AC710 [Ligand Id: 8095] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2206278
  • colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
  • colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Mouse [ChEMBL: CHEMBL5570] [GtoPdb: 1806] [UniProtKB: P09581]
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  • colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
GtoPdb - - 8.8 pKd 1.57 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5570] [GtoPdb: 1806] [UniProtKB: P09581]
ChEMBL Inhibition of CSF1R in mouse M-NFS-60 cells assessed as inhibition of cell proliferation after 72 hrs by Celltiter-Blue assay B 7.33 pIC50 46.3 nM IC50 ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
GtoPdb - - 8.8 pKd 1.57 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
ChEMBL Binding affinity to CSF1R expressed in HEK-293 cells after 1 hr B 8.8 pKd 1.57 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
ChEMBL Inhibition of M-CSF-induced FK506 -fussed CSF1R phosphorylation expressed in HEK293 cells after 2 hrs by sandwich ELISA B 7.98 pIC50 10.5 nM IC50 ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Binding affinity to PDGFRalpha expressed in HEK-293 cells B 8.89 pKd 1.3 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
GtoPdb - - 8.89 pKd 1.3 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
ChEMBL Inhibition of PDGFRbeta phosphorylation in human MG63 cells B 8.11 pIC50 7.7 nM IC50 ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
GtoPdb - - 9 pKd 1 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
ChEMBL Binding affinity to PDGFRbeta expressed in HEK-293 cells B 9 pKd 1 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
GtoPdb - - 9 pKd 1 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
ChEMBL Binding affinity to KIT expressed in HEK-293 cells B 9 pKd 1 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
ChEMBL Inhibition of KIT phosphorylation in human H526 cells B 8.92 pIC50 1.2 nM IC50 ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
GtoPdb - - 9.3 pKd 0.5 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
ChEMBL Binding affinity to FLT3 expressed in HEK-293 cells after 1 hr B 9.3 pKd 0.5 nM Kd ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]
ChEMBL Inhibition of FLT3 phosphorylation in human MV4-11 cells B 8.7 pIC50 2 nM IC50 ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421]

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]