Reaction Details
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Histone-arginine methyltransferase CARM1
Ligand
BDBM178101
Substrate
n/a
Meas. Tech.
PRMT Biochemical Assays
Ki
>37500±0.0 nM
IC50
>75000±0.0 nM
Citation
Eram, MS; Shen, Y; Szewczyk, MM; Wu, H; Senisterra, G; Li, F; Butler, KV; Kaniskan, Hÿ; Speed, BA; Dela Seña, C; Dong, A; Zeng, H; Schapira, M; Brown, PJ; Arrowsmith, CH; Barsyte-Lovejoy, D; Liu, J; Vedadi, M; Jin, J A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol 11:772-81 (2016) [PubMed] Article More Info.:
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:
BDBM178101
Synonyms:
N1-Methyl-N1-((5-(3-(trifluoromethyl)phenyl)-2H-1,2,3-triazol-4-yl)methyl)ethane-1,2-diamine (Compound 1)
Type:
Small organic molecule
Emp. Form.:
C13H16F3N5
Mol. Mass.:
299.2948
SMILES:
CN(CCN)Cc1n[nH]nc1-c1cccc(c1)C(F)(F)F
Structure:
