Reaction Details |
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Target | Protein-glutamine gamma-glutamyltransferase 2 |
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Ligand | BDBM185176 |
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Substrate/Competitor | n/a |
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Meas. Tech. | TG Activity Assays |
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IC50 | 775± 35 nM |
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Citation | Badarau, E; Wang, Z; Rathbone, DL; Costanzi, A; Thibault, T; Murdoch, CE; El Alaoui, S; Bartkeviciute, M; Griffin, M Development of Potent and Selective Tissue Transglutaminase Inhibitors: Their Effect on TG2 Function and Application in Pathological Conditions. Chem Biol22:1347-61 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein-glutamine gamma-glutamyltransferase 2 |
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Name: | Protein-glutamine gamma-glutamyltransferase 2 |
Synonyms: | Protein-glutamine gamma-glutamyltransferase | Protein-glutamine gamma-glutamyltransferase 2 (TG2) | TGM2 | TGM2_HUMAN | Tissue transglutaminase | Tissue transglutaminase (TG2) | Transglutaminase 2 (TGM2) | Transglutaminase C | Transglutaminase-2 |
Type: | Protein |
Mol. Mass.: | 77309.30 |
Organism: | Homo sapiens (Human) |
Description: | P21980 |
Residue: | 687 |
Sequence: | MAEELVLERCDLELETNGRDHHTADLCREKLVVRRGQPFWLTLHFEGRNYEASVDSLTFS
VVTGPAPSQEAGTKARFPLRDAVEEGDWTATVVDQQDCTLSLQLTTPANAPIGLYRLSLE
ASTGYQGSSFVLGHFILLFNAWCPADAVYLDSEEERQEYVLTQQGFIYQGSAKFIKNIPW
NFGQFEDGILDICLILLDVNPKFLKNAGRDCSRRSSPVYVGRVVSGMVNCNDDQGVLLGR
WDNNYGDGVSPMSWIGSVDILRRWKNHGCQRVKYGQCWVFAAVACTVLRCLGIPTRVVTN
YNSAHDQNSNLLIEYFRNEFGEIQGDKSEMIWNFHCWVESWMTRPDLQPGYEGWQALDPT
PQEKSEGTYCCGPVPVRAIKEGDLSTKYDAPFVFAEVNADVVDWIQQDDGSVHKSINRSL
IVGLKISTKSVGRDEREDITHTYKYPEGSSEEREAFTRANHLNKLAEKEETGMAMRIRVG
QSMNMGSDFDVFAHITNNTAEEYVCRLLLCARTVSYNGILGPECGTKYLLNLNLEPFSEK
SVPLCILYEKYRDCLTESNLIKVRALLVEPVINSYLLAERDLYLENPEIKIRILGEPKQK
RKLVAEVSLQNPLPVALEGCTFTVEGAGLTEEQKTVEIPDPVEAGEEVKVRMDLLPLHMG
LHKLVVNFESDKLKAVKGFRNVIIGPA
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BDBM185176 |
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n/a |
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Name | BDBM185176 |
Synonyms: | [2-[[2-[4-(1-Adamantylmethoxycarbonyl)piperazin-1-yl]-2-oxo-ethyl]amino]-2-oxoethyl]-dimethyl-sulfonium bromide (1f) |
Type | Small organic molecule |
Emp. Form. | C22H36N3O4S |
Mol. Mass. | 438.603 |
SMILES | C[S+](C)CC(=O)NCC(=O)N1CCN(CC1)C(=O)OCC12CC3CC(CC(C3)C1)C2 |TLB:23:24:28:22.27.21,27:22:29:26.28.25,27:26:29:23.22.21,THB:23:22:28:29.24.25| |
Structure |
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