Reaction Details Report a problem with these data
Target
Histone-arginine methyltransferase CARM1
Ligand
BDBM50311712
Substrate
n/a
Meas. Tech.
ChEMBL_618689 (CHEMBL1102467)
IC50
>10000±n/a nM
Citation
 Therrien, E; Larouche, G; Manku, S; Allan, M; Nguyen, N; Styhler, S; Robert, MF; Goulet, AC; Besterman, JM; Nguyen, H; Wahhab, A 1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1). Bioorg Med Chem Lett 19:6725-32 (2009) [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:
BDBM50311712
Synonyms:
5-(2-methoxybenzyl)-8-((2-(methylamino)ethylamino)methyl)-2-(trifluoromethyl)pyrazolo[1,5-a]quinoxalin-4(5H)-one | CHEMBL1079704
Type:
Small organic molecule
Emp. Form.:
C23H24F3N5O2
Mol. Mass.:
459.4642
SMILES:
CNCCNCc1ccc2n(Cc3ccccc3OC)c(=O)c3cc(nn3c2c1)C(F)(F)F
Structure:
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