Target
Histone-arginine methyltransferase CARM1
Ligand
BDBM50328743
Substrate
n/a
Meas. Tech.
ChEMBL_675522 (CHEMBL1273735)
IC50
2000000±n/a nM
Citation
 Feng, YLi, MWang, BZheng, YG Discovery and mechanistic study of a class of protein arginine methylation inhibitors. J Med Chem 53:6028-39 (2010) [PubMed]  Article
Target
Name:
Histone-arginine methyltransferase CARM1
Synonyms:
CARM1_MOUSE | Carm1 | Coactivator-associated arginine methyltransferase 1 | Histone-Arginine Methyltransferase CARM1 | Prmt4 | Protein arginine N-methyltransferase 4
Type:
Homodimer; chromatin regulator; methyltransferase
Mol. Mass.:
65855.95
Organism:
Mus musculus (mouse)
Description:
Assays were using N-terminal His-tagged, recombinant mouse CARM1 (expressed in Sf9 cells and purified using Ni-NTA agarose chromatography).
Residue:
608
Sequence:
MAAAAATAVGPGAGSAGVAGPGGAGPCATVSVFPGARLLTIGDANGEIQRHAEQQALRLEVRAGPDAAGIALYSHEDVCVFKCSVSRETECSRVGRQSFIITLGCNSVLIQFATPHDFCSFYNILKTCRGHTLERSVFSERTEESSAVQYFQFYGYLSQQQNMMQDYVRTGTYQRAILQNHTDFKDKIVLDVGCGSGILSFFAAQAGARKIYAVEASTMAQHAEVLVKSNNLTDRIVVIPGKVEEVSLPEQVDIIISEPMGYMLFNERMLESYLHAKKYLKPSGNMFPTIGDVHLAPFTDEQLYMEQFTKANFWYQPSFHGVDLSALRGAAVDEYFRQPVVDTFDIRILMAKSVKYTVNFLEAKEGDLHRIEIPFKFHMLHSGLVHGLAFWFDVAFIGSIMTVWLSTAPTEPLTHWYQVRCLFQSPLFAKAGDTLSGTCLLIANKRQSYDISIVAQVDQTGSKSSNLLDLKNPFFRYTGTTPSPPPGSHYTSPSENMWNTGSTYNLSSGVAVAGMPTAYDLSSVIAGGSSVGHNNLIPLANTGIVNHTHSRMGSIMSTGIVQGSSGAQGGGGSSSAHYAVNNQFTMGGPAISMASPMSIPTNTMHYGS
  
Inhibitor
Name:
BDBM50328743
Synonyms:
3-((4-acetamidophenyl)diazenyl)-4-hydroxy-7-(3-(5-hydroxy-6-((E)-phenyldiazenyl)-7-sulfonaphthalen-2-yl)ureido)naphthalene-2-sulfonate | 3-((4-acetamidophenyl)diazenyl)-4-hydroxy-7-(3-(5-hydroxy-6-(phenyldiazenyl)-7-sulfonaphthalen-2-yl)ureido)naphthalene-2-sulfonic acid | CHEMBL1092740 | NSC-47762
Type:
Small organic molecule
Emp. Form.:
C35H27N7O10S2
Mol. Mass.:
769.76
SMILES:
CC(=O)Nc1ccc(cc1)N=Nc1c(O)c2ccc(NC(=O)Nc3ccc4c(O)c(N=Nc5ccccc5)c(cc4c3)S(O)(=O)=O)cc2cc1S(O)(=O)=O |w:31.32,11.12|
Structure:
Search PDB for entries with ligand similarity: