compound 25b [PMID: 22564207] [Ligand Id: 8139] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2064666
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
  • This target only has 0 pki data point
  • 0
1 CHEMBL2064666_lig_chart_1 ALK tyrosine kinase receptor Human
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  • mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
  • This target only has 0 pki data point
  • 0
2 CHEMBL2064666_lig_chart_2 c-Jun N-terminal kinase 1 Human
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  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
  • This target only has 0 pki data point
  • 0
3 CHEMBL2064666_lig_chart_3 Focal adhesion kinase 1 Human
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
4 CHEMBL2064666_lig_chart_4 HERG Human
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  • Insulin receptor in Human [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
  • This target only has 0 pki data point
  • 0
5 CHEMBL2064666_lig_chart_5 Insulin receptor Human
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  • mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851]
  • This target only has 0 pki data point
  • 0
6 CHEMBL2064666_lig_chart_6 Mitogen-activated protein kinase kinase kinase kinase 2 Human
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  • NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285]
  • This target only has 0 pki data point
  • 0
7 CHEMBL2064666_lig_chart_7 NUAK family SNF1-like kinase 1 Human
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  • ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
  • This target only has 0 pki data point
  • 0
8 CHEMBL2064666_lig_chart_8 Ribosomal protein S6 kinase alpha 1 Human
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  • ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha 2 in Human [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349]
  • This target only has 0 pki data point
  • 0
9 CHEMBL2064666_lig_chart_9 Ribosomal protein S6 kinase alpha 2 Human
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  • ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
  • This target only has 0 pki data point
  • 0
10 CHEMBL2064666_lig_chart_10 Ribosomal protein S6 kinase alpha 3 Human
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  • ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha 6 in Human [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32]
  • This target only has 0 pki data point
  • 0
11 CHEMBL2064666_lig_chart_11 Ribosomal protein S6 kinase alpha 6 Human
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  • checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
  • This target only has 0 pki data point
  • 0
12 CHEMBL2064666_lig_chart_12 Serine/threonine-protein kinase Chk2 Human
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  • tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
  • This target only has 0 pki data point
  • 0
13 CHEMBL2064666_lig_chart_13 Tyrosine kinase non-receptor protein 2 Human
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  • protein tyrosine kinase 6/Tyrosine-protein kinase BRK in Human [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
  • This target only has 0 pki data point
  • 0
14 CHEMBL2064666_lig_chart_14 Tyrosine-protein kinase BRK Human
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  • FER tyrosine kinase/Tyrosine-protein kinase FER in Human [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
  • This target only has 0 pki data point
  • 0
15 CHEMBL2064666_lig_chart_15 Tyrosine-protein kinase FER Human
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  • FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase FES in Human [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
  • This target only has 0 pki data point
  • 0
16 CHEMBL2064666_lig_chart_16 Tyrosine-protein kinase FES Human
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
  • This target only has 0 pki data point
  • 0
17 CHEMBL2064666_lig_chart_17 Tyrosine-protein kinase receptor FLT3 Human
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
  • This target only has 0 pki data point
  • 0
18 CHEMBL2064666_lig_chart_18 Vascular endothelial growth factor receptor 3 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Inhibition of ALK tyrosine phosphorylation in human Karpas-299 cells after 2 hrs in presence of mouse plasma B 7.7 pIC50 20 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
ChEMBL Inhibition of NPM-ALK phosphorylation in human SUP-M2 cells after 2 to 3 hrs by ELISA B 7.7 pIC50 20 nM IC50 J Med Chem (2016) 59: 7478-7496 [PMID:27527804]
GtoPdb - - 8.72 pIC50 1.9 nM IC50 J Med Chem (2012) 55: 4580-93 [PMID:22564207]
ChEMBL Inhibition of human ALK cytoplasmic domain expressed in baculovirus using GST-PLCgamma as substrate preincubated for 15 mins before substrate addition measured after 1 hr by time resolved fluorescence assay B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
ChEMBL Inhibition of human ALK expressed in baculovirus using recombinant GST PLC-gamma as substrate assessed as phosphorylation of the substrate after 15 mins by TRF assay B 8.72 pIC50 1.9 nM IC50 J Med Chem (2016) 59: 7478-7496 [PMID:27527804]
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL Inhibition of human JNK1alpha1 B 6.95 pIC50 112 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Inhibition of FAK phosphorylation in human HCC827 cells after 2 to 2.5 hrs by immunoblot analysis B 6.03 pIC50 944 nM IC50 J Med Chem (2016) 59: 7478-7496 [PMID:27527804]
ChEMBL Inhibition of human FAK B 6.88 pIC50 133 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
ChEMBL Inhibition of human FAK expressed in baculovirus after 30 mins using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate by TRF assay B 7.6 pIC50 25 nM IC50 J Med Chem (2016) 59: 7478-7496 [PMID:27527804]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 7478-7496 [PMID:27527804]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of INSR (unknown origin) by cell based assay B 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 7478-7496 [PMID:27527804]
ChEMBL Inhibition of recombinant human INSR expressed in baculovirus using ATP as substrate after 15 mins by TRF assay B 6.18 pIC50 662 nM IC50 J Med Chem (2016) 59: 7478-7496 [PMID:27527804]
mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851]
ChEMBL Inhibition of human GCK B 7.22 pIC50 60 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285]
ChEMBL Inhibition of human ARK5 B 7.59 pIC50 26 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
GtoPdb NuaK1 is reported by its synonym ARK5 in the referencing article. - 7.59 pIC50 26 nM IC50 J Med Chem (2012) 55: 4580-93 [PMID:22564207]
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
ChEMBL Inhibition of human Rsk1 B 7.21 pIC50 61 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Med Chem (2012) 55: 4580-93 [PMID:22564207]
ChEMBL Inhibition of human Rsk3 B 8.15 pIC50 7 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL Inhibition of human Rsk2 B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
GtoPdb - - 7.89 pIC50 13 nM IC50 J Med Chem (2012) 55: 4580-93 [PMID:22564207]
ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32]
GtoPdb - - 7.72 pIC50 19 nM IC50 J Med Chem (2012) 55: 4580-93 [PMID:22564207]
ChEMBL Inhibition of human Rsk4 B 7.72 pIC50 19 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
ChEMBL Inhibition of human CHK2 B 7.54 pIC50 29 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
GtoPdb - - 7.54 pIC50 29 nM IC50 J Med Chem (2012) 55: 4580-93 [PMID:22564207]
tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
ChEMBL Inhibition of human ACK1 B 7.39 pIC50 41 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
protein tyrosine kinase 6/Tyrosine-protein kinase BRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
ChEMBL Inhibition of human BRK B 7.14 pIC50 73 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
FER tyrosine kinase/Tyrosine-protein kinase FER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
GtoPdb - - 7.07 pIC50 85 nM IC50 J Med Chem (2012) 55: 4580-93 [PMID:22564207]
ChEMBL Inhibition of human Fer B 7.07 pIC50 85 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase FES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
GtoPdb - - 7 pIC50 99 nM IC50 J Med Chem (2012) 55: 4580-93 [PMID:22564207]
ChEMBL Inhibition of human Fes B 7 pIC50 99 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of human Flt3 B 7.06 pIC50 88 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Inhibition of human Flt4 B 7.32 pIC50 48 nM IC50 J. Med. Chem. (2012) 55: 4580-4593 [PMID:22564207]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]