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 |