compound 25b [PMID: 22564207] [Ligand Id: 8139] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
