linsitinib [Ligand Id: 7423] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1091644 (Linsitinib, ASP-7487, OSI-906, OSI-906AA)
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
There should be some charts here, you may need to enable JavaScript!
  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
There should be some charts here, you may need to enable JavaScript!
  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
There should be some charts here, you may need to enable JavaScript!
  • Insulin receptor-related receptor in Human [GtoPdb: 1802] [UniProtKB: P14616]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of recombinant EGFR (unknown origin) using poly-GT peptide as substrate by Transcreener assay B 4.9 pIC50 >12500 nM IC50 ACS Med. Chem. Lett. (2014) 5: 298-303 [PMID:24900830]
ChEMBL Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2452-2455 [PMID:20346655]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Inhibition of recombinant c-MET (unknown origin) using poly-AEKY peptide as substrate after 60 mins by ADPGlo assay B 4.9 pIC50 >12500 nM IC50 ACS Med. Chem. Lett. (2014) 5: 298-303 [PMID:24900830]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
GtoPdb Biochemical enzyme inhibition assay. - 7.46 pIC50 35 nM IC50 Future Med Chem (2009) 1: 1153-71 [PMID:21425998]
ChEMBL Inhibition of human IGF1R expressed in mouse 3T3 cells by ELISA based assay B 7.62 pIC50 24 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1176-1180 [PMID:21251824]
ChEMBL Inhibition of full length human IGF-1R overexpressed in mouse NIH 3T3 cells assessed as IGF1-induced protein phosphorylation incubated for 2 hrs prior to IGF1 induction measured after 15 mins by ELISA B 7.62 pIC50 24 nM IC50 ACS Med. Chem. Lett. (2013) 4: 627-631 [PMID:24900721]
ChEMBL Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA B 7.74 pIC50 18 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2452-2455 [PMID:20346655]
ChEMBL Inhibition of IGF-1 receptor (unknown origin) in presence of [gamma33P]ATP B 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2057-2064 [PMID:26951753]
ChEMBL Inhibition of GST-tagged IGF-1R catalytic domain (unknown origin) using omnia Y peptide-12 as substrate assessed as inhibition of substrate phosphorylation preincubated for 24 hrs prior to substrate addition by fluorescence assay B 7.89 pIC50 13 nM IC50 ACS Med. Chem. Lett. (2013) 4: 627-631 [PMID:24900721]
ChEMBL Inhibition of GST-tagged IGF-1R catalytic domain (unknown origin) using omnia Y peptide-12 as substrate assessed as inhibition of substrate phosphorylation by fluorescence assay B 7.92 pIC50 12 nM IC50 ACS Med. Chem. Lett. (2013) 4: 627-631 [PMID:24900721]
ChEMBL Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation B 8.12 pIC50 7.6 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2057-2064 [PMID:26951753]
ChEMBL Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis B 8.55 pIC50 2.8 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2057-2064 [PMID:26951753]
ChEMBL Inhibition of IGF1R (unknown origin) using poly-G1 as substrate incubated for 10 mins prior to substrate addition measured after 1 hr by time-resolved fluorescence assay B 8.7 pIC50 2 nM IC50 Eur. J. Med. Chem. (2015) 92: 246-256 [PMID:25559205]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation B 6.9 pIC50 126 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2057-2064 [PMID:26951753]
GtoPdb In a kinase screening selectivity assay. - 7.12 pIC50 75 nM IC50 Future Med Chem (2009) 1: 1153-71 [PMID:21425998]
ChEMBL Inhibition of insulin receptor (unknown origin) in presence of [gamma33P]ATP B 7.47 pIC50 34 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2057-2064 [PMID:26951753]
ChEMBL Inhibition of recombinant INSR (unknown origin) using fluorescent dye-labelled KKSRGDYMTMQIG peptide peptide as substrate after 1 hr by IMAP assay B 7.74 pIC50 18 nM IC50 ACS Med. Chem. Lett. (2014) 5: 298-303 [PMID:24900830]
ChEMBL Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2057-2064 [PMID:26951753]
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL Antimalarial activity: Liver Stage Plasmodium berghei sporozoite Luciferase assay IC50 (uM) F 6.44 pIC50 360 nM IC50 MMV Pathogen Box Bioactivity Data
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity: Asexual Blood Stage Plasmodium falciparum 3D7 IC50 (uM) F 5.7 pIC50 >2000 nM IC50 MMV Pathogen Box Bioactivity Data
ChEMBL Antimalarial activity: Asexual Blood Stage Plasmodium falciparum Dd2 IC50 (uM) F 5.7 pIC50 >2000 nM IC50 MMV Pathogen Box Bioactivity Data
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2452-2455 [PMID:20346655]
Insulin receptor-related receptor in Human [GtoPdb: 1802] [UniProtKB: P14616]
GtoPdb - - 7.12 pIC50 75 nM IC50 Future Med Chem (2009) 1: 1153-71 [PMID:21425998]

ChEMBL data shown on this page come from version 27:

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]