lorlatinib [Ligand Id: 7476] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3286830 (Lorbrena, Lorlatinib, PF-06463922) |
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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 L1196M mutant (unknown origin) | B | 8.09 | pKi | 8.2 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| GtoPdb | Note that this is inhibition of the ALK L1196M mutant enzyme. | - | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2014) 57: 4720-44 [PMID:24819116] |
| 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 | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2018) 61: 6401-6420 [PMID:29589935] |
| ChEMBL | Inhibition of ALK (unknown origin) | B | 9.15 | pKi | 0.7 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) | B | 9.15 | pKi | 0.7 | nM | Ki | ACS Med Chem Lett (2018) 9: 878-883 [PMID:30258534] |
| 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 | 10.15 | pKi | <0.07 | nM | Ki | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| ChEMBL | Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| ChEMBL | Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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 | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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 | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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 | 8.05 | pIC50 | 9 | 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 | 8.38 | pIC50 | 4.2 | 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 | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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 | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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: 4720-4744 [PMID:24819116] |
| 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) by TR-FRET-based Z'-LYTE assay | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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) by TR-FRET-based Z'-LYTE assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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 NRTK1 (unknown origin) by TR-FRET-based Z'-LYTE assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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) by off-chip mobility shift assay | B | 7.64 | pKi | 23 | nM | Ki | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| ChEMBL | Inhibition of TrkB (unknown origin) | B | 7.64 | pKi | 23 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| 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 NRTK3 (unknown origin) by TR-FRET-based Z'-LYTE assay | B | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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) by TR-FRET-based Z'-LYTE assay | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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 G2032R mutant (unknown origin) | B | 7.92 | pKi | 12 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| ChEMBL | Inhibition of ROS1 L2026M mutant (unknown origin) | B | 10 | pKi | 0.1 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| ChEMBL | Inhibition of wild type ROS1 (unknown origin) | B | 10.6 | pKi | <0.03 | nM | Ki | Eur J Med Chem (2017) 134: 348-356 [PMID:28431340] |
| ChEMBL | Inhibition of ROS1 (unknown origin) | B | 10.6 | pKi | <0.03 | nM | Ki | ACS Med Chem Lett (2018) 9: 878-883 [PMID:30258534] |
| ChEMBL | Inhibition of ROS1 (unknown origin) by off-chip mobility shift assay | B | 10.7 | pKi | <0.02 | nM | Ki | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| GtoPdb | - | - | 11.3 | pKi | 0 | nM | Ki | Mol Cancer Ther (2013) : A277 |
| 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) by TR-FRET-based Z'-LYTE assay | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| 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) by TR-FRET-based Z'-LYTE assay | B | 8.48 | pIC50 | 3.3 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase FES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332] | ||||||||
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2014) 57: 4720-44 [PMID:24819116] |
| ChEMBL | Inhibition of FES (unknown origin) by TR-FRET-based Z'-LYTE assay | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
| fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685] | ||||||||
| ChEMBL | Inhibition of FRK (unknown origin) by TR-FRET-based Z'-LYTE assay | B | 7.28 | pIC50 | 53 | nM | IC50 | J Med Chem (2014) 57: 4720-4744 [PMID:24819116] |
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]
