belizatinib [Ligand Id: 10474] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2172308 |
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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] | ||||||||
| 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] |
| neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor 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 1/High affinity nerve growth factor receptor 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] |
| ChEMBL | Enzyme Assay: In each well of a 384-well plate, 1 nM-1.5 nM of wild type NTRK1 enzyme (BPS Bioscience; 40280) was incubated in a total of 12.5 μL of buffer (100 mM HEPES pH 7.5, 0.015% Brij 35, 10 mM MgCl2, 1 mM DTT) with 1-2 μM CSKtide (Tuft's University or Anaspec; FITC-AHA-KKKKD DIYFFFG-NH2) and 1 mM ATP at 25° C. for 60 minutes in the presence or absence of a dosed concentration series of compound (1% DMSO final concentration). The reaction was stopped by the addition of 70 μL of Stop buffer (100 mM HEPES pH 7.5, 0.015% Brij 35, 35 mM EDTA and 0.2% of Coating Reagent 3 (Caliper Lifesciences)). The plate was then read on a Caliper EZReader 2 (protocol settings: −1.7 psi, upstream voltage −500, downstream voltage −3000, post sample sip 35 s). Data was normalized to 0% and 100% inhibition controls and the IC50 calculated using a 4-parameter fit in the CORE LIMS. | B | 8.64 | pIC50 | 2.3 | nM | IC50 | US-10370379-B2. Compounds and compositions useful for treating disorders related to NTRK (2019) |
| 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 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] |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase 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] |
| 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] |
| MER proto-oncogene, tyrosine kinase/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] |
| 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 36:
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]
