AGL 2043 [Ligand Id: 5918] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2218927
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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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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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Mouse [ChEMBL: CHEMBL3074] [GtoPdb: 2206] [UniProtKB: P05480]
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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 EGFR in human A431 cells incubated for 2 hrs followed by EGF stimulation and measured after 10 mins by immunoblot assay B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem (2019) 27: 16-35 [PMID:30502116]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of IGFR1 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem (2019) 27: 16-35 [PMID:30502116]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Inhibition of human PDGFR beta B 7.05 pIC50 90 nM IC50 Bioorg Med Chem (2019) 27: 16-35 [PMID:30502116]
GtoPdb Using purified human PDGFRβ - 7.05 pIC50 90 nM IC50 Bioorg Med Chem (2003) 11: 2007-18 [PMID:12670652]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of c-KIT in human M-07e cells assessed as reduction in tyrphostin activity incubated for 2 hrs followed by KIT ligand stimulation by immunoblotting analysis B 6 pIC50 1000 nM IC50 Bioorg Med Chem (2019) 27: 16-35 [PMID:30502116]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of human FLT3 expressed in mouse BAF3 cells assessed as reduction in tyrphostin activity incubated for 2 hrs followed by FLT3 ligand stimulation by immunoblot analysis B 6 pIC50 1000 nM IC50 Bioorg Med Chem (2019) 27: 16-35 [PMID:30502116]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3074] [GtoPdb: 2206] [UniProtKB: P05480]
ChEMBL Inhibition of SRC in transformed mouse NIH3T3 cells by SDS-PAGE based immunoblot assay B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem (2019) 27: 16-35 [PMID:30502116]

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]