Reaction Details |
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Target | Histone-arginine methyltransferase CARM1 |
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Ligand | BDBM50598001 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2225428 (CHEMBL5138941) |
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IC50 | 1900±n/a nM |
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Citation | Iannelli, G; Milite, C; Marechal, N; Cura, V; Bonnefond, L; Troffer-Charlier, N; Feoli, A; Rescigno, D; Wang, Y; Cipriano, A; Viviano, M; Bedford, MT; Cavarelli, J; Castellano, S; Sbardella, G Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach. J Med Chem65:11574-11606 (2022) [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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BDBM50598001 |
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n/a |
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Name | BDBM50598001 |
Synonyms: | CHEMBL5196058 |
Type | Small organic molecule |
Emp. Form. | C32H42N8O5 |
Mol. Mass. | 618.7265 |
SMILES | COc1ccc(CCNC(=O)[C@@H](N)CC[C@H](CNCc2ccccc2)C[C@H]2O[C@H]([C@H](O)[C@@H]2O)n2cnc3c(N)ncnc23)cc1 |r| |
Structure |
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