compound 1 [PMID: 22795084] [Ligand Id: 7032] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2325441 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678] | ||||||||
| ChEMBL | Binding affinity to 6xHis-tagged recombinant human PRMT3 by surface plasmon resonance analysis | B | 5.02 | pKd | 9500 | nM | Kd | J Med Chem (2015) 58: 1596-1629 [PMID:25406853] |
| GtoPdb | IC50 was measured using a SAHH (S-adenosylhomocysteine hydrolase)-coupled in vitro assay. | - | 5.6 | pIC50 | 2500 | nM | IC50 | Structure (2012) 20: 1425-35 [PMID:22795084] |
| ChEMBL | Inhibition of full length PRMT3 (unknown origin) using biotinylated histone H4 as substrate after 60 mins in presence of [3H]S-adenosylmethionine by scintillation proximity assay | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2018) 61: 1204-1217 [PMID:29244490] |
| ChEMBL | Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (2013) 56: 2110-2124 [PMID:23445220] |
| ChEMBL | Inhibition of recombinant human PRMT3 (211 to 531) using histone-4 (1 to 24) as substrate by S-adenosylhomocysteine hydrolase-coupled assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2015) 58: 1596-1629 [PMID:25406853] |
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]
