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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]