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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




Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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.


Citation and Details
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.


Citation and Details
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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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


Citation and Details
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


Citation and Details
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.


Citation and Details
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


Citation and Details
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)...


Citation and Details
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


Citation and Details
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)...


Citation and Details
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


Citation and Details
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


Citation and Details
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...


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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)


Citation and Details
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.


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
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


Citation and Details
More data for this
Ligand-Target Pair
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