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 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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]