| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-arginine methyltransferase CARM1 |
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| Ligand | BDBM27650 |
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| Substrate/Competitor | Histone H3 |
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| Meas. Tech. | Inhibition of CARM-1 Enzymatic Activity |
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| pH | 9±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 220±n/a nM |
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| Citation |  Allan, M; Manku, S; Therrien, E; Nguyen, N; Styhler, S; Robert, MF; Goulet, AC; Petschner, AJ; Rahil, G; Robert Macleod, A; Déziel, R; Besterman, JM; Nguyen, H; Wahhab, A N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1). Bioorg Med Chem Lett19:1218-23 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Histone-arginine methyltransferase CARM1 |
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| Name: | Histone-arginine methyltransferase CARM1 |
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| Synonyms: | CARM1_MOUSE | Carm1 | Coactivator-associated arginine methyltransferase 1 | Histone-Arginine Methyltransferase CARM1 | Prmt4 | Protein arginine N-methyltransferase 4 |
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| Type: | Homodimer; chromatin regulator; methyltransferase |
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| Mol. Mass.: | 65855.95 |
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| Organism: | Mus musculus (mouse) |
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| Description: | Assays were using N-terminal His-tagged, recombinant mouse CARM1 (expressed in Sf9 cells and purified using Ni-NTA agarose chromatography). |
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| Residue: | 608 |
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| Sequence: | MAAAAATAVGPGAGSAGVAGPGGAGPCATVSVFPGARLLTIGDANGEIQRHAEQQALRLE
VRAGPDAAGIALYSHEDVCVFKCSVSRETECSRVGRQSFIITLGCNSVLIQFATPHDFCS
FYNILKTCRGHTLERSVFSERTEESSAVQYFQFYGYLSQQQNMMQDYVRTGTYQRAILQN
HTDFKDKIVLDVGCGSGILSFFAAQAGARKIYAVEASTMAQHAEVLVKSNNLTDRIVVIP
GKVEEVSLPEQVDIIISEPMGYMLFNERMLESYLHAKKYLKPSGNMFPTIGDVHLAPFTD
EQLYMEQFTKANFWYQPSFHGVDLSALRGAAVDEYFRQPVVDTFDIRILMAKSVKYTVNF
LEAKEGDLHRIEIPFKFHMLHSGLVHGLAFWFDVAFIGSIMTVWLSTAPTEPLTHWYQVR
CLFQSPLFAKAGDTLSGTCLLIANKRQSYDISIVAQVDQTGSKSSNLLDLKNPFFRYTGT
TPSPPPGSHYTSPSENMWNTGSTYNLSSGVAVAGMPTAYDLSSVIAGGSSVGHNNLIPLA
NTGIVNHTHSRMGSIMSTGIVQGSSGAQGGGGSSSAHYAVNNQFTMGGPAISMASPMSIP
TNTMHYGS
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| BDBM27650 |
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| Histone H3 |
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| Name: | Histone H3 |
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| 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 |
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| Type: | Other Protein Type |
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| Mol. Mass.: | 15409.01 |
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| Organism: | Mus musculus (mouse) |
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| Description: | Tritiated S-Adenosyl-Methionine (SAM) was used as a methyl donor co-factor. |
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| Residue: | 136 |
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| Sequence: | MARTKQTARKSTGGKAPRKQLATKAARKSAPATGGVKKPHRYRPGTVALREIRRYQKSTE
LLIRKLPFQRLVREIAQDFKTDLRFQSSAVMALQEASEAYLVGLFEDTNLCAIHAKRVTI
MPKDIQLARRIRGERA
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