PQ401 [Ligand Id: 5048] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL439259 (TCMDC-125497)
  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of recombinant IGF1R by ELISA B 4.73 pIC50 18700 nM IC50 Bioorg Med Chem (2010) 18: 5995-6005 [PMID:20643554]
ChEMBL Inhibition of IGF1R-dependent tumor cell growth in human MCNeuA cells B 4.82 pIC50 15000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of IGF1R autophosphorylation in human MCF7 cells B 4.92 pIC50 12000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of IGF1R autophosphorylation in human MCF7 cells by ELISA B 4.92 pIC50 12000 nM IC50 J Med Chem (2009) 52: 4981-5004 [PMID:19610618]
ChEMBL Inhibition of IGF1R-dependent tumor cell growth in human MCF7 cells B 5.1 pIC50 8000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
GtoPdb - - 6 pIC50 <1000 nM IC50 Mol Cancer Ther (2006) 5: 1079-86 [PMID:16648580]
ChEMBL Inhibition of IGF1R autophosphorylation in human MCF7 cells by Western blot analysis B 6 pIC50 <1000 nM IC50 J Med Chem (2009) 52: 4981-5004 [PMID:19610618]
ChEMBL Inhibition of IGF1R autophosphorylation B 6 pIC50 <1000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against chloroquine-sensetive Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs F 7.28 pEC50 53 nM EC50 ACS Med Chem Lett (2010) 1: 460-465 [PMID:21243104]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs F 6.41 pEC50 390 nM EC50 ACS Med Chem Lett (2010) 1: 460-465 [PMID:21243104]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]