assay Description
Inhibition of Tyk2 (unknown origin) using 25 uM of ATP and Tyr3 peptide by Z'-LYTE kinase assay


J Med Chem 58: 7596-602 (2015)

More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146028
PNG
(CHEMBL3764030)
Show SMILES CC(C)[C@H](C)n1cc(-c2ccn(C)n2)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C15H20N6O/c1-8(2)9(3)21-7-10(11-5-6-20(4)19-11)13-12(15(21)22)14(16)18-17-13/h5-9H,1-4H3,(H3,16,17,18)/t9-/s2
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n/an/a 5.5n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198392
PNG
(US9216999, 193)
Show SMILES C(NCc1ccccc1)[C@H]1CC[C@@H](CC1)c1nnn2cnc3[nH]ccc3c12
Show InChI InChI=1/C21H24N6/c1-2-4-15(5-3-1)12-22-13-16-6-8-17(9-7-16)19-20-18-10-11-23-21(18)24-14-27(20)26-25-19/h1-5,10-11,14,16-17,22-23H,6-9,12-13H2/t16-,17-
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n/an/a 5.5n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198286
PNG
(US9216999, 93)
Show SMILES N#Cc1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)cc1
Show InChI InChI=1/C22H23N7/c23-11-15-1-3-16(4-2-15)12-24-13-17-5-7-18(8-6-17)20-21-19-9-10-25-22(19)26-14-29(21)28-27-20/h1-4,9-10,14,17-18,24-25H,5-8,12-13H2/t17-,18-
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n/an/a 5.90n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50035837
PNG
(CHEMBL3359926)
Show SMILES C[C@@]1(CCC[C@H]1Nc1c(cnn2cccc12)C(N)=O)C#N
Show InChI InChI=1/C15H17N5O/c1-15(9-16)6-2-5-12(15)19-13-10(14(17)21)8-18-20-7-3-4-11(13)20/h3-4,7-8,12,19H,2,5-6H2,1H3,(H2,17,21)/t12-,15-/s2
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n/an/a 6n/an/an/an/an/an/a



Bristol-Myers Squibb Company

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin) by caliper assay


Citation and Details
More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146035
PNG
(CHEMBL3764637)
Show SMILES CC(C)C(C)n1cc(-c2ccn(C)n2)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C15H20N6O/c1-8(2)9(3)21-7-10(11-5-6-20(4)19-11)13-12(15(21)22)14(16)18-17-13/h5-9H,1-4H3,(H3,16,17,18)
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n/an/a 6.30n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146071
PNG
(CHEMBL3764463)
Show SMILES Nc1n[nH]c2c(cn(-c3ccccc3Cl)c(=O)c12)-c1ccccn1
Show InChI InChI=1S/C17H12ClN5O/c18-11-5-1-2-7-13(11)23-9-10(12-6-3-4-8-20-12)15-14(17(23)24)16(19)22-21-15/h1-9H,(H3,19,21,22)
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n/an/a 6.70n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM239953
PNG
(US9403801, 12)
Show SMILES Cn1cc(Nc2ncc(Cl)c(NC3CC4CN(CC4C3)C(=O)CC#N)n2)cn1
Show InChI InChI=1/C18H21ClN8O/c1-26-10-14(6-22-26)24-18-21-7-15(19)17(25-18)23-13-4-11-8-27(9-12(11)5-13)16(28)2-3-20/h6-7,10-13H,2,4-5,8-9H2,1H3,(H2,21,23,24,25)
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n/an/a 7n/an/an/an/an/an/a



CALITOR SCIENCES, LLC; SUNSHINE LAKE PHARMA CO., LTD.

US Patent


Assay Description
TYK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM GGMEDIYFEFMGGKKK, 10 mM MgAcetate and [γ-33P-ATP](specific activity approx...


US Patent US9403801 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50152601
PNG
(CHEMBL3780467)
Show SMILES COC(=O)C1CCc2[nH]c(nc2C1)-c1c(N[C@@H]2CC[C@H](N)CC2)cc[nH]c1=O
Show InChI InChI=1/C20H27N5O3/c1-28-20(27)11-2-7-14-16(10-11)25-18(24-14)17-15(8-9-22-19(17)26)23-13-5-3-12(21)4-6-13/h8-9,11-13H,2-7,10,21H2,1H3,(H,24,25)(H2,22,23,26)/t11?,12-,13+
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n/an/a 7n/an/an/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin)


Bioorg Med Chem Lett 26: 1803-8 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50035849
PNG
(CHEMBL3359915)
Show SMILES C[C@@]1(O)CC[C@@H](Nc2c(cnn3cccc23)C(N)=O)C1(C)C
Show InChI InChI=1/C16H22N4O2/c1-15(2)12(6-7-16(15,3)22)19-13-10(14(17)21)9-18-20-8-4-5-11(13)20/h4-5,8-9,12,19,22H,6-7H2,1-3H3,(H2,17,21)/t12-,16-/s2
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n/an/a 7n/an/an/an/an/an/a



Bristol-Myers Squibb Company

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin) by caliper assay


Citation and Details
More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM26198
PNG
(4-tert-butyl-15-fluoro-3,5,10-triazatetracyclo[11....)
Show SMILES CC(C)(C)c1nc2c([nH]1)c1ccc(F)cc1c1c2cc[nH]c1=O
Show InChI InChI=1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
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n/an/a 7n/an/an/an/a7.530



University of Luxembourg



Assay Description
Enzyme assay affinity-purified GST fusions of the active kinase domains (GST-Jak1(866-1154), GST-Jak2(808-1132), GST-Jak3(811-1124) and GST-Tyk2(888-...


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
JAK2/TYK2


(Homo sapiens (Human))
BDBM50355403
PNG
(CHEMBL261386)
Show SMILES Fc1ccc2c3[nH]c(nc3c3cc[nH]c(=O)c3c2c1)-c1ccccc1Cl
Show InChI InChI=1S/C20H11ClFN3O/c21-15-4-2-1-3-12(15)19-24-17-11-6-5-10(22)9-14(11)16-13(18(17)25-19)7-8-23-20(16)26/h1-9H,(H,23,26)(H,24,25)
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n/an/a 7n/an/an/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Inhibition of TYK2


Citation and Details
More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198570
PNG
(US9216999, 367)
Show SMILES IC[C@H]1CC[C@@H](CC1)c1nnn2cnc3[nH]ccc3c12
Show InChI InChI=1/C14H16IN5/c15-7-9-1-3-10(4-2-9)12-13-11-5-6-16-14(11)17-8-20(13)19-18-12/h5-6,8-10,16H,1-4,7H2/t9-,10-
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n/an/a 7.30n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50035842
PNG
(CHEMBL3359908)
Show SMILES CC1(C)CCC[C@H]1Nc1c(cnn2cccc12)C(N)=O
Show InChI InChI=1/C15H20N4O/c1-15(2)7-3-6-12(15)18-13-10(14(16)20)9-17-19-8-4-5-11(13)19/h4-5,8-9,12,18H,3,6-7H2,1-2H3,(H2,16,20)/t12-/s2
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n/an/a 8n/an/an/an/an/an/a



Bristol-Myers Squibb Company

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin) by caliper assay


Citation and Details
More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50021656
PNG
(BARICITINIB | INCB-028050 | LY-3009104)
Show SMILES CCS(=O)(=O)N1CC(CC#N)(C1)n1cc(cn1)-c1ncnc2[nH]ccc12
Show InChI InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)
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n/an/a 8.70n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198306
PNG
(US9216999, 113)
Show SMILES CS(=O)(=O)c1ccc(CNC[C@H]2CC[C@@H](CC2)c2nnn3cnc4[nH]ccc4c23)cc1
Show InChI InChI=1/C22H26N6O2S/c1-31(29,30)18-8-4-16(5-9-18)13-23-12-15-2-6-17(7-3-15)20-21-19-10-11-24-22(19)25-14-28(21)27-26-20/h4-5,8-11,14-15,17,23-24H,2-3,6-7,12-13H2,1H3/t15-,17-
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n/an/a 8.70n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50193995
PNG
(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Show SMILES C[C@@H]1CCN(C[C@@H]1N(C)c1ncnc2[nH]ccc12)C(=O)CC#N
Show InChI InChI=1S/C16H20N6O/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20)/t11-,13+/m1/s1
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n/an/a 8.90n/an/an/an/an/an/a



Eberhard-Karls-University Tuebingen



Assay Description
A commercial assay by Reaction Biology Corp.


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
JAK2/TYK2


(Homo sapiens (Human))
BDBM50152596
PNG
(CHEMBL3781427)
Show SMILES O=c1[nH]ccc(NC2CCOCC2)c1-c1nc2ccccc2[nH]1
Show InChI InChI=1S/C17H18N4O2/c22-17-15(16-20-12-3-1-2-4-13(12)21-16)14(5-8-18-17)19-11-6-9-23-10-7-11/h1-5,8,11H,6-7,9-10H2,(H,20,21)(H2,18,19,22)
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n/an/a 9n/an/an/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Inhibition of TYK2 (unknown origin)


Bioorg Med Chem Lett 26: 1803-8 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198572
PNG
(US9216999, 369)
Show SMILES [N-]=[N]=NC[C@H]1CC[C@@H](CC1)c1nnn2cnc3[nH]ccc3c12
Show InChI InChI=1/C14H16N8/c15-20-18-7-9-1-3-10(4-2-9)12-13-11-5-6-16-14(11)17-8-22(13)21-19-12/h5-6,8-10,16H,1-4,7H2/q-1/t9-,10-
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n/an/a 9.20n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146029
PNG
(CHEMBL3764383)
Show SMILES CC(C)[C@@H](C)n1cc(-c2ccc(cn2)N2CCOCC2)c2[nH]nc(N)c2c1=O
Show InChI InChI=1/C20H26N6O2/c1-12(2)13(3)26-11-15(18-17(20(26)27)19(21)24-23-18)16-5-4-14(10-22-16)25-6-8-28-9-7-25/h4-5,10-13H,6-9H2,1-3H3,(H3,21,23,24)/t13-/s2
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n/an/a 9.70n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM198269
PNG
(US9216999, 76)
Show SMILES SC[C@H]1CC[C@@H](CC1)c1nnn2cnc3[nH]ccc3c12
Show InChI InChI=1/C14H17N5S/c20-7-9-1-3-10(4-2-9)12-13-11-5-6-15-14(11)16-8-19(13)18-17-12/h5-6,8-10,15,20H,1-4,7H2/t9-,10-
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n/an/a 9.70n/an/an/an/a7.5n/a



Nissan Chemical Industries, Ltd.

US Patent


Assay Description
JAK1, JAK2, JAK3 and Tyk2 were purchased from Carna Biosciences, Inc. As the substrate, LANCE Ultra ULight-JAK1 Peptide (manufactured by PerkinElmer ...


US Patent US9216999 (2015)

More data for this
Ligand-Target Pair
JAK2/TYK2


(Homo sapiens (Human))
BDBM50146072
PNG
(CHEMBL3765131)
Show SMILES Cn1ccc(n1)-c1cn(-c2ccccc2Cl)c(=O)c2c(N)n[nH]c12
Show InChI InChI=1S/C16H13ClN6O/c1-22-7-6-11(21-22)9-8-23(12-5-3-2-4-10(12)17)16(24)13-14(9)19-20-15(13)18/h2-8H,1H3,(H3,18,19,20)
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n/an/a 9.90n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent sub...


J Med Chem 59: 733-49 (2016)

More data for this
Ligand-Target Pair
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