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

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ChEMBL ligand: CHEMBL1091644 (Linsitinib, ASP-7487, OSI-906, OSI-906AA)
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
  • This target only has 0 pki data point
  • 0
1 CHEMBL1091644_lig_chart_1 ATP-binding cassette sub-family G member 2 Human
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
  • This target only has 0 pki data point
  • 0
2 CHEMBL1091644_lig_chart_2 Epidermal growth factor receptor erbB1 Human
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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
  • This target only has 0 pki data point
  • 0
3 CHEMBL1091644_lig_chart_3 Hepatocyte growth factor receptor Human
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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
  • This target only has 0 pki data point
  • 0
4 CHEMBL1091644_lig_chart_4 Insulin-like growth factor I receptor Human
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  • Insulin receptor in Human [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
  • This target only has 0 pki data point
  • 0
5 CHEMBL1091644_lig_chart_5 Insulin receptor Human
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  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • This target only has 0 pki data point
  • 0
6 CHEMBL1091644_lig_chart_6 P-glycoprotein 1 Human
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  • Plasmodium berghei [ChEMBL: CHEMBL612653]
  • This target only has 0 pki data point
  • 0
7 CHEMBL1091644_lig_chart_7 Plasmodium berghei Plasmodium berghei
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
8 CHEMBL1091644_lig_chart_8 Plasmodium falciparum Plasmodium falciparum
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
  • This target only has 0 pki data point
  • 0
9 CHEMBL1091644_lig_chart_9 Receptor protein-tyrosine kinase erbB-2 Human
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  • Insulin receptor-related receptor in Human [GtoPdb: 1802] [UniProtKB: P14616]
  • This target only has 0 pki data point
  • 0
10 CHEMBL1091644_lig_chart_10 Insulin receptor-related receptor Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of ABCG2 (unknown origin) expressed in MDCK2 cells co-expressing BCRP (unknown origin) assessed as potentiation of SN-38-induced cytotoxicity measured after 72 hrs by MTT assay B 6.98 pEC50 104 nM EC50 Eur J Med Chem (2019) 164: 193-213 [PMID:30594677]
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]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assay B 5.68 pEC50 2090 nM EC50 Eur J Med Chem (2019) 164: 193-213 [PMID:30594677]
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 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]