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

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ChEMBL ligand: CHEMBL3286830 (Lorbrena, Lorlatinib, Lorviqua, PF-06463922)
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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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 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 Binding affinity to ALK L1196M mutant (unknown origin) assessed as inhibition constant B 9.15 pKi 0.7 nM Ki RSC Med Chem (2024) 15: 399-415 [PMID:38389874]
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 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 Affinity Biochemical interaction (Microfluidic mobility shift assay) EUB0000690a ALK B 10.15 pKi <0.07 nM Ki Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
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 Binding affinity to ALK (unknown origin) assessed as inhibition of constant B 10.15 pKi <0.07 nM Ki RSC Med Chem (2024) 15: 399-415 [PMID:38389874]
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 Affinity On-target Cellular interaction (ELISA (ALK phosphoryaltion in 3T3-EML4-ALK engineered cell lines)) EUB0000690a ALK B 8.89 pIC50 1.3 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3
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]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a EGFR B 6.5 pKi 319 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a EGFR B 7.25 pKi 56 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a PTK2 B 7.77 pKi 17 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a LTK B 8.57 pKi 2.7 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a NTRK1 B 7.62 pKi 24 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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]
ChEMBL Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a NTRK2 B 7.64 pKi 23 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
ChEMBL Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a NTRK3 B 7.34 pKi 46 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a PTK2B B 7.85 pKi 14 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 ROS1 L2026M mutant (unknown origin) in presence of ATP by microfluidic mobility shift assay B 10 pKi 0.1 nM Ki J Med Chem (2020) 63: 10726-10741 [PMID:32432477]
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 Affinity Biochemical interaction (Microfluidic mobility shift assay) EUB0000690a ROS1 B 10.6 pKi <0.03 nM Ki Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
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
ChEMBL Affinity On-target Cellular interaction (Sandwich ELISA (cell-based ROS1-fusion assay)) EUB0000690a ROS1 B 9.28 pIC50 <0.53 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Phenotypic Cellular interaction (Free plasma tumor growth inhibition assay) EUB0000690a ROS1 F 8.24 pEC50 5.8 nM EC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
ChEMBL Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a TNK2 B 7.77 pKi 17 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a FER B 8.48 pKi 3.3 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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]
ChEMBL Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a FES B 8.22 pKi 6 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a FRK B 7.28 pKi 53 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Selectivity interaction (Z’-LYTE assay (SelectScreen Invitrogen)) EUB0000690a JAK2 B 6.28 pKi 529 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3

ChEMBL data shown on this page come from version 34:

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]