ceritinib [Ligand Id: 7397] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2403108 (Ceritinib, LDK378, NVP-LDK378-NX, Zykadia, LDK-378, NVP-LDK-378-NX)
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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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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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
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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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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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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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  • Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
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  • p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177]
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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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  • FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
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  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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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 Binding affinity to wild-type human partial length ALK (I1088 to E1409 residues) expressed in mammalian expression system by KINOMEscan assay B 8.89 pKd 1.3 nM Kd Eur J Med Chem (2018) 151: 304-314 [PMID:29627725]
ChEMBL Inhibition of ALK (unknown origin) B 5.43 pKi 3700 nM Ki J Med Chem (2019) 62: 10005-10025 [PMID:31188592]
ChEMBL Inhibition of human N-terminal GST-tagged ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay B 4.04 pIC50 91000 nM IC50 Eur J Med Chem (2018) 158: 322-333 [PMID:30223120]
ChEMBL Inhibition of human N-terminal GST-tagged ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay B 4.46 pIC50 35000 nM IC50 Eur J Med Chem (2018) 158: 322-333 [PMID:30223120]
ChEMBL Inhibition of human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay B 5.54 pIC50 2900 nM IC50 Eur J Med Chem (2018) 158: 322-333 [PMID:30223120]
ChEMBL Inhibition of N-terminal GST-tagged human ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay B 6.7 pIC50 201 nM IC50 Eur J Med Chem (2019) 171: 297-309 [PMID:30927566]
ChEMBL Inhibition of wild-type ALK (unknown origin) B 6.7 pIC50 198 nM IC50 Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain G1202R mutant using srctide as substrate incubated for 1 hr by mobility shift assay B 6.71 pIC50 197 nM IC50 Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532]
ChEMBL Inhibition of ALK F1174L mutant (unknown origin) B 6.94 pIC50 114.3 nM IC50 Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) G1202R mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay B 7.04 pIC50 91 nM IC50 Eur J Med Chem (2018) 143: 123-136 [PMID:29174809]
ChEMBL Inhibition of ALK F1174L mutant auto-phosphorylation in human Kelly cells after 3 hrs by MSD assay B 7.1 pIC50 79 nM IC50 J Med Chem (2019) 62: 2618-2637 [PMID:30789735]
ChEMBL Inhibition of ALK L1196M mutant (unknown origin) using peptide as substrate after 60 mins by HTRF assay B 7.19 pIC50 64 nM IC50 Eur J Med Chem (2016) 123: 80-89 [PMID:27474925]
ChEMBL Inhibition of ALK L1196M mutant (unknown origin) B 7.32 pIC50 47.65 nM IC50 Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443]
ChEMBL Inhibition of TEL-fused ALK (unknown origin) by cell-based assay B 7.39 pIC50 40.7 nM IC50 J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252]
ChEMBL Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cells B 7.39 pIC50 40.7 nM IC50 J. Med. Chem. (2013) 56: 5673-5674 [PMID:23837797]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) L1196M mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay B 7.46 pIC50 35 nM IC50 Eur J Med Chem (2018) 143: 123-136 [PMID:29174809]
ChEMBL Inhibition of ALK L1196M mutant (unknown origin) after 30 mins by HTRF assay B 7.54 pIC50 29 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 1720-1725 [PMID:26923695]
ChEMBL Inhibition of ALK L1196M mutant (unknown origin) by homogeneous time resolved fluorescence assay B 7.54 pIC50 29 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3992-3998 [PMID:26235945]
ChEMBL Inhibition of ALK L1196M mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay B 7.54 pIC50 29 nM IC50 Eur J Med Chem (2017) 126: 536-549 [PMID:27915169]
ChEMBL Inhibition of ALK L1196M mutant (unknown origin) using TK as substrate after 30 mins by HTRF assay B 7.54 pIC50 29 nM IC50 Bioorg Med Chem Lett (2017) 27: 2185-2191 [PMID:28385505]
ChEMBL Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay B 7.59 pIC50 26 nM IC50 J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252]
ChEMBL Inhibition of GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of wild type ALK (unknown origin) using TK as substrate after 30 mins by HTRF assay B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2017) 27: 2185-2191 [PMID:28385505]
ChEMBL Inhibition of wild-type ALK (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2017) 126: 536-549 [PMID:27915169]
ChEMBL Inhibition of wild type ALK (unknown origin) after 30 mins by HTRF assay B 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 1720-1725 [PMID:26923695]
ChEMBL Inhibition of wild type ALK (unknown origin) by homogeneous time resolved fluorescence assay B 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3992-3998 [PMID:26235945]
ChEMBL Inhibition of ALK G1202R mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2017) 126: 536-549 [PMID:27915169]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) S1206Y mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay B 8.34 pIC50 4.6 nM IC50 Eur J Med Chem (2018) 143: 123-136 [PMID:29174809]
ChEMBL Inhibition of ALK (unknown origin) by TR-FRET assay B 8.4 pIC50 3.94 nM IC50 J Med Chem (2019) 62: 10927-10954 [PMID:31419130]
ChEMBL Inhibition of purified ALK (unknown origin) after 60 mins by ELISA kinase assay B 8.47 pIC50 3.4 nM IC50 Eur. J. Med. Chem. (2014) 86: 438-448 [PMID:25200979]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) G1269A mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay B 8.47 pIC50 3.4 nM IC50 Eur J Med Chem (2018) 143: 123-136 [PMID:29174809]
ChEMBL Inhibition of recombinant ALK (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA B 8.47 pIC50 3.4 nM IC50 Eur J Med Chem (2018) 144: 386-397 [PMID:29288940]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain L1196M mutant expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay B 8.51 pIC50 3.1 nM IC50 Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay B 8.54 pIC50 2.9 nM IC50 Eur J Med Chem (2018) 143: 123-136 [PMID:29174809]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) C1156Y mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay B 8.54 pIC50 2.9 nM IC50 Eur J Med Chem (2018) 143: 123-136 [PMID:29174809]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay B 8.57 pIC50 2.7 nM IC50 Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) T1151 insertion mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay B 8.6 pIC50 2.5 nM IC50 Eur J Med Chem (2018) 143: 123-136 [PMID:29174809]
ChEMBL Inhibition of ALK (unknown origin) using peptide as substrate after 60 mins by HTRF assay B 8.64 pIC50 2.3 nM IC50 Eur J Med Chem (2016) 123: 80-89 [PMID:27474925]
ChEMBL Inhibition of N-terminal GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay B 8.64 pIC50 2.3 nM IC50 Eur J Med Chem (2019) 171: 297-309 [PMID:30927566]
ChEMBL Inhibition of EML4-fused ALK (unknown origin) by cell-based assay B 8.66 pIC50 2.2 nM IC50 J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252]
ChEMBL Inhibition of ALK C1156Y mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2017) 126: 536-549 [PMID:27915169]
ChEMBL Inhibition of N-terminal GST-tagged human ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2019) 171: 297-309 [PMID:30927566]
ChEMBL Inhibition of ALK F1174L mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2017) 126: 536-549 [PMID:27915169]
ChEMBL Inhibition of ALK G1269A mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay B 8.85 pIC50 1.4 nM IC50 Eur J Med Chem (2017) 126: 536-549 [PMID:27915169]
ChEMBL Inhibition of ALK (unknown origin) after 60 mins B 9.7 pIC50 0.2 nM IC50 J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252]
ChEMBL Inhibition of ALK (unknown origin) B 9.7 pIC50 0.2 nM IC50 J. Med. Chem. (2013) 56: 5673-5674 [PMID:23837797]
GtoPdb - - 9.7 pIC50 0.2 nM IC50 J Med Chem (2013) 56: 5675-90 [PMID:23742252]
ChEMBL Inhibition of ALK L1152R mutant in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay B 5.46 pEC50 3490 nM EC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of ALK L1152R mutant in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay in presence of osimertinib B 5.49 pEC50 3210 nM EC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 (unknown origin) after 60 mins B 5.4 pIC50 3970 nM IC50 J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Inhibition of CDK4 (unknown origin) after 60 mins B 5.33 pIC50 4720 nM IC50 J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay B 3 pIC50 >1000000 nM IC50 Eur J Med Chem (2018) 158: 322-333 [PMID:30223120]
ChEMBL Inhibition of wild type GST-tagged human EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay B 5.67 pIC50 2156 nM IC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2018) 143: 123-136 [PMID:29174809]
ChEMBL Inhibition of N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2019) 171: 297-309 [PMID:30927566]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) cytoplasmic domain expressed in baculovirus expression system using Srctide as substrate incubated for 1 hr by mobility shift assay B 6 pIC50 >1000 nM IC50 Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532]
ChEMBL Inhibition of EGFR (unknown origin) using peptide as substrate after 60 mins by HTRF assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2016) 123: 80-89 [PMID:27474925]
ChEMBL Inhibition of EGFR (unknown origin) after 60 mins B 6.05 pIC50 900 nM IC50 J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252]
ChEMBL Inhibition of GST-tagged human EGFR T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay B 7.55 pIC50 28 nM IC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of GST-tagged human EGFR T790M/L858R double mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay B 7.72 pIC50 19