Reaction Details |
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Target | Histone-arginine methyltransferase CARM1 |
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Ligand | BDBM50158375 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1564179 (CHEMBL3784076) |
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IC50 | 27±n/a nM |
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Citation | Ferreira de Freitas, R; Eram, MS; Szewczyk, MM; Steuber, H; Smil, D; Wu, H; Li, F; Senisterra, G; Dong, A; Brown, PJ; Hitchcock, M; Moosmayer, D; Stegmann, CM; Egner, U; Arrowsmith, C; Barsyte-Lovejoy, D; Vedadi, M; Schapira, M Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor. J Med Chem59:1176-83 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone-arginine methyltransferase CARM1 |
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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: | MAAAAAAVGPGAGGAGSAVPGGAGPCATVSVFPGARLLTIGDANGEIQRHAEQQALRLEV
RAGPDSAGIALYSHEDVCVFKCSVSRETECSRVGKQSFIITLGCNSVLIQFATPNDFCSF
YNILKTCRGHTLERSVFSERTEESSAVQYFQFYGYLSQQQNMMQDYVRTGTYQRAILQNH
TDFKDKIVLDVGCGSGILSFFAAQAGARKIYAVEASTMAQHAEVLVKSNNLTDRIVVIPG
KVEEVSLPEQVDIIISEPMGYMLFNERMLESYLHAKKYLKPSGNMFPTIGDVHLAPFTDE
QLYMEQFTKANFWYQPSFHGVDLSALRGAAVDEYFRQPVVDTFDIRILMAKSVKYTVNFL
EAKEGDLHRIEIPFKFHMLHSGLVHGLAFWFDVAFIGSIMTVWLSTAPTEPLTHWYQVRC
LFQSPLFAKAGDTLSGTCLLIANKRQSYDISIVAQVDQTGSKSSNLLDLKNPFFRYTGTT
PSPPPGSHYTSPSENMWNTGSTYNLSSGMAVAGMPTAYDLSSVIASGSSVGHNNLIPLAN
TGIVNHTHSRMGSIMSTGIVQGSSGAQGSGGGSTSAHYAVNSQFTMGGPAISMASPMSIP
TNTMHYGS
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BDBM50158375 |
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n/a |
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Name | BDBM50158375 |
Synonyms: | CHEMBL3781284 |
Type | Small organic molecule |
Emp. Form. | C24H20F3N7O2 |
Mol. Mass. | 495.4565 |
SMILES | C[C@@H](N)C(=O)NCc1cccc(c1)-n1nc(cc1-c1nnc(o1)-c1cccc2[nH]ccc12)C(F)(F)F |r| |
Structure |
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