lorlatinib [Ligand Id: 7476] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3286830 (Lorlatinib, Lorbrena, PF-06463922)
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
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  • leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
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  • neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
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  • protein tyrosine kinase 2 beta/Protein tyrosine kinase 2 beta in Human [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
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  • c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
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  • tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
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  • FER tyrosine kinase/Tyrosine-protein kinase FER in Human [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
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  • FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase FES in Human [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
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  • fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685]
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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 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) 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 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]