Reaction Details
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Protein arginine N-methyltransferase 8
Ligand
BDBM178101
Substrate
n/a
Meas. Tech.
PRMT Biochemical Assays
Ki
1500±250 nM
IC50
3000±500 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:
Protein arginine N-methyltransferase 8
Synonyms:
ANM8_HUMAN | HRMT1L3 | HRMT1L3 | HRMT1L4 | Heterogeneous nuclear ribonucleoprotein methyltransferase-like protein 4 | PRMT8 | Protein arginine N-methyltransferase 8 | Protein arginine N-methyltransferase 8 (PRMT8) | Protein arginine methyltransferase 8 (PRMT8)
Type:
Protein
Mol. Mass.:
45293.70
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
394
Sequence:
MGMKHSSRCLLLRRKMAENAAESTEVNSPPSQPPQPVVPAKPVQCVHHVSTQPSCPGRGKMSKLLNPEEMTSRDYYFDSYAHFGIHEEMLKDEVRTLTYRNSMYHNKHVFKDKVVLDVGSGTGILSMFAAKAGAKKVFGIECSSISDYSEKIIKANHLDNIITIFKGKVEEVELPVEKVDIIISEWMGYCLFYESMLNTVIFARDKWLKPGGLMFPDRAALYVVAIEDRQYKDFKIHWWENVYGFDMTCIRDVAMKEPLVDIVDPKQVVTNACLIKEVDIYTVKTEELSFTSAFCLQIQRNDYVHALVTYFNIEFTKCHKKMGFSTAPDAPYTHWKQTVFYLEDYLTVRRGEEIYGTISMKPNAKNVRDLDFTVDLDFKGQLCETSVSNDYKMR
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:
