JNJ-28312141 [Ligand Id: 5689] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1908842 (JNJ-28312141)
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  • 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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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • RIO kinase 3/Serine/threonine-protein kinase RIO3 in Human [ChEMBL: CHEMBL5659] [GtoPdb: 2188] [UniProtKB: O14730]
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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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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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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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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]astemizole from human ERG potassium channel B 5 pIC50 >10000 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
GtoPdb - - 8.49 pKd 3.2 nM Kd Nat Biotechnol (2011) 29: 1046-51 [PMID:22037378]
GtoPdb - - 9.16 pIC50 0.69 nM IC50 Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542]
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 FMS-mediated proliferation in CSF1-stimulated bone marrow-derived mouse macrophages assessed as inhibition of incorporation of bromodeoxyuridine into the DNA after 30 hrs by ELISA B 8.59 pIC50 2.6 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
GtoPdb - - 8.49 pKd 3.2 nM Kd Nat Biotechnol (2011) 29: 1046-51 [PMID:22037378]
GtoPdb - - 9.16 pIC50 0.69 nM IC50 Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542]
ChEMBL Inhibition of FMS mediated phosphorylation using SYEGNSYTFIDPTQ as substrate after 80 mins by fluorescence polarization B 9.16 pIC50 0.69 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
ChEMBL Inhibition of FMS B 9.16 pIC50 0.69 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Inhibition of TRKA in human TF1 cells assessed as inhibition of NGF-induced cell proliferation after 72 hrs by CellTiter-Glo assay B 6.82 pIC50 150 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
GtoPdb - - 7.82 pIC50 15 nM IC50 Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542]
ChEMBL Inhibition of TRKA B 7.82 pIC50 15 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
RIO kinase 3/Serine/threonine-protein kinase RIO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5659] [GtoPdb: 2188] [UniProtKB: O14730]
ChEMBL Binding affinity to RIOK3 (unknown origin) B 5.7 pKd 2000 nM Kd US-20200216545-A1. Compositions and methods for treating beta-globinopathies (null)
ChEMBL Binding affinity to RIOK3 (unknown origin) B 5.7 pKd 1995.26 nM Kd US-20200216545-A1. Compositions and methods for treating beta-globinopathies (null)
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 KIT in human Mo7e cells assessed as inhibition of SCF-induced cell proliferation after 72 hrs by CellTiter-Glo assay B 7.39 pIC50 41 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
GtoPdb - - 8.3 pIC50 5 nM IC50 Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542]
ChEMBL Inhibition of KIT B 8.3 pIC50 5 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK in human Jurkat cells assessed as inhibition of PMA and antiCD3-induced IL2 secretion after 24 hrs by ELISA B 5.41 pIC50 3900 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
ChEMBL Inhibition of LCK B 7.06 pIC50 88 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
GtoPdb - - 7.06 pIC50 88 nM IC50 Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
GtoPdb - - 7.52 pIC50 30 nM IC50 Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542]
ChEMBL Inhibition of FLT3 B 7.52 pIC50 30 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
ChEMBL Inhibition of FLT3 in human MV411 cells assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay B 7.68 pIC50 21 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Inhibition of AXL overexpressed in human HEK cells assessed as inhibition of GAS6-induced autophosphorylation by immunoblot assay B 5.59 pIC50 2600 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]
ChEMBL Inhibition of AXL B 7.92 pIC50 12 nM IC50 J Med Chem (2011) 54: 7860-7883 [PMID:22039836]

ChEMBL data shown on this page come from version 32:

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]