compound 8e [PMID: 24432909] [Ligand Id: 8137] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL3128069
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Mouse [ChEMBL: CHEMBL5771] [GtoPdb: 1839] [UniProtKB: P97793]
There should be some charts here, you may need to enable JavaScript!
  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
There should be some charts here, you may need to enable JavaScript!
  • leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
There should be some charts here, you may need to enable JavaScript!
  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
There should be some charts here, you may need to enable JavaScript!
  • neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
There should be some charts here, you may need to enable JavaScript!
  • neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
There should be some charts here, you may need to enable JavaScript!
  • protein tyrosine kinase 2 beta/Protein tyrosine kinase 2 beta in Human [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
There should be some charts here, you may need to enable JavaScript!
  • c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
There should be some charts here, you may need to enable JavaScript!
  • tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
There should be some charts here, you may need to enable JavaScript!
  • FER tyrosine kinase/Tyrosine-protein kinase FER in Human [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
There should be some charts here, you may need to enable JavaScript!
  • FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase FES in Human [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
There should be some charts here, you may need to enable JavaScript!
  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
There should be some charts here, you may need to enable JavaScript!
  • mitogen-activated protein kinase kinase kinase 9 in Human [GtoPdb: 2084] [UniProtKB: P80192]
There should be some charts here, you may need to enable JavaScript!
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 human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to Km levels of ATP addition measured after 1 hr by microfluidic mobility shift assay B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to ATP addition measured after 1 hr by microfluidic mobility shift assay B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2014) 57: 4720-4744 [PMID:24819116]
ChEMBL Inhibition of wild type human recombinant ALK kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to ATP addition measured after 1 hr by microfluidic mobility shift assay B 10 pKi <0.1 nM Ki J. Med. Chem. (2014) 57: 4720-4744 [PMID:24819116]
ChEMBL Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK G1269A mutant after 72 hrs by CellTiter Glo assay F 7.62 pIC50 24 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK L1196M mutant after 72 hrs by CellTiter Glo assay F 7.68 pIC50 21 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA B 8.18 pIC50 6.6 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA B 8.18 pIC50 6.6 nM IC50 J. Med. Chem. (2014) 57: 4720-4744 [PMID:24819116]
ChEMBL Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA B 8.35 pIC50 4.5 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA B 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of ALK-fusion driven cell proliferation in human KARPAS299 cells after 72 hrs by CellTiter Glo assay F 8.77 pIC50 1.7 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells after 72 hrs by CellTiter Glo assay F 8.89 pIC50 1.3 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of ALK L1196M mutant in mouse NIH-3T3 cells B 9.1 pIC50 0.8 nM IC50 J Med Chem (2019) 62: 10927-10954 [PMID:31419130]
ChEMBL Inhibition of human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA B 9.1 pIC50 0.8 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
GtoPdb - - 9.1 pIC50 0.8 nM IC50 J Med Chem (2014) 57: 1170-87 [PMID:24432909]
ChEMBL Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA B 9.12 pIC50 0.76 nM IC50 J. Med. Chem. (2014) 57: 4720-4744 [PMID:24819116]
ChEMBL Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA B 9.22 pIC50 0.6 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ChEMBL Inhibition of ALK L1196M (unknown origin) B 9.7 pIC50 0.2 nM IC50 J Med Chem (2019) 62: 10927-10954 [PMID:31419130]
ChEMBL Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA B 9.7 pIC50 0.2 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5771] [GtoPdb: 1839] [UniProtKB: P97793]
ChEMBL Inhibition of ALK in mouse NIH-3T3 cells B 9.1 pIC50 0.8 nM IC50 J Med Chem (2019) 62: 10927-10954 [PMID:31419130]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Inhibition of PTK2 (unknown origin) using Km levels of ATP B 7.8 pIC50 16 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
ChEMBL Inhibition of LTK (unknown origin) using Km levels of ATP B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
GtoPdb - - 8.7 pIC50 2 nM IC50 J Med Chem (2014) 57: 1170-87 [PMID:24432909]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Inhibition of NTRK1 (unknown origin) using Km levels of ATP B 7.77 pIC50 17 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
ChEMBL Inhibition of NTRK2 (unknown origin) using Km levels of ATP B 8.4 pIC50 4 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Med Chem (2014) 57: 1170-87 [PMID:24432909]
neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
ChEMBL Inhibition of NTRK3 (unknown origin) using Km levels of ATP B 7.74 pIC50 18 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
protein tyrosine kinase 2 beta/Protein tyrosine kinase 2 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
ChEMBL Inhibition of PTK2B (unknown origin) using Km levels of ATP B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
ChEMBL Inhibition of ROS1 (unknown origin) by Pfizer mobility shift assay B 10.7 pKi 0.02 nM Ki J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
GtoPdb Value calculated from tight-binding (Morrison) equation for competitive inhibitors tested in a Pfizer mobility shift assay. - 10.7 pKi 0.02 nM Ki J Med Chem (2014) 57: 1170-87 [PMID:24432909]
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 TNK2 (unknown origin) using Km levels of ATP B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
FER tyrosine kinase/Tyrosine-protein kinase FER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
ChEMBL Inhibition of FER (unknown origin) using Km levels of ATP B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
GtoPdb - - 8.7 pIC50 2 nM IC50 J Med Chem (2014) 57: 1170-87 [PMID:24432909]
FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase FES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Med Chem (2014) 57: 1170-87 [PMID:24432909]
ChEMBL Inhibition of FES (unknown origin) using Km levels of ATP B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 (unknown origin) using Km levels of ATP B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2014) 57: 1170-1187 [PMID:24432909]
mitogen-activated protein kinase kinase kinase 9 in Human [GtoPdb: 2084] [UniProtKB: P80192]
GtoPdb - - 7.42 pIC50 38 nM IC50 J Med Chem (2018) 61: 8078-8087 [PMID:29863360]

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]