| Method | Compound | Target | Secondary Assays |
|---|---|---|---|
| Radiotracer Assays | |||
| Filter Binding | Chaetocin [6] | SU(VAR)3-9 | Biochemical and cellular immunoblot, MS |
| Pyrazole Amide 7b [68] | PRMT4 | PRMT1, PRMT3 selectivity (filter binding) | |
| [14C]-Labeling | Sinefungin [69] | N.D. | N.D. |
| Antibody-Based Assays | |||
| DELFIA | BIX-01294, BIX-01338 [13, 32] | G9a, GLP | MS, Cellular expression analysis, ChIP |
| ELISA | AMI-1, AMI-5 [12] | Hmt1p, PRMT1 | Filter binding, ERα-reporter gene assay |
| Coupled Enzyme Assays | |||
| FDH-Coupled | Myricetin, β-lapachone [45] | JMJD2E | MS |
| 8-hydroxyquinolines [43] | JMJD2E, 2A | MS, FRAP | |
| Mass Spectrometry (MS) | |||
| Disulfiram or selenium derivatives [70] | JMJD2A | Zn(II)-ejection assay | |
| Fluorescence Polarization (FP) | |||
| Stilbamidine, allantodapsone, RM-65 [14, 71] | RmtA, PRMT1 | TRF, ERα -reporter gene assay, cellular IHC | |
| Crystallography/Modeling/Virtual Screening | |||
| UNC-0321 [17] | G9a, GLP | SAHH-coupled assay, AlphaScreen, FP, MCE | |
| E70 [72] | GLP | MS, ITC, cellular expression analysis | |
| Tranylcypromine-Lys conjugates [73] | LSD1 | HRP-coupled assay, cellular immunoblot | |
| 2,4-PDCA [33] | JMJD2E, 2A | FDH-coupled assay, MS, crystallography | |
| 4-dimethyl-amino-benzyl-NOG [74] | JMJD2A, 2C, 2D | Biochemical and cellular immunoblot | |
| N-oxalyl-D-tyrosine derivatives [75] | JMJD2A | MS, FDH-coupled assay, crystallography | |
| Structural or Mechanistic Similarity | |||
| Tranylcypromine [48] | LSD1 | Immunoblot, ChIP, transcriptional analysis | |
| Lys4-cyclopropyl and propargylamine H3 peptide derivatives [50] | LSD1 | HRP-coupled assay, MS | |
| Bisguanidine and biguanide polyamine analogs [54] | LSD1 | Biochemical and cellular immunoblot, transcriptional analysis, ChIP | |
| N-oxalylglycine (NOG) [76] | JMJD2E, 2a, 2B | Immunoblot, FDH-coupled assay | |
| Succinic acid [77] | JMJD2D | Biochemical and cellular immunoblot | |