Target
Histone-arginine methyltransferase CARM1
Ligand
BDBM50511922
Substrate
n/a
Meas. Tech.
ChEMBL_1846164 (CHEMBL4346591)
IC50
51000±n/a nM
Citation
 Shen, YLi, FSzewczyk, MMHalabelian, LPark, KSChau, IDong, AZeng, HChen, HMeng, FBarsyte-Lovejoy, DArrowsmith, CHBrown, PJLiu, JVedadi, MJin, J Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor. J Med Chem 63:5477-5487 (2020) [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:
BDBM50511922
Synonyms:
CHEMBL4539314
Type:
Small organic molecule
Emp. Form.:
C17H21N3O2
Mol. Mass.:
299.3675
SMILES:
CN(CCO)Cc1c[nH]cc1-c1cccc(NC(=O)C=C)c1
Structure:
Search PDB for entries with ligand similarity: