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Compile Data Set for Download or QSAR

Found 27 hits Enz. Inhib. hit(s) with Target = 'Tyrosine-protein kinase JAK3' and Ligand = 'BDBM209866'   
Target/Host
(Institution)
LigandTarget/Host
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
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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6.31n/an/an/an/an/an/a7.5n/a



Pfizer Worldwide R&D



Assay Description
Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...


ACS Chem Biol 11: 3442-3451 (2016)


Article DOI: 10.1021/acschembio.6b00677
BindingDB Entry DOI: 10.7270/Q2PN94F8
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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6.31E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system by KT2...


J Med Chem 60: 1971-1993 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01694
BindingDB Entry DOI: 10.7270/Q2TX3JC2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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US Patent
n/an/a 0.300n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half log dilution series was created in DMSO...


US Patent US9617258 (2017)


BindingDB Entry DOI: 10.7270/Q2JD4ZWG
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 0.300n/an/an/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of human recombinant GST tagged JAK3 kinase domain (781 to 1124 amino acids) expressed in insect cells in presence of ATP


Bioorg Med Chem Lett 29: 2034-2041 (2019)


Article DOI: 10.1016/j.bmcl.2019.06.042
BindingDB Entry DOI: 10.7270/Q2H70KB6
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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TBA

Assay Description
JAK Caliper Enzyme Assay at 4 μM: Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half ...


Citation and Details

BindingDB Entry DOI: 10.7270/Q29026XR
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 0.300n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...


J Med Chem 60: 1971-1993 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01694
BindingDB Entry DOI: 10.7270/Q2TX3JC2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 0.300n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of ATP at Km concentration by coupled PK...


J Med Chem 61: 10665-10699 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01308
BindingDB Entry DOI: 10.7270/Q25T3P53
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 0.346n/an/an/an/a7.425



Pfizer Worldwide R&D



Assay Description
Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...


ACS Chem Biol 11: 3442-3451 (2016)


Article DOI: 10.1021/acschembio.6b00677
BindingDB Entry DOI: 10.7270/Q2PN94F8
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 0.350n/an/an/an/an/an/a



Eberhard-Karls-University Tuebingen

Curated by ChEMBL


Assay Description
Inhibition of JAK3 (unknown origin)


Bioorg Med Chem Lett 27: 4229-4237 (2017)


Article DOI: 10.1016/j.bmcl.2017.07.079
BindingDB Entry DOI: 10.7270/Q27P91Z2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 0.400n/an/an/an/an/an/a



Peking University

Curated by ChEMBL


Assay Description
Inhibition of human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system in presence of 6 uM ATP by HTRF assa...


J Med Chem 62: 1054-1066 (2019)


Article DOI: 10.1021/acs.jmedchem.8b01823
BindingDB Entry DOI: 10.7270/Q20G3PFP
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 2.30n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00922
BindingDB Entry DOI: 10.7270/Q2H1361P
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 2.32n/an/an/an/an/an/a


TBA



Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 2.42n/an/an/an/an/an/a


TBA



Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 33n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of JAK3 (unknown origin)


J Med Chem 62: 8973-8995 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00444
BindingDB Entry DOI: 10.7270/Q2930XJS
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 33n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant human JAK3 assessed as phosphorylation level in presence of 1 mM ATP


Citation and Details

Article DOI: 10.1016/j.bmcl.2021.127862
BindingDB Entry DOI: 10.7270/Q21V5JNK
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 33n/an/an/an/an/an/a



China Pharmaceutical University

Curated by ChEMBL


Assay Description
Inhibition of JAK3 (unknown origin)


Bioorg Med Chem 27: 1646-1657 (2019)


Article DOI: 10.1016/j.bmc.2019.03.009
BindingDB Entry DOI: 10.7270/Q2PC35WG
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 33n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...


J Med Chem 60: 1971-1993 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01694
BindingDB Entry DOI: 10.7270/Q2TX3JC2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 33n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/...


J Med Chem 61: 10665-10699 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01308
BindingDB Entry DOI: 10.7270/Q25T3P53
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 33n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01467
BindingDB Entry DOI: 10.7270/Q24Q801K
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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US Patent
n/an/a 33.1n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half log dilution series was created in DMSO...


US Patent US9617258 (2017)


BindingDB Entry DOI: 10.7270/Q2JD4ZWG
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 33.1n/an/an/an/a7.425



Pfizer Worldwide R&D



Assay Description
Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...


ACS Chem Biol 11: 3442-3451 (2016)


Article DOI: 10.1021/acschembio.6b00677
BindingDB Entry DOI: 10.7270/Q2PN94F8
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 33.1n/an/an/an/an/an/a


TBA

Assay Description
JAK Caliper Enzyme Assay at 1 mM ATP: Test article was solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. An 11-point half l...


Citation and Details

BindingDB Entry DOI: 10.7270/Q29026XR
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 51n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of JAK3 in human PBMC assessed as inhibition of IL-15 induced STAT5 phosphorylation preincubated for 75 mins followed by IL-15 addition an...


J Med Chem 60: 1971-1993 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01694
BindingDB Entry DOI: 10.7270/Q2TX3JC2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 90n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system in pre...


J Med Chem 60: 1971-1993 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01694
BindingDB Entry DOI: 10.7270/Q2TX3JC2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 106n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of JAK3 in human whole blood assessed as free drug concentration required for inhibition of IL-15 induced STAT5 phosphorylation preincubat...


J Med Chem 60: 1971-1993 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01694
BindingDB Entry DOI: 10.7270/Q2TX3JC2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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n/an/a 197n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of JAK3 in human whole blood assessed as inhibition of IL-15 induced STAT5 phosphorylation preincubated for 45 mins followed by IL-15 addi...


J Med Chem 60: 1971-1993 (2017)


Article DOI: 10.1021/acs.jmedchem.6b01694
BindingDB Entry DOI: 10.7270/Q2TX3JC2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase JAK3


(Homo sapiens (Human))
BDBM209866
PNG
(PF-06651600 | US11111242, Example 5 | US2023034848...)
Show SMILES C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
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antibodypedia
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UniChem
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n/an/a 202n/an/an/an/an/an/a



Peking University

Curated by ChEMBL


Assay Description
Inhibition of human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system in presence of 1 mM ATP by HTRF assa...


J Med Chem 62: 1054-1066 (2019)


Article DOI: 10.1021/acs.jmedchem.8b01823
BindingDB Entry DOI: 10.7270/Q20G3PFP
More data for this
Ligand-Target Pair