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ChEMBL ligand: CHEMBL2064666 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]