AG-270 [Ligand Id: 14386] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4573938
  • methionine adenosyltransferase 2A/S-adenosylmethionine synthase isoform type-2 in Human [ChEMBL: CHEMBL3313835] [GtoPdb: 3341] [UniProtKB: P31153]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
methionine adenosyltransferase 2A/S-adenosylmethionine synthase isoform type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313835] [GtoPdb: 3341] [UniProtKB: P31153]
ChEMBL Inhibition of MAT2a in wild type human HCT-116 cells assessed as reduction in symmetric dimethyl arginine formation incubated for 48 hrs by Hoechst 33342 staining based fluorescence analysis B 4.5 pIC50 >31622.78 nM IC50 J Med Chem (2024) 67: 4541-4559 [PMID:38466661]
ChEMBL Inhibition of recombinant His6-tagged MAT2A (unknown origin) expressed in SF9 insect cells using L-Met as substrate preincubated for 60 mins followed by substrate and ATP addition and measured after 60 mins by spectrophotometric analysis B 7 pIC50 <100 nM IC50 US-20180079753-A1. Inhibitors of cellular metabolic processes (2018)
GtoPdb - - 7.17 pIC50 68.3 nM IC50 MedComm (2020) (2024) 5: e705 [PMID:39309689]
ChEMBL Inhibition of recombinant MAT2A (unknown origin) expressed in baculovirus infected Sf9 insect cells using L-methionine as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by Kinase-Glo Luminescent assay B 7.34 pIC50 46 nM IC50 J Med Chem (2023) 66: 4849-4867 [PMID:36961373]
ChEMBL Inhibition of human MAT2A B 7.37 pIC50 43 nM IC50 Bioorg Med Chem Lett (2023) 94: 129450-129450 [PMID:37591318]
GtoPdb - - 7.85 pIC50 14 nM IC50 J Med Chem (2021) 64: 4430-4449 [PMID:33829783]
ChEMBL Inhibition of recombinant human MAT2A expressed in baculovirus infected Sf9 cells assessed as S-adenosyl methionine production using L-methionine as substrate incubated for 60 mins followed by substrate addition and measured after 60 mins B 7.85 pIC50 14 nM IC50 J Med Chem (2021) 64: 4430-4449 [PMID:33829783]
ChEMBL Inhibition of MAT2a in human HCT116- MTAP null cells assessed as reduction in symmetric dimethyl arginine formation incubated for 48 hrs by Hoechst 33342 staining based fluorescence analysis B 8 pIC50 10 nM IC50 J Med Chem (2024) 67: 4541-4559 [PMID:38466661]
ChEMBL Inhibition of MAT2a (unknown origin) using methionine and ATP as substrate assessed as reduction in S-adenosyl-L-methionine formation incubated for 300 mins by RapidFire-Mass Spectrometry analysis B 9.4 pIC50 0.4 nM IC50 J Med Chem (2024) 67: 4541-4559 [PMID:38466661]

ChEMBL data shown on this page come from version 36:

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]