UZH2 [Ligand Id: 13111] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL5077332
  • methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/N6-adenosine-methyltransferase catalytic subunit in Human [ChEMBL: CHEMBL4739695] [GtoPdb: 3181] [UniProtKB: Q86U44]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/N6-adenosine-methyltransferase catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739695] [GtoPdb: 3181] [UniProtKB: Q86U44]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Med Chem (2021) 64: 12738-12760 [PMID:34431664]
ChEMBL Inhibition of recombinant METLL3 (unknown origin) expressed in baculovirus infected Sf9 cells assessed as decrease in N6-methyladenosine level in oligonucleotide substrate by TR-FRET assay B 8.3 pIC50 5 nM IC50 J Med Chem (2021) 64: 12738-12760 [PMID:34431664]
ChEMBL Thermal stabilization of recombinant METTL3 (354 to 580 residues) (unknown origin) expressed in HEK293T cells assessed as non-aggregated METTL3-ePL protein incubated for 1 hr and cells heated 46 degC by luminescence-based InCELL Pulse assay B 5.7 pEC50 2000 nM EC50 J Med Chem (2021) 64: 12738-12760 [PMID:34431664]
ChEMBL Thermal stabilization of endogenously expressing full length METTL3 in human MOLM-13 cells assessed as stabilized METTL3 incubated for at 54 degC by Western blotting based CETSA assay B 6.07 pEC50 850 nM EC50 J Med Chem (2021) 64: 12738-12760 [PMID:34431664]

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]