AMI-1 [Ligand Id: 7028] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL221047 (NSC-45174)
  • protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
ChEMBL Binding affinity to human recombinant GST-PRMT1 expressed Escherichia coli BL21 by SPR assay B 6.09 pKd 810 nM Kd J Med Chem (2012) 55: 9875-9890 [PMID:23095008]
ChEMBL Inhibition of human recombinant GST-PRMT1 expressed in BL21 cells B 4.04 pIC50 92000 nM IC50 J Med Chem (2007) 50: 1241-1253 [PMID:17323938]
ChEMBL Inhibition of human GST-tagged PRMT1-mediated arginine methylation expressed in Escherichia coli BL21 (DE3) using H4(1-20) and [14C]-AdoMet by scintillation counting B 4.04 pIC50 91200 nM IC50 J Med Chem (2010) 53: 6028-6039 [PMID:20666457]
ChEMBL Inhibition of histidine tagged recombinant PRMT1 expressed in Escherichia coli BL21 (DE3) cells using Histone H4(1-20) substrate preincubated for 5 mins measured after 8 mins by liquid scintillation counting B 4.11 pIC50 76900 nM IC50 J Med Chem (2012) 55: 7978-7987 [PMID:22928876]
GtoPdb - - 5.06 pIC50 8810 nM IC50 J Biol Chem (2004) 279: 23892-9 [PMID:15056663]
ChEMBL Inhibition of human recombinant PRMT1 by TRF assay B 5.92 pIC50 1200 nM IC50 J Med Chem (2007) 50: 2319-2325 [PMID:17432842]
RmtA in Emericella nidulans (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075069] [UniProtKB: Q5VLE3]
ChEMBL Inhibition of Aspergillus nidulans recombinant GST-RmtA expressed in BL21 cells B 4.06 pIC50 88000 nM IC50 J Med Chem (2007) 50: 1241-1253 [PMID:17323938]
ChEMBL Inhibition of Aspergillus nidulans RmtA by TRF assay B 4.47 pIC50 33800 nM IC50 J Med Chem (2007) 50: 2319-2325 [PMID:17432842]

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]