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| ChEMBL ligand: CHEMBL4573938 |
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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]