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Patent code US10858364

Compile Data Set for Download or QSAR
Found 15 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Tyrosine-protein kinase BTK


(Homo sapiens (Human))
BDBM474107
PNG
(Pazopanib metabolite M27 | US10858364, Compound M2...)
Show SMILES Cc1n(C)nc2cc(Nc3ccnc(Nc4ccc(C)c(c4)S(N)(=O)=O)n3)ccc12
Show InChI InChI=1S/C20H21N7O2S/c1-12-4-5-15(11-18(12)30(21,28)29)24-20-22-9-8-19(25-20)23-14-6-7-16-13(2)27(3)26-17(16)10-14/h4-11H,1-3H3,(H2,21,28,29)(H2,22,23,24,25)
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188n/an/an/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
Inhibitory activity on BTK wild type (BTK-WT) and BTK Cys481Ser mutant (BTK-C481S) was measured using the LanthaScreen assay technology from ThermoFi...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase BTK


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a 5n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
TBDBTK enzyme (His-BTK (Millipore catalog #14-552)), is diluted to 0.4 U/mL in KR buffer (10 mM Tris-HCl, 10 mM MgCl2, 0.01% Tween-20, 0.05% NaN3, 1 ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase BTK


(Homo sapiens (Human))
BDBM474106
PNG
(US10858364, Formula (II))
Show SMILES COc1cc(ccc1C(=O)Nc1ccccn1)-c1nc(C(=O)CCCNC(=O)C#CC)n2ccnc(N)c12
Show InChI InChI=1S/C27H25N7O4/c1-3-7-22(36)30-13-6-8-19(35)26-33-23(24-25(28)31-14-15-34(24)26)17-10-11-18(20(16-17)38-2)27(37)32-21-9-4-5-12-29-21/h4-5,9-12,14-16H,6,8,13H2,1-2H3,(H2,28,31)(H,30,36)(H,29,32,37)
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n/an/a 9.30n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
TBDBTK enzyme (His-BTK (Millipore catalog #14-552)), is diluted to 0.4 U/mL in KR buffer (10 mM Tris-HCl, 10 mM MgCl2, 0.01% Tween-20, 0.05% NaN3, 1 ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Cytoplasmic tyrosine-protein kinase BMX


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a 15n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
BMX, TXK, EGFR, ERBB2, ERBB4, JAK3, BLK kinase activity was measured using the Z′-LYTE assay at Thermo Fisher. A 10-point dose response (final ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase BTK


(Homo sapiens (Human))
BDBM474107
PNG
(Pazopanib metabolite M27 | US10858364, Compound M2...)
Show SMILES Cc1n(C)nc2cc(Nc3ccnc(Nc4ccc(C)c(c4)S(N)(=O)=O)n3)ccc12
Show InChI InChI=1S/C20H21N7O2S/c1-12-4-5-15(11-18(12)30(21,28)29)24-20-22-9-8-19(25-20)23-14-6-7-16-13(2)27(3)26-17(16)10-14/h4-11H,1-3H3,(H2,21,28,29)(H2,22,23,24,25)
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n/an/a 39n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
Ramos B cells (ATCC, cat no. CRL-1923) were plated in 24-wells culture plates at 2106 cells per well in a total volume of 900 μL DMEMF12+10% FB...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase TXK


(Homo sapiens (Human))
BDBM474106
PNG
(US10858364, Formula (II))
Show SMILES COc1cc(ccc1C(=O)Nc1ccccn1)-c1nc(C(=O)CCCNC(=O)C#CC)n2ccnc(N)c12
Show InChI InChI=1S/C27H25N7O4/c1-3-7-22(36)30-13-6-8-19(35)26-33-23(24-25(28)31-14-15-34(24)26)17-10-11-18(20(16-17)38-2)27(37)32-21-9-4-5-12-29-21/h4-5,9-12,14-16H,6,8,13H2,1-2H3,(H2,28,31)(H,30,36)(H,29,32,37)
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n/an/a 59n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
BMX, TXK, EGFR, ERBB2, ERBB4, JAK3, BLK kinase activity was measured using the Z′-LYTE assay at Thermo Fisher. A 10-point dose response (final ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Receptor protein-tyrosine kinase erbB-4


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a 343n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
BMX, TXK, EGFR, ERBB2, ERBB4, JAK3, BLK kinase activity was measured using the Z′-LYTE assay at Thermo Fisher. A 10-point dose response (final ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase TEC


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a 345n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
TEC enzyme (LifeTech # PV3269) and Eu-anti-HIS antibody (Invitrogen # PV5596) are mixed and diluted in kinase buffer (50 mM Hepes pH 7.5+10 mM MgCl2+...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Receptor tyrosine-protein kinase erbB-2


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a 552n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
BMX, TXK, EGFR, ERBB2, ERBB4, JAK3, BLK kinase activity was measured using the Z′-LYTE assay at Thermo Fisher. A 10-point dose response (final ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase TXK


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a 567n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
BMX, TXK, EGFR, ERBB2, ERBB4, JAK3, BLK kinase activity was measured using the Z′-LYTE assay at Thermo Fisher. A 10-point dose response (final ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase Blk


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a 6.17E+3n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
BMX, TXK, EGFR, ERBB2, ERBB4, JAK3, BLK kinase activity was measured using the Z′-LYTE assay at Thermo Fisher. A 10-point dose response (final ...


US Patent US10858364 (2020)

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


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a>1.00E+4n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
BMX, TXK, EGFR, ERBB2, ERBB4, JAK3, BLK kinase activity was measured using the Z′-LYTE assay at Thermo Fisher. A 10-point dose response (final ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase ITK/TSK


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a>1.00E+4n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
TBITK enzyme (Millipore #14-660M) is diluted to 0.2 U/mL in KR buffer (10 mM Tris-HCl, 10 mM MgCl2, 0.01% Tween-20, 0.1% NaN3, 1 mM DTT, 2 mM MnCl2, ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM474105
PNG
(US10858364, formula (I))
Show SMILES CC#CC(=O)NCCCC(=O)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Show InChI InChI=1S/C26H23N7O3/c1-2-6-21(35)29-14-5-7-19(34)25-32-22(23-24(27)30-15-16-33(23)25)17-9-11-18(12-10-17)26(36)31-20-8-3-4-13-28-20/h3-4,8-13,15-16H,5,7,14H2,1H3,(H2,27,30)(H,29,35)(H,28,31,36)
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n/an/a>1.00E+4n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
BMX, TXK, EGFR, ERBB2, ERBB4, JAK3, BLK kinase activity was measured using the Z′-LYTE assay at Thermo Fisher. A 10-point dose response (final ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
Tyrosine-protein kinase ITK/TSK


(Homo sapiens (Human))
BDBM474106
PNG
(US10858364, Formula (II))
Show SMILES COc1cc(ccc1C(=O)Nc1ccccn1)-c1nc(C(=O)CCCNC(=O)C#CC)n2ccnc(N)c12
Show InChI InChI=1S/C27H25N7O4/c1-3-7-22(36)30-13-6-8-19(35)26-33-23(24-25(28)31-14-15-34(24)26)17-10-11-18(20(16-17)38-2)27(37)32-21-9-4-5-12-29-21/h4-5,9-12,14-16H,6,8,13H2,1-2H3,(H2,28,31)(H,30,36)(H,29,32,37)
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n/an/a>1.00E+4n/an/an/an/an/an/a



Acerta Pharma B.V.

US Patent


Assay Description
TBITK enzyme (Millipore #14-660M) is diluted to 0.2 U/mL in KR buffer (10 mM Tris-HCl, 10 mM MgCl2, 0.01% Tween-20, 0.1% NaN3, 1 mM DTT, 2 mM MnCl2, ...


US Patent US10858364 (2020)

More data for this
Ligand-Target Pair
* indicates data uncertainty>20%