Reaction Details |
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Target | Histone-arginine methyltransferase CARM1 |
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Ligand | BDBM27659 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_500555 (CHEMBL971420) |
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IC50 | 80±n/a nM |
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Citation | Huynh, T; Chen, Z; Pang, S; Geng, J; Bandiera, T; Bindi, S; Vianello, P; Roletto, F; Thieffine, S; Galvani, A; Vaccaro, W; Poss, MA; Trainor, GL; Lorenzi, MV; Gottardis, M; Jayaraman, L; Purandare, AV Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1). Bioorg Med Chem Lett19:2924-7 (2009) [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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BDBM27659 |
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n/a |
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Name | BDBM27659 |
Synonyms: | 1-(3-{[(2S)-2-aminopropanamido]methyl}phenyl)-N-benzyl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide | CHEMBL466658 | pyrazole scaffold, 1a |
Type | Small organic molecule |
Emp. Form. | C22H22F3N5O2 |
Mol. Mass. | 445.4376 |
SMILES | C[C@H](N)C(=O)NCc1cccc(c1)-n1nc(cc1C(=O)NCc1ccccc1)C(F)(F)F |r| |
Structure |
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