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 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]
