Target
Histone-arginine methyltransferase CARM1
Ligand
BDBM178103
Substrate
n/a
Meas. Tech.
ChEMBL_2146490 (CHEMBL5030836)
IC50
4.0±n/a nM
Citation
 Shen, YLi, FSzewczyk, MMHalabelian, LChau, IEram, MSDela Seña, CPark, KSMeng, FChen, HZeng, HDong, AWu, HTrush, VVMcLeod, DZepeda-Velázquez, CACampbell, RMMader, MMWatson, BMSchapira, MArrowsmith, CHAl-Awar, RBarsyte-Lovejoy, DKaniskan, HÜBrown, PJVedadi, MJin, J A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6. J Med Chem 64:3697-3706 (2021) [PubMed]  Article 
Target
Name:
Histone-arginine methyltransferase CARM1
Synonyms:
CARM1 | CARM1_HUMAN | Coactivator-associated arginine methyltransferase 1 | Coactivator-associated arginine methyltransferase 1 (CARM1) | PRMT4 | Protein arginine N-methyltransferase 4 | Protein arginine methyltransferase 4 (PRMT4)
Type:
Protein
Mol. Mass.:
65855.47
Organism:
Homo sapiens (Human)
Description:
Q86X55
Residue:
608
Sequence:
MAAAAAAVGPGAGGAGSAVPGGAGPCATVSVFPGARLLTIGDANGEIQRHAEQQALRLEVRAGPDSAGIALYSHEDVCVFKCSVSRETECSRVGKQSFIITLGCNSVLIQFATPNDFCSFYNILKTCRGHTLERSVFSERTEESSAVQYFQFYGYLSQQQNMMQDYVRTGTYQRAILQNHTDFKDKIVLDVGCGSGILSFFAAQAGARKIYAVEASTMAQHAEVLVKSNNLTDRIVVIPGKVEEVSLPEQVDIIISEPMGYMLFNERMLESYLHAKKYLKPSGNMFPTIGDVHLAPFTDEQLYMEQFTKANFWYQPSFHGVDLSALRGAAVDEYFRQPVVDTFDIRILMAKSVKYTVNFLEAKEGDLHRIEIPFKFHMLHSGLVHGLAFWFDVAFIGSIMTVWLSTAPTEPLTHWYQVRCLFQSPLFAKAGDTLSGTCLLIANKRQSYDISIVAQVDQTGSKSSNLLDLKNPFFRYTGTTPSPPPGSHYTSPSENMWNTGSTYNLSSGMAVAGMPTAYDLSSVIASGSSVGHNNLIPLANTGIVNHTHSRMGSIMSTGIVQGSSGAQGSGGGSTSAHYAVNSQFTMGGPAISMASPMSIPTNTMHYGS
  
Inhibitor
Name:
BDBM178103
Synonyms:
MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1H-pyrrol-3-yl)methyl)-N1-methylethane-1,2-diamine
Type:
Small organic molecule
Emp. Form.:
C17H25N3O
Mol. Mass.:
287.3999
SMILES:
CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN
Structure:
Search PDB for entries with ligand similarity: