belizatinib [Ligand Id: 10474] 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: CHEMBL2172308 |
|---|
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] | ||||||||
| GtoPdb | Binding affinity in vitro. | - | 9.44 | pKd | 0.36 | nM | Kd | J Med Chem (2012) 55: 6523-40 [PMID:22734674] |
| ChEMBL | Binding affinity to human ALK by Ambit titration assay | B | 9.44 | pKd | 0.36 | nM | Kd | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| ChEMBL | Inhibition of ALK Tyr1604 phosphorylation by cell based assay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| ChEMBL | Inhibition of ALK (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2019) 62: 10927-10954 [PMID:31419130] |
| ChEMBL | Inhibition of ALK enzyme | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay | B | 6.64 | pIC50 | 231 | nM | IC50 | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617] | ||||||||
| GtoPdb | Binding affinity in vitro. | - | 8.24 | pKd | 5.7 | nM | Kd | J Med Chem (2012) 55: 6523-40 [PMID:22734674] |
| ChEMBL | Binding affinity to human IRAK1 by Ambit titration assay | B | 8.24 | pKd | 5.7 | nM | Kd | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376] | ||||||||
| GtoPdb | Binding affinity in vitro. | - | 8.6 | pKd | 2.5 | nM | Kd | J Med Chem (2012) 55: 6523-40 [PMID:22734674] |
| ChEMBL | Binding affinity to human LTK by Ambit titration assay | B | 8.6 | pKd | 2.5 | nM | Kd | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| 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 | Binding affinity to human MAP4K2 by Ambit titration assay | B | 7.96 | pKd | 11 | nM | Kd | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| GtoPdb | Binding affinity in vitro. | - | 7.96 | pKd | 11 | nM | Kd | J Med Chem (2012) 55: 6523-40 [PMID:22734674] |
| 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 TRKA (unknown origin) | B | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| 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 TRKB (unknown origin) | B | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| 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 TRKC (unknown origin) | B | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| GtoPdb | Binding affinity in vitro. | - | 7.74 | pKd | 18 | nM | Kd | J Med Chem (2012) 55: 6523-40 [PMID:22734674] |
| ChEMBL | Binding affinity to human MER by Ambit titration assay | B | 7.74 | pKd | 18 | nM | Kd | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| GtoPdb | Binding affinity in vitro. | - | 7.55 | pKd | 28 | nM | Kd | J Med Chem (2012) 55: 6523-40 [PMID:22734674] |
| ChEMBL | Binding affinity to human LCK by Ambit titration assay | B | 7.55 | pKd | 28 | nM | Kd | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Binding affinity to human FLT3 by Ambit titration assay | B | 7.38 | pKd | 42 | nM | Kd | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| GtoPdb | Binding affinity in vitro. | - | 7.38 | pKd | 42 | nM | Kd | J Med Chem (2012) 55: 6523-40 [PMID:22734674] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Binding affinity to human AXL by Ambit titration assay | B | 7.54 | pKd | 29 | nM | Kd | J Med Chem (2012) 55: 6523-6540 [PMID:22734674] |
| GtoPdb | Binding affinity in vitro. | - | 7.54 | pKd | 29 | nM | Kd | J Med Chem (2012) 55: 6523-40 [PMID:22734674] |
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]
