Target
Histone-arginine methyltransferase CARM1
Ligand
BDBM27648
Substrate
Histone H3
Meas. Tech.
Inhibition of CARM-1 Enzymatic Activity
pH
9±n/a
Temperature
295.15±n/a K
IC50
>10000±n/a nM
Citation
 Allan, MManku, STherrien, ENguyen, NStyhler, SRobert, MFGoulet, ACPetschner, AJRahil, GRobert Macleod, ADéziel, RBesterman, JMNguyen, HWahhab, A N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1). Bioorg Med Chem Lett 19:1218-23 (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:
BDBM27648
Synonyms:
1-(2-{[(2S)-2-aminopropanamido]methyl}-1-benzofuran-7-yl)-N-[(2-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide | pyrazole scaffold, 29
Type:
Small organic molecule
Emp. Form.:
C25H24F3N5O4
Mol. Mass.:
515.4844
SMILES:
COc1ccccc1CNC(=O)c1cc(nn1-c1cccc2cc(CNC(=O)[C@H](C)N)oc12)C(F)(F)F |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H3
Synonyms:
H3-143 | H3-53 | H3-B | H3-F | H3.2 | H3.2-221 | H3.2-614 | H3.2-615 | H3.2-616 | H32_MOUSE | H3b | H3c2 | H3f | Hist1h3b | Hist1h3c | Hist1h3d | Hist1h3e | Hist1h3f | Hist2h3b | Hist2h3c1 | Hist2h3c2 | Hist2h3ca1 | Hist2h3ca2
Type:
Other Protein Type
Mol. Mass.:
15409.01
Organism:
Mus musculus (mouse)
Description:
Tritiated S-Adenosyl-Methionine (SAM) was used as a methyl donor co-factor.
Residue:
136
Sequence:
MARTKQTARKSTGGKAPRKQLATKAARKSAPATGGVKKPHRYRPGTVALREIRRYQKSTELLIRKLPFQRLVREIAQDFKTDLRFQSSAVMALQEASEAYLVGLFEDTNLCAIHAKRVTIMPKDIQLARRIRGERA