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Compile Data Set for Download or QSAR

Found 255 hits Enz. Inhib. hit(s) with Target = 'Tyrosine-protein kinase CSK' AND taxid = 9606   
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
Tyrosine-protein kinase CSK


(Homo sapiens (human))
BDBM50142887
PNG
(1-(tert-butyl)-3-(4-chlorophenyl)-4-aminopyrazolo[...)
Show SMILES CC(C)(C)n1nc(-c2ccc(Cl)cc2)c2c(N)ncnc12
Show InChI InChI=1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)
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Article
PubMed
730n/an/an/an/an/an/an/an/a



University of Dundee

Curated by PDSP Ki Database




Biochem J 371: 199-204 (2003)

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


(Homo sapiens (human))
BDBM50341519
PNG
((S)-3-(4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl...)
Show SMILES CNc1cncc(n1)-c1c[nH]c(=O)c(NC(=O)c2ccc(cc2)N2CCC[C@H]2CN2CCCC2)c1
Show InChI InChI=1S/C26H31N7O2/c1-27-24-16-28-15-23(30-24)19-13-22(26(35)29-14-19)31-25(34)18-6-8-20(9-7-18)33-12-4-5-21(33)17-32-10-2-3-11-32/h6-9,13-16,21H,2-5,10-12,17H2,1H3,(H,27,30)(H,29,35)(H,31,34)/t21-/m0/s1
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>1.00E+3n/an/an/an/an/an/an/an/a



Vertex Pharmaceuticals (Europe) Ltd.

Curated by ChEMBL


Assay Description
Inhibition of CSK


J Med Chem 54: 2341-50 (2011)

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


(Homo sapiens (human))
BDBM50305126
PNG
(7-(2-(dimethylamino)ethoxy)-2-(4-phenoxyphenyl)-9,...)
Show SMILES CN(C)CCOc1ccc2Nc3c(C(N)=O)c(nn3CCc2c1)-c1ccc(Oc2ccccc2)cc1
Show InChI InChI=1S/C28H29N5O3/c1-32(2)16-17-35-23-12-13-24-20(18-23)14-15-33-28(30-24)25(27(29)34)26(31-33)19-8-10-22(11-9-19)36-21-6-4-3-5-7-21/h3-13,18,30H,14-17H2,1-2H3,(H2,29,34)
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n/an/a 1.70n/an/an/an/an/an/a



Taisho Pharmaceutical Co., Ltd

Curated by ChEMBL


Assay Description
Inhibition of Csk


Bioorg Med Chem Lett 20: 112-6 (2010)

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


(Homo sapiens (human))
BDBM50357312
PNG
(IBRUTINIB | US9108973, Ref 1 | US9181263, 1 | US92...)
Show SMILES Nc1ncnc2n(nc(-c3ccc(Oc4ccccc4)cc3)c12)[C@@H]1CCCN(C1)C(=O)C=C
Show InChI InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m1/s1
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US Patent
n/an/a 2.20n/an/an/an/an/an/a



PHARMACYCLICS LLC

US Patent


Assay Description
IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme in...


US Patent US9181263 (2015)

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


(Homo sapiens (human))
BDBM50357312
PNG
(IBRUTINIB | US9108973, Ref 1 | US9181263, 1 | US92...)
Show SMILES Nc1ncnc2n(nc(-c3ccc(Oc4ccccc4)cc3)c12)[C@@H]1CCCN(C1)C(=O)C=C
Show InChI InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m1/s1
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US Patent
n/an/a 2.20n/an/an/an/an/an/a



Pharmacyclics LLC

US Patent


Assay Description
IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction condition...


US Patent US9278100 (2016)

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


(Homo sapiens (human))
BDBM97672
PNG
(US8476284, 40 | US9133201, 10 | US9181263, 9 | US9...)
Show SMILES Nc1ncnc2n(nc(-c3ccc(Oc4ccccc4)cc3)c12)[C@@H]1CC[C@@H](CC1)NC(=O)C=C
Show InChI InChI=1S/C26H26N6O2/c1-2-22(33)30-18-10-12-19(13-11-18)32-26-23(25(27)28-16-29-26)24(31-32)17-8-14-21(15-9-17)34-20-6-4-3-5-7-20/h2-9,14-16,18-19H,1,10-13H2,(H,30,33)(H2,27,28,29)/t18-,19+
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US Patent
n/an/a 2.40n/an/an/an/an/an/a



Pharmacyclics LLC

US Patent


Assay Description
IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction condition...


US Patent US9278100 (2016)

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


(Homo sapiens (human))
BDBM97672
PNG
(US8476284, 40 | US9133201, 10 | US9181263, 9 | US9...)
Show SMILES Nc1ncnc2n(nc(-c3ccc(Oc4ccccc4)cc3)c12)[C@@H]1CC[C@@H](CC1)NC(=O)C=C
Show InChI InChI=1S/C26H26N6O2/c1-2-22(33)30-18-10-12-19(13-11-18)32-26-23(25(27)28-16-29-26)24(31-32)17-8-14-21(15-9-17)34-20-6-4-3-5-7-20/h2-9,14-16,18-19H,1,10-13H2,(H,30,33)(H2,27,28,29)/t18-,19+
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n/an/a 2.40n/an/an/an/an/an/a



PHARMACYCLICS LLC

US Patent


Assay Description
IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme in...


US Patent US9181263 (2015)

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


(Homo sapiens (human))
BDBM50305146
PNG
(4-amino-5-(2,6-difluorobenzoyl)-2-(4-phenoxyphenyl...)
Show SMILES NC(=O)c1c(N)c([nH]c1-c1ccc(Oc2ccccc2)cc1)C(=O)c1c(F)cccc1F
Show InChI InChI=1S/C24H17F2N3O3/c25-16-7-4-8-17(26)18(16)23(30)22-20(27)19(24(28)31)21(29-22)13-9-11-15(12-10-13)32-14-5-2-1-3-6-14/h1-12,29H,27H2,(H2,28,31)
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n/an/a 4.5n/an/an/an/an/an/a



Taisho Pharmaceutical Co., Ltd

Curated by ChEMBL


Assay Description
Inhibition of Csk


Bioorg Med Chem Lett 20: 108-11 (2010)

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


(Homo sapiens (human))
BDBM93207
PNG
(Kinase inhibitor, 5)
Show SMILES Cc1ccc(NC(=O)c2cccc(c2)C(F)(F)F)cc1-c1ccc2nc(Nc3ccc(OCCN)cc3)ncc2c1
Show InChI InChI=1S/C31H26F3N5O2/c1-19-5-7-25(37-29(40)21-3-2-4-23(16-21)31(32,33)34)17-27(19)20-6-12-28-22(15-20)18-36-30(39-28)38-24-8-10-26(11-9-24)41-14-13-35/h2-12,15-18H,13-14,35H2,1H3,(H,37,40)(H,36,38,39)
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n/an/a 8.40n/an/an/an/a7.525



University of Washington



Assay Description
Fluorescence assay used for determination of catch and release efficiency.


ACS Chem Biol 8: 691-9 (2013)

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


(Homo sapiens (human))
BDBM81375
PNG
(Amine compound, 12a)
Show SMILES Cc1ccc(NC(=O)c2cccc(c2)C(F)(F)F)cc1Nc1ncccc1-c1ncnc(Nc2ccc(OCCNC(=O)COCCOCCOCCOCCN)cc2)n1
Show InChI InChI=1S/C41H46F3N9O7/c1-28-7-8-32(50-39(55)29-4-2-5-30(24-29)41(42,43)44)25-35(28)52-37-34(6-3-14-47-37)38-48-27-49-40(53-38)51-31-9-11-33(12-10-31)60-17-15-46-36(54)26-59-23-22-58-21-20-57-19-18-56-16-13-45/h2-12,14,24-25,27H,13,15-23,26,45H2,1H3,(H,46,54)(H,47,52)(H,50,55)(H,48,49,51,53)
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n/an/a 16.3n/an/an/an/a7.5n/a



University of Washington



Assay Description
In vitro activity assay using various kinases.


Chem Biol 17: 195-206 (2010)

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


(Homo sapiens (human))
BDBM50114585
PNG
((R)-7-[4-(4-Methyl-piperazin-1-yl)-cyclohexyl]-5-(...)
Show SMILES CN1CCN(CC1)[C@H]1CC[C@H](CC1)n1cc(-c2ccc(Oc3ccccc3)cc2)c2c(N)ncnc12
Show InChI InChI=1S/C29H34N6O/c1-33-15-17-34(18-16-33)22-9-11-23(12-10-22)35-19-26(27-28(30)31-20-32-29(27)35)21-7-13-25(14-8-21)36-24-5-3-2-4-6-24/h2-8,13-14,19-20,22-23H,9-12,15-18H2,1H3,(H2,30,31,32)/t22-,23+
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PubMed
n/an/a 41n/an/an/an/an/an/a



Abbott Bioresearch Center

Curated by ChEMBL


Assay Description
Inhibition of human Tyrosine-protein kinase CSK


Bioorg Med Chem Lett 12: 1683-6 (2002)

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


(Homo sapiens (human))
BDBM4552
PNG
(4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-...)
Show SMILES COc1cc(Nc2c(cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)C#N)c(Cl)cc1Cl
Show InChI InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31)
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n/an/a 63n/an/an/an/an/an/a



Center for Molecular Medicine of the Austrian Academy of Sciences

Curated by ChEMBL


Assay Description
Inhibition of CSK


Leukemia 23: 477-85 (2009)

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


(Homo sapiens (human))
BDBM50340571
PNG
((3-((2-(3,5-dimorpholinophenylamino)pyrimidin-4-yl...)
Show SMILES CN(c1ccnc(Nc2cc(cc(c2)N2CCOCC2)N2CCOCC2)n1)c1cc(CO)ccc1C
Show InChI InChI=1S/C27H34N6O3/c1-20-3-4-21(19-34)15-25(20)31(2)26-5-6-28-27(30-26)29-22-16-23(32-7-11-35-12-8-32)18-24(17-22)33-9-13-36-14-10-33/h3-6,15-18,34H,7-14,19H2,1-2H3,(H,28,29,30)
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n/an/a 80n/an/an/an/an/an/a



Centre de Recherches

Curated by ChEMBL


Assay Description
Inhibition of CSK


Bioorg Med Chem Lett 21: 2207-11 (2011)

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


(Homo sapiens (human))
BDBM81376
PNG
(Amine compound, 13a)
Show SMILES Cc1ccc(NC(=O)c2cccc(c2)C(F)(F)F)cc1Nc1ncccc1-c1cc(Nc2ccc(OCCNC(=O)COCCOCCOCCOCCN)cc2)ncn1
Show InChI InChI=1S/C42H47F3N8O7/c1-29-7-8-33(52-41(55)30-4-2-5-31(24-30)42(43,44)45)25-36(29)53-40-35(6-3-14-48-40)37-26-38(50-28-49-37)51-32-9-11-34(12-10-32)60-17-15-47-39(54)27-59-23-22-58-21-20-57-19-18-56-16-13-46/h2-12,14,24-26,28H,13,15-23,27,46H2,1H3,(H,47,54)(H,48,53)(H,52,55)(H,49,50,51)
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n/an/a 140n/an/an/an/a7.5n/a



University of Washington



Assay Description
In vitro activity assay using various kinases.


Chem Biol 17: 195-206 (2010)

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


(Homo sapiens (human))
BDBM50096279
PNG
(CHEMBL3577124)
Show SMILES CNc1ncc2cc(c(C)nc2n1)-c1cc(NC(=O)NCCC(C)(C)C)c(F)cc1C
Show InChI InChI=1S/C18H13N3O5/c22-14(23)5-4-10-8-21-13-7-12-9(6-15(24)25)2-1-3-11(12)16(13)20-18(26)17(21)19-10/h1-5,8H,6-7H2,(H,20,26)(H,22,23)(H,24,25)/b5-4+
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n/an/a 290n/an/an/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Competitive binding affinity to CSK in human A375 cells after 15 mins in presence of ATP analogue


J Med Chem 58: 4165-79 (2015)

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


(Homo sapiens (human))
BDBM50142887
PNG
(1-(tert-butyl)-3-(4-chlorophenyl)-4-aminopyrazolo[...)
Show SMILES CC(C)(C)n1nc(-c2ccc(Cl)cc2)c2c(N)ncnc12
Show InChI InChI=1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)
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n/an/a 500n/an/an/an/an/an/a



University of Delhi, Delhi 110007, India



Assay Description
The kinase reaction was initiated with the incubation of the 2.5 µL of the reaction cocktail (0.7 nM of His6-Src kinase domain in kinase buffer)...


Bioorg Chem 53: 75-82 (2014)

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


(Homo sapiens (human))
BDBM50298225
PNG
(CHEMBL2069955 | CHEMBL573578 | NM-PP1)
Show SMILES CC(C)(C)n1nc(Cc2cccc3ccccc23)c2c(N)ncnc12
Show InChI InChI=1S/C20H21N5/c1-20(2,3)25-19-17(18(21)22-12-23-19)16(24-25)11-14-9-6-8-13-7-4-5-10-15(13)14/h4-10,12H,11H2,1-3H3,(H2,21,22,23)
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n/an/a 510n/an/an/an/an/an/a



University of Dundee

Curated by ChEMBL


Assay Description
Inhibition of CSK in the presence of 20uM ATP


Biochem J 408: 297-315 (2007)

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


(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 600n/an/an/an/an/an/a



University of Delhi, Delhi 110007, India



Assay Description
The kinase reaction was initiated with the incubation of the 2.5 µL of the reaction cocktail (0.7 nM of His6-Src kinase domain in kinase buffer)...


Bioorg Chem 53: 75-82 (2014)

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


(Homo sapiens (human))
BDBM25116
PNG
(1-tert-butyl-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]...)
Show SMILES Cc1ccc(cc1)-c1nn(c2ncnc(N)c12)C(C)(C)C
Show InChI InChI=1S/C16H19N5/c1-10-5-7-11(8-6-10)13-12-14(17)18-9-19-15(12)21(20-13)16(2,3)4/h5-9H,1-4H3,(H2,17,18,19)
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n/an/a 640n/an/an/an/an/an/a



University of Dundee

Curated by ChEMBL


Assay Description
Inhibition of CSK in the presence of 20uM ATP


Biochem J 408: 297-315 (2007)

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


(Homo sapiens (human))
BDBM50193874
PNG
(7-(2,6-dimethylphenyl)-5-methyl-N-(4-(2-(pyrrolidi...)
Show SMILES Cc1cccc(C)c1-c1cc(C)c2nc(Nc3ccc(OCCN4CCCC4)cc3)nnc2c1
Show InChI InChI=1S/C28H31N5O/c1-19-7-6-8-20(2)26(19)22-17-21(3)27-25(18-22)31-32-28(30-27)29-23-9-11-24(12-10-23)34-16-15-33-13-4-5-14-33/h6-12,17-18H,4-5,13-16H2,1-3H3,(H,29,30,32)
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n/an/a 659n/an/an/an/an/an/a



TargeGen, Inc.

Curated by ChEMBL


Assay Description
Inhibition of CSK


Bioorg Med Chem Lett 16: 5546-50 (2006)

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


(Homo sapiens (human))
BDBM50433806
PNG
(CHEMBL2382016)
Show SMILES NC(N)=NCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O
Show InChI InChI=1S/C85H110N30O10/c86-81(87)96-31-11-26-61-71(116)111-66(36-46-41-101-56-21-6-1-16-51(46)56)76(121)106-62(27-12-32-97-82(88)89)72(117)112-68(38-48-43-103-58-23-8-3-18-53(48)58)78(123)108-64(29-14-34-99-84(92)93)74(119)114-70(40-50-45-105-60-25-10-5-20-55(50)60)80(125)110-65(30-15-35-100-85(94)95)75(120)115-69(39-49-44-104-59-24-9-4-19-54(49)59)79(124)109-63(28-13-33-98-83(90)91)73(118)113-67(77(122)107-61)37-47-42-102-57-22-7-2-17-52(47)57/h1-10,16-25,41-45,61-70,101-105H,11-15,26-40H2,(H,106,121)(H,107,122)(H,108,123)(H,109,124)(H,110,125)(H,111,116)(H,112,117)(H,113,118)(H,114,119)(H,115,120)(H4,86,87,96)(H4,88,89,97)(H4,90,91,98)(H4,92,93,99)(H4,94,95,100)/t61-,62-,63-,64-,65-,66-,67-,68-,69-,70-/m0/s1
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n/an/a 800n/an/an/an/an/an/a



University of Rhode Island

Curated by ChEMBL


Assay Description
Inhibition of GST-fused Csk (unknown origin) expressed in Escherichia coli using polyE4Y as substrate after 20 mins by scintillation counting analysi...


Bioorg Med Chem Lett 23: 3230-4 (2013)

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


(Homo sapiens (human))
BDBM12255
PNG
(AZD0530 | CHEMBL217092 | Compound 33 | N-(5-chloro...)
Show SMILES CN1CCN(CCOc2cc(OC3CCOCC3)c3c(Nc4c5OCOc5ccc4Cl)ncnc3c2)CC1
Show InChI InChI=1S/C27H32ClN5O5/c1-32-6-8-33(9-7-32)10-13-35-19-14-21-24(23(15-19)38-18-4-11-34-12-5-18)27(30-16-29-21)31-25-20(28)2-3-22-26(25)37-17-36-22/h2-3,14-16,18H,4-13,17H2,1H3,(H,29,30,31)
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n/an/a 840n/an/an/an/an/an/a



Amgen, Inc.

Curated by ChEMBL


Assay Description
Inhibition of CSK


J Med Chem 53: 4332-53 (2010)

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


(Homo sapiens (human))
BDBM12255
PNG
(AZD0530 | CHEMBL217092 | Compound 33 | N-(5-chloro...)
Show SMILES CN1CCN(CCOc2cc(OC3CCOCC3)c3c(Nc4c5OCOc5ccc4Cl)ncnc3c2)CC1
Show InChI InChI=1S/C27H32ClN5O5/c1-32-6-8-33(9-7-32)10-13-35-19-14-21-24(23(15-19)38-18-4-11-34-12-5-18)27(30-16-29-21)31-25-20(28)2-3-22-26(25)37-17-36-22/h2-3,14-16,18H,4-13,17H2,1H3,(H,29,30,31)
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n/an/a 840n/an/an/an/an/an/a



Harvard Medical School

Curated by ChEMBL


Assay Description
Inhibition of Csk


Proc Natl Acad Sci USA 104: 19936-41 (2007)

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


(Homo sapiens (human))
BDBM50192071
PNG
((13R,15S)-13-methyl-16-oxa-8,9,12,22,24-pentaazahe...)
Show SMILES C[C@@H]1C[C@H]2CN1CCn1[nH]c3c(cccc3c1=O)-c1nc3c(O2)cccc3[nH]c1=O
Show InChI InChI=1S/C22H21N5O3/c1-12-10-13-11-26(12)8-9-27-22(29)15-5-2-4-14(18(15)25-27)19-21(28)23-16-6-3-7-17(30-13)20(16)24-19/h2-7,12-13,25H,8-11H2,1H3,(H,23,28)/t12-,13+/m1/s1
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n/an/a>1.00E+3n/an/an/an/an/an/a



Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories

Curated by ChEMBL


Assay Description
Inhibition of CSK


Bioorg Med Chem Lett 16: 5122-6 (2006)

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


(Homo sapiens (human))
BDBM50095952
PNG
(CHEMBL3593777)
Show SMILES NC(=O)c1cnc2[nH]ccc2c1N[C@@H]1CCN(C[C@@H]1F)c1ccc(cn1)C#N
Show InChI InChI=1S/C15H23N5O5/c1-2-4-24-5-3-9-18-13(16)10-14(19-9)20(7-17-10)15-12(23)11(22)8(6-21)25-15/h7-8,11-12,15,21-23H,2-6H2,1H3,(H2,16,18,19)/t8-,11+,12+,15?/m1/s1
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n/an/a>1.00E+3n/an/an/an/an/an/a



Astellas Pharma Inc.

Curated by ChEMBL


Assay Description
Inhibition of CSK (unknown origin)


Bioorg Med Chem 23: 4871-83 (2015)

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


(Homo sapiens (human))
BDBM25617
PNG
(N-[3-({5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl}carb...)
Show SMILES CCCS(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(Cl)cc23)c1F
Show InChI InChI=1S/C17H14ClF2N3O3S/c1-2-5-27(25,26)23-13-4-3-12(19)14(15(13)20)16(24)11-8-22-17-10(11)6-9(18)7-21-17/h3-4,6-8,23H,2,5H2,1H3,(H,21,22)
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n/an/a 1.50E+3n/an/an/an/a7.522



Plexxikon



Assay Description
Enzyme activity was assayed using Z-LYTE Enzymatic Kinase Assay format (Invitrogen Corp., Carlsbad, CA) according to the manufacturer instructions.


Proc Natl Acad Sci U S A 105: 3041-6 (2008)

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


(Homo sapiens (human))
BDBM50229961
PNG
(1-(1,1-dimethylethyl)-3-(1-naphthalenyl)-1H-pyrazo...)
Show SMILES CC(C)(C)n1nc(-c2cccc3ccccc23)c2c(N)ncnc12
Show InChI InChI=1S/C19H19N5/c1-19(2,3)24-18-15(17(20)21-11-22-18)16(23-24)14-10-6-8-12-7-4-5-9-13(12)14/h4-11H,1-3H3,(H2,20,21,22)
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n/an/a 1.97E+3n/an/an/an/an/an/a



University of Dundee

Curated by ChEMBL


Assay Description
Inhibition of CSK in the presence of 20uM ATP


Biochem J 408: 297-315 (2007)

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


(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 2.10E+3n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Inhibition of Tyrosine-protein kinase CSK


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

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


(Homo sapiens (human))
BDBM50200197
PNG
((S)-2-amino-N-hydroxy-3-(4-hydroxyphenyl)propaneth...)
Show SMILES N[C@@H](Cc1ccc(O)cc1)C(=S)NO
Show InChI InChI=1S/C9H12N2O2S/c10-8(9(14)11-13)5-6-1-3-7(12)4-2-6/h1-4,8,12-13H,5,10H2,(H,11,14)/t8-/m0/s1
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n/an/a 2.50E+3n/an/an/an/an/an/a



University of Rhode Island

Curated by ChEMBL


Assay Description
Inhibition of CSK measured as poly-E4Y phosphorylation by acid precipitation assay in presence of 0.2 mM CoCl2


J Med Chem 49: 7532-9 (2006)

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


(Homo sapiens (human))
BDBM50345739
PNG
(1-isopropyl-3-(6-methoxynaphthalen-2-yl)-1H-pyrazo...)
Show SMILES COc1ccc2cc(ccc2c1)-c1nn(C(C)C)c2ncnc(N)c12
Show InChI InChI=1S/C19H19N5O/c1-11(2)24-19-16(18(20)21-10-22-19)17(23-24)14-5-4-13-9-15(25-3)7-6-12(13)8-14/h4-11H,1-3H3,(H2,20,21,22)
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n/an/a 2.60E+3n/an/an/an/an/an/a



University of Washington

Curated by ChEMBL


Assay Description
Inhibition of human CSK using Ac-KKKKEEIYFFF-OH as substrate after 180 mins


J Med Chem 55: 2416-26 (2012)

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


(Homo sapiens (human))
BDBM92633
PNG
(Thiazolidine-dione, 2)
Show SMILES CC(=C)CN1C(SC(=C)C1=O)=NN=c1scc(O)n1C
Show InChI InChI=1S/C12H14N4O2S2/c1-7(2)5-16-10(18)8(3)20-12(16)14-13-11-15(4)9(17)6-19-11/h6,17H,1,3,5H2,2,4H3
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n/an/a 3.00E+3n/an/an/an/an/an/a



Ciba-Geigy Ltd.



Assay Description
Determination of EGF receptor kinase activity was performed as described using A431 membranes as the enzyme source and agiotensin II as substrate.


J Biol Chem 265: 22255-61 (1990)

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


(Homo sapiens (human))
BDBM50345740
PNG
(3-(6-ethoxynaphthalen-2-yl)-1-isopropyl-1H-pyrazol...)
Show SMILES CCOc1ccc2cc(ccc2c1)-c1nn(C(C)C)c2ncnc(N)c12
Show InChI InChI=1S/C20H21N5O/c1-4-26-16-8-7-13-9-15(6-5-14(13)10-16)18-17-19(21)22-11-23-20(17)25(24-18)12(2)3/h5-12H,4H2,1-3H3,(H2,21,22,23)
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n/an/a 3.10E+3n/an/an/an/an/an/a



University of Washington

Curated by ChEMBL


Assay Description
Inhibition of human CSK using Ac-KKKKEEIYFFF-OH as substrate after 180 mins


J Med Chem 55: 2416-26 (2012)

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


(Homo sapiens (human))
BDBM50200187
PNG
((S)-2-amino-N-hydroxy-3-(4-iodophenyl)propanamide ...)
Show SMILES N[C@@H](Cc1ccc(I)cc1)C(=O)NO
Show InChI InChI=1S/C9H11IN2O2/c10-7-3-1-6(2-4-7)5-8(11)9(13)12-14/h1-4,8,14H,5,11H2,(H,12,13)/t8-/m0/s1
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n/an/a 3.20E+3n/an/an/an/an/an/a



University of Rhode Island

Curated by ChEMBL


Assay Description
Inhibition of CSK measured as poly-E4Y phosphorylation by acid precipitation assay in presence of 0.2 mM CoCl2


J Med Chem 49: 7532-9 (2006)

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


(Homo sapiens (human))
BDBM50200208
PNG
((S)-2-amino-N-hydroxy-3-(4-isopropylphenyl)propana...)
Show SMILES CC(C)c1ccc(C[C@H](N)C(=O)NO)cc1
Show InChI InChI=1S/C12H18N2O2/c1-8(2)10-5-3-9(4-6-10)7-11(13)12(15)14-16/h3-6,8,11,16H,7,13H2,1-2H3,(H,14,15)/t11-/m0/s1
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n/an/a 3.30E+3n/an/an/an/an/an/a



University of Rhode Island

Curated by ChEMBL


Assay Description
Inhibition of CSK measured as poly-E4Y phosphorylation by acid precipitation assay in presence of 0.2 mM CoCl2


J Med Chem 49: 7532-9 (2006)

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


(Homo sapiens (human))
BDBM50200198
PNG
((S)-2-amino-N-hydroxy-3-(4-hydroxy-3,5-diiodopheny...)
Show SMILES N[C@@H](Cc1cc(I)c(O)c(I)c1)C(=O)NO
Show InChI InChI=1S/C9H10I2N2O3/c10-5-1-4(2-6(11)8(5)14)3-7(12)9(15)13-16/h1-2,7,14,16H,3,12H2,(H,13,15)/t7-/m0/s1
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n/an/a 3.40E+3n/an/an/an/an/an/a



University of Rhode Island

Curated by ChEMBL


Assay Description
Inhibition of CSK measured as poly-E4Y phosphorylation by acid precipitation assay in presence of 0.2 mM CoCl2


J Med Chem 49: 7532-9 (2006)

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


(Homo sapiens (human))
BDBM50200190
PNG
((S)-2-amino-N-hydroxy-3-(2-iodophenyl)propanamide ...)
Show SMILES N[C@@H](Cc1ccccc1I)C(=O)NO
Show InChI InChI=1S/C9H11IN2O2/c10-7-4-2-1-3-6(7)5-8(11)9(13)12-14/h1-4,8,14H,5,11H2,(H,12,13)/t8-/m0/s1
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n/an/a 3.40E+3n/an/an/an/an/an/a



University of Rhode Island

Curated by ChEMBL


Assay Description
Inhibition of CSK measured as poly-E4Y phosphorylation by acid precipitation assay in presence of 0.2 mM CoCl2


J Med Chem 49: 7532-9 (2006)

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


(Homo sapiens (human))
BDBM50386693
PNG
(CHEMBL2048912)
Show SMILES CC(C)(N)C(=O)NCCn1ccc2ncnc(Nc3ccc(Oc4cccc5sncc45)c(Cl)c3)c12
Show InChI InChI=1S/C25H24ClN7O2S/c1-25(2,27)24(34)28-9-11-33-10-8-18-22(33)23(30-14-29-18)32-15-6-7-20(17(26)12-15)35-19-4-3-5-21-16(19)13-31-36-21/h3-8,10,12-14H,9,11,27H2,1-2H3,(H,28,34)(H,29,30,32)
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n/an/a 3.90E+3n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of CSK using ATP preincubated with compound for 5 mins measured after 10 mins


J Med Chem 55: 3975-91 (2012)

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


(Homo sapiens (human))
BDBM92632
PNG
(Thiazolidine-dione, 1)
Show SMILES Cn1c(O)csc1=NN=C1SC(=C)C(=O)N1CC=C
Show InChI InChI=1S/C11H12N4O2S2/c1-4-5-15-9(17)7(2)19-11(15)13-12-10-14(3)8(16)6-18-10/h4,6,16H,1-2,5H2,3H3
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n/an/a 4.00E+3n/an/an/an/an/an/a



Ciba-Geigy Ltd.



Assay Description
Determination of EGF receptor kinase activity was performed as described using A431 membranes as the enzyme source and agiotensin II as substrate.


J Biol Chem 265: 22255-61 (1990)

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


(Homo sapiens (human))
BDBM8793
PNG
(7-[4-(4-methylpiperazin-1-yl)cyclohexyl]-5-(4-phen...)
Show SMILES CN1CCN(CC1)[C@H]1CC[C@@H](CC1)n1cc(-c2ccc(Oc3ccccc3)cc2)c2c(N)ncnc12
Show InChI InChI=1S/C29H34N6O/c1-33-15-17-34(18-16-33)22-9-11-23(12-10-22)35-19-26(27-28(30)31-20-32-29(27)35)21-7-13-25(14-8-21)36-24-5-3-2-4-6-24/h2-8,13-14,19-20,22-23H,9-12,15-18H2,1H3,(H2,30,31,32)/t22-,23-
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n/an/a 4.27E+3n/an/an/an/an/an/a



Abbott Bioresearch Center

Curated by ChEMBL


Assay Description
Inhibition of human Csk tyrosine kinase


Bioorg Med Chem Lett 12: 1683-6 (2002)

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


(Homo sapiens (human))
BDBM50088912
PNG
(2-(4-(4-amino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-...)
Show SMILES Nc1ncnc2n(cc(-c3ccccc3)c12)-c1ccc(CNCCO)cc1
Show InChI InChI=1S/C21H21N5O/c22-20-19-18(16-4-2-1-3-5-16)13-26(21(19)25-14-24-20)17-8-6-15(7-9-17)12-23-10-11-27/h1-9,13-14,23,27H,10-12H2,(H2,22,24,25)
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n/an/a 4.30E+3n/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Tested for inhibition of protein tyrosine kinase Csk phosphorylation in intact cells


Bioorg Med Chem Lett 10: 945-9 (2000)

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


(Homo sapiens (human))
BDBM50358430
PNG
(CHEMBL1614725)
Show SMILES CC(C)(O)CC(=O)NCCn1ccc2ncnc(Nc3ccc(Oc4cccc(c4)C(F)(F)F)c(Cl)c3)c12
Show InChI InChI=1S/C26H25ClF3N5O3/c1-25(2,37)14-22(36)31-9-11-35-10-8-20-23(35)24(33-15-32-20)34-17-6-7-21(19(27)13-17)38-18-5-3-4-16(12-18)26(28,29)30/h3-8,10,12-13,15,37H,9,11,14H2,1-2H3,(H,31,36)(H,32,33,34)
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n/an/a 4.70E+3n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of N-terminus flag-tagged CSK expressed in baculovirus infected insect cells using ATP as substrate after 10 mins


J Med Chem 54: 8030-50 (2011)

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


(Homo sapiens (human))
BDBM50200189
PNG
((S)-2-amino-N-hydroxy-3-[4-(nitrophenyl)phenyl]pro...)
Show SMILES N[C@@H](Cc1ccc(cc1)-c1ccc(cc1)[N+]([O-])=O)C(=O)NO
Show InChI InChI=1S/C15H15N3O4/c16-14(15(19)17-20)9-10-1-3-11(4-2-10)12-5-7-13(8-6-12)18(21)22/h1-8,14,20H,9,16H2,(H,17,19)/t14-/m0/s1
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n/an/a 4.90E+3n/an/an/an/an/an/a



University of Rhode Island

Curated by ChEMBL


Assay Description
Inhibition of CSK measured as poly-E4Y phosphorylation by acid precipitation assay in presence of 0.2 mM CoCl2


J Med Chem 49: 7532-9 (2006)

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


(Homo sapiens (human))
BDBM50088905
PNG
(2-(3-(4-amino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-...)
Show SMILES Nc1ncnc2n(cc(-c3ccccc3)c12)-c1cccc(CNCCO)c1
Show InChI InChI=1S/C21H21N5O/c22-20-19-18(16-6-2-1-3-7-16)13-26(21(19)25-14-24-20)17-8-4-5-15(11-17)12-23-9-10-27/h1-8,11,13-14,23,27H,9-10,12H2,(H2,22,24,25)
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n/an/a 5.00E+3n/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Tested for inhibition of protein tyrosine kinase Csk phosphorylation in intact cells


Bioorg Med Chem Lett 10: 945-9 (2000)

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


(Homo sapiens (human))
BDBM50088903
PNG
(2-((4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-...)
Show SMILES COc1cccc(c1)-c1cn(-c2ccc(CCN(C)CCO)cc2)c2ncnc(N)c12
Show InChI InChI=1S/C24H27N5O2/c1-28(12-13-30)11-10-17-6-8-19(9-7-17)29-15-21(18-4-3-5-20(14-18)31-2)22-23(25)26-16-27-24(22)29/h3-9,14-16,30H,10-13H2,1-2H3,(H2,25,26,27)
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n/an/a>5.00E+3n/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Tested for inhibition of protein tyrosine kinase Csk phosphorylation in intact cells


Bioorg Med Chem Lett 10: 945-9 (2000)

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


(Homo sapiens (human))
BDBM50088900
PNG
(5,7-Diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine ...)
Show SMILES Nc1ncnc2n(cc(-c3ccccc3)c12)-c1ccccc1
Show InChI InChI=1S/C18H14N4/c19-17-16-15(13-7-3-1-4-8-13)11-22(18(16)21-12-20-17)14-9-5-2-6-10-14/h1-12H,(H2,19,20,21)
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n/an/a>5.00E+3n/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Tested for inhibition of protein tyrosine kinase Csk phosphorylation in intact cells


Bioorg Med Chem Lett 10: 945-9 (2000)

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


(Homo sapiens (human))
BDBM50088898
PNG
(2-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d...)
Show SMILES COc1cccc(c1)-c1cn(-c2ccc(CC(=O)NCCO)cc2)c2ncnc(N)c12
Show InChI InChI=1S/C23H23N5O3/c1-31-18-4-2-3-16(12-18)19-13-28(23-21(19)22(24)26-14-27-23)17-7-5-15(6-8-17)11-20(30)25-9-10-29/h2-8,12-14,29H,9-11H2,1H3,(H,25,30)(H2,24,26,27)
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n/an/a>5.00E+3n/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Tested for inhibition of protein tyrosine kinase Csk phosphorylation in intact cells


Bioorg Med Chem Lett 10: 945-9 (2000)

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


(Homo sapiens (human))
BDBM50088908
PNG
(5-(3-Methoxy-phenyl)-7-phenyl-7H-pyrrolo[2,3-d]pyr...)
Show SMILES COc1cccc(c1)-c1cn(-c2ccccc2)c2ncnc(N)c12
Show InChI InChI=1S/C19H16N4O/c1-24-15-9-5-6-13(10-15)16-11-23(14-7-3-2-4-8-14)19-17(16)18(20)21-12-22-19/h2-12H,1H3,(H2,20,21,22)
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n/an/a>5.00E+3n/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Tested for inhibition of protein tyrosine kinase Csk phosphorylation in intact cells


Bioorg Med Chem Lett 10: 945-9 (2000)

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


(Homo sapiens (human))
BDBM50088899
PNG
(2-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d...)
Show SMILES COc1cccc(c1)-c1cn(-c2ccc(CNCCO)cc2)c2ncnc(N)c12
Show InChI InChI=1S/C22H23N5O2/c1-29-18-4-2-3-16(11-18)19-13-27(22-20(19)21(23)25-14-26-22)17-7-5-15(6-8-17)12-24-9-10-28/h2-8,11,13-14,24,28H,9-10,12H2,1H3,(H2,23,25,26)
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n/an/a>5.00E+3n/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Tested for inhibition of protein tyrosine kinase Csk phosphorylation in intact cells


Bioorg Med Chem Lett 10: 945-9 (2000)

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


(Homo sapiens (human))
BDBM50088902
PNG
((3-(4-amino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-...)
Show SMILES Nc1ncnc2n(cc(-c3ccccc3)c12)-c1cccc(CO)c1
Show InChI InChI=1S/C19H16N4O/c20-18-17-16(14-6-2-1-3-7-14)10-23(19(17)22-12-21-18)15-8-4-5-13(9-15)11-24/h1-10,12,24H,11H2,(H2,20,21,22)
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n/an/a>5.00E+3n/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Tested for inhibition of protein tyrosine kinase Csk phosphorylation in intact cells


Bioorg Med Chem Lett 10: 945-9 (2000)

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


(Homo sapiens (human))
BDBM50391643
PNG
(CHEMBL2148052 | CHEMBL2148053)
Show SMILES CC(C)(C(=O)NCCn1ccc2ncnc(Nc3ccc(Oc4cccc(Cl)c4)c(Cl)c3)c12)S(C)(=O)=O
Show InChI InChI=1S/C25H25Cl2N5O4S/c1-25(2,37(3,34)35)24(33)28-10-12-32-11-9-20-22(32)23(30-15-29-20)31-17-7-8-21(19(27)14-17)36-18-6-4-5-16(26)13-18/h4-9,11,13-15H,10,12H2,1-3H3,(H,28,33)(H,29,30,31)
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n/an/a 5.10E+3n/an/an/an/an/an/a



Takeda Pharmaceutical Co. Ltd

Curated by ChEMBL


Assay Description
Inhibition of CSK after 5 mins


Bioorg Med Chem 20: 6171-80 (2012)

More data for this
Ligand-Target Pair
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