WZ4002 [Ligand Id: 9176] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1229592
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • cathepsin C/Dipeptidyl peptidase I in Human [ChEMBL: CHEMBL2252] [GtoPdb: 2344] [UniProtKB: P53634]
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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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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Mouse [ChEMBL: CHEMBL3099] [GtoPdb: 1923] [UniProtKB: P00520]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • erb-b2 receptor tyrosine kinase 4 in Human [GtoPdb: 1799] [UniProtKB: Q15303]
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  • BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451]
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  • Bruton tyrosine kinase in Human [GtoPdb: 1948] [UniProtKB: Q06187]
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  • IL2 inducible T cell kinase in Human [GtoPdb: 2046] [UniProtKB: Q08881]
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  • NUAK family kinase 1 in Human [GtoPdb: 2129] [UniProtKB: O60285]
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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 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 6 pIC50 990 nM IC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
cathepsin C/Dipeptidyl peptidase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2252] [GtoPdb: 2344] [UniProtKB: P53634]
ChEMBL Inhibition of CatL-activated recombinant human C-terminal His10-tagged cathepsin C (25 to 463 residues) expressed in mouse myeloma cells using Gly-Phe-AFC as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins B 5.68 pIC50 2100 nM IC50 J Med Chem (2019) 62: 5901-5919 [PMID:31145622]
ChEMBL Inhibition of cathepsin C (unknown origin) B 5.68 pIC50 2100 nM IC50 J Med Chem (2019) 62: 5901-5919 [PMID:31145622]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Binding affinity to EGFR B 7.34 pKd 46 nM Kd J. Med. Chem. (2012) 55: 2711-2723 [PMID:22339342]
GtoPdb - - 7.34 pKd 46 nM Kd Nature (2009) 462: 1070-4 [PMID:20033049]
ChEMBL Binding affinity to EGFR L858R mutant B 7.54 pKd 29 nM Kd J. Med. Chem. (2012) 55: 2711-2723 [PMID:22339342]
ChEMBL Binding affinity to partial length human EGFR L858R/T790M double mutant expressed in mammalian system by KINOMEscan assay B 9.52 pKd 0.3 nM Kd J Med Chem (2016) 59: 6580-6594 [PMID:26882288]
ChEMBL Binding affinity to partial length human EGFR L858R/T790M double mutant expressed in mammalian system by KINOMEscan assay B 9.52 pKd 0.3 nM Kd J Med Chem (2016) 59: 6580-6594 [PMID:26882288]
ChEMBL Inhibition of EGFR in human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay B 4.74 pIC50 18210 nM IC50 Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338]
ChEMBL Inhibition of EGFR E746_A750 deletion/T790M mutant in human growth-resistant PC9 cells assessed as reduction in cell viability after 72 hrs by MTT assay B 5.07 pIC50 8600 nM IC50 Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338]
ChEMBL Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method B 5.69 pIC50 2050 nM IC50 J Med Chem (2017) 60: 4636-4656 [PMID:28482151]
ChEMBL Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay B 5.93 pIC50 1180 nM IC50 J. Med. Chem. (2013) 56: 7025-7048 [PMID:23930994]
ChEMBL Inhibition of wild-type EGFR phosphorylation in human A431 cells preincubated for 1 hr followed by EGF stimulation measured after 45 mins by ELISA B 6.15 pIC50 710 nM IC50 Bioorg Med Chem Lett (2018) 28: 1257-1261 [PMID:29534926]
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 6.92 pIC50 120 nM IC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of EGFR E746_A750 deletion mutant in human PC9 cells assessed as reduction in cell viability after 72 hrs by MTT assay B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338]
ChEMBL Inhibition of wild type recombinant human EGFR preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay B 7.1 pIC50 79 nM IC50 Eur. J. Med. Chem. (2015) 104: 115-126 [PMID:26451770]
ChEMBL Inhibition of EGFR L858R/T790M mutant phosphorylation in human NCI-H1975 cells after 1 hr by ELISA B 7.34 pIC50 46 nM IC50 Bioorg Med Chem Lett (2018) 28: 1257-1261 [PMID:29534926]
ChEMBL Inhibition of wild-type EGFR (unknown origin) expressed in baculovirus expression system after 1 hr by ELISA B 7.51 pIC50 31.1 nM IC50 Bioorg. Med. Chem. (2016) 24: 2673-2680 [PMID:27131639]
ChEMBL Inhibition of human recombinant EGFR T790M/L858R double mutant preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay B 7.51 pIC50 31 nM IC50 Eur. J. Med. Chem. (2015) 104: 115-126 [PMID:26451770]
ChEMBL Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay B 7.64 pIC50 23 nM IC50 J. Med. Chem. (2013) 56: 7025-7048 [PMID:23930994]
ChEMBL Inhibition of recombinant human GST-tagged wild-type EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay B 7.74 pIC50 18 nM IC50 Bioorg Med Chem Lett (2018) 28: 1257-1261 [PMID:29534926]
ChEMBL Inhibition of wild type N-terminal His6-tagged human EGFR kinase domain (702 to 1016 residues) expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. (2015) 23: 2767-2780 [PMID:25975640]
ChEMBL Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay B 8 pIC50 10 nM IC50 J. Med. Chem. (2015) 58: 6844-6863 [PMID:26275028]
ChEMBL Inhibition of EGFR T790M/L858R mutant (unknown origin) expressed in baculovirus expression system after 1 hr by ELISA B 8.01 pIC50 9.7 nM IC50 Bioorg. Med. Chem. (2016) 24: 2673-2680 [PMID:27131639]
ChEMBL Inhibition of wild type EGFR kinase (unknown origin) after 1.5 hrs by FRET-based Z'-Lyte assay B 8.19 pIC50 6.47 nM IC50 MedChemComm (2012) 3: 1155-1159
ChEMBL Inhibition of EGFR L858R/T790M mutant (unknown origin) using Poly(Glu,Tyr)4:1 as substrate incubated for 1 hr by ELISA B 8.19 pIC50 6.4 nM IC50 MedChemComm (2015) 6: 1693-1697
ChEMBL Inhibition of EGFR after 1.5 hr by FRET assay B 8.21 pIC50 6.18 nM IC50 J. Med. Chem. (2012) 55: 2711-2723 [PMID:22339342]
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 8.3 pIC50 5 nM IC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of EGFR (unknown origin) after 1.5 hr by FRET-based Z-lyte assay B 8.36 pIC50 4.4 nM IC50 Eur. J. Med. Chem. (2014) 77: 75-83 [PMID:24607591]
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 8.4 pIC50 4 nM IC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of wild type EGFR (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay B 8.49 pIC50 3.2 nM IC50 J. Med. Chem. (2013) 56: 4738-4748 [PMID:23668441]
ChEMBL Inhibition of wild type EGFR (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay B 8.49 pIC50 3.2 nM IC50 Eur. J. Med. Chem. (2013) 66: 82-90 [PMID:23792318]
ChEMBL Inhibition of recombinant human GST-tagged EGFR L858R/T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2018) 28: 1257-1261 [PMID:29534926]
ChEMBL Inhibition of wild type EGFR (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assay B 8.67 pIC50 2.16 nM IC50 J. Med. Chem. (2013) 56: 7821-7837 [PMID:24053674]
ChEMBL Inhibition of EGFR (unknown origin) using biotin-labelled peptide as substrate preincubated for 2 hrs followed by substrate addition and measured after 30 mins by HTRF FRET assay B 8.77 pIC50 1.7 nM IC50 J Med Chem (2019) 62: 5901-5919 [PMID:31145622]
ChEMBL Inhibition of EGFR L858R mutant (unknown origin) B 8.96 pIC50 1.1 nM IC50 J Med Chem (2017) 60: 4636-4656 [PMID:28482151]
ChEMBL Inhibition of human recombinant GST-tagged EGFR L858R mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 15 mins by HTRF assay B 9 pIC50 <1 nM IC50 J Med Chem (2017) 60: 7725-7744 [PMID:28853575]
ChEMBL Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay B 9 pIC50 <1 nM IC50 J. Med. Chem. (2015) 58: 6844-6863 [PMID:26275028]
ChEMBL Inhibition of human N-terminal GST-fused EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 15 mins by HTFR assay B 9 pIC50 <1 nM IC50 J Med Chem (2017) 60: 5613-5637 [PMID:28603991]
ChEMBL Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 20 mins by HTRF assay B 9 pIC50 <1 nM IC50 J Med Chem (2017) 60: 7725-7744 [PMID:28853575]
ChEMBL Inhibition of human N-terminal GST-fused EGFR T790M/L858R double mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 20 mins by HTFR assay B 9 pIC50 <1 nM IC50 J Med Chem (2017) 60: 5613-5637 [PMID:28603991]
ChEMBL Inhibition of EGFR L858R/T790M mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay B 9.1 pIC50 0.8 nM IC50 Eur. J. Med. Chem. (2013) 66: 82-90 [PMID:23792318]
ChEMBL Inhibition of EGFR L858R/T90M double mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay B 9.1 pIC50 0.8 nM IC50 J. Med. Chem. (2013) 56: 4738-4748 [PMID:23668441]
ChEMBL Inhibition of EGFR L858R/T790M mutant (unknown origin) after 1.5 hr by FRET-based Z-lyte assay B 9.15 pIC50 0.7 nM IC50 Eur. J. Med. Chem. (2014) 77: 75-83 [PMID:24607591]
ChEMBL Inhibition of EGFR T790M/L858R double mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assay B 9.18 pIC50 0.66 nM IC50 J. Med. Chem. (2013) 56: 7821-7837 [PMID:24053674]
ChEMBL Inhibition of EGFR L858R/T790M double mutant (unknown origin) B 9.3 pIC50 <0.5 nM IC50 J Med Chem (2017) 60: 4636-4656 [PMID:28482151]
ChEMBL Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay B 6 pEC50 989 nM EC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay B 7.17 pEC50 68 nM EC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay B 7.51 pEC50 31 nM EC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay B 7.57 pEC50 27 nM EC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ChEMBL Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay B 7.59 pEC50 26 nM EC50 Eur J Med Chem (2017) 136: 497-510 [PMID:28528303]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3099] [GtoPdb: 1923] [UniProtKB: P00520]
ChEMBL Inhibition of ABL T315I mutant in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay B 4.79 pIC50 16280 nM IC50 Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338]
ChEMBL Inhibition of ABL in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay B 5.01 pIC50 9690 nM IC50 Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Binding affinity to JAK3 (unknown origin) B 6.82 pKd 150 nM Kd J. Med. Chem. (2015) 58: 6589-6606 [PMID:26258521]
erb-b2 receptor tyrosine kinase 4 in Human [GtoPdb: 1799] [UniProtKB: Q15303]
GtoPdb - - 7.55 pKd 28 nM Kd Nature (2009) 462: 1070-4 [PMID:20033049]
BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451]
GtoPdb - - 6.7 pKd 200 nM Kd Nature (2009) 462: 1070-4 [PMID:20033049]
Bruton tyrosine kinase in Human [GtoPdb: 1948] [UniProtKB: Q06187]
GtoPdb - - 7.37 pKd 43 nM Kd Nature (2009) 462: 1070-4 [PMID:20033049]
IL2 inducible T cell kinase in Human [GtoPdb: 2046] [UniProtKB: Q08881]
GtoPdb - - 7.37 pKd 43 nM Kd Nature (2009) 462: 1070-4 [PMID:20033049]
NUAK family kinase 1 in Human [GtoPdb: 2129] [UniProtKB: O60285]
GtoPdb - - 7.04 pKd 91 nM Kd Nature (2009) 462: 1070-4 [PMID:20033049]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]