Reaction Details |
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Target | Tyrosine-protein phosphatase non-receptor type 1 [M114V] |
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Ligand | BDBM13814 |
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Substrate/Competitor | BDBM13594 |
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Meas. Tech. | PTP1B and TCPTP Inhibition Assay |
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pH | 6.3±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 45±8 nM |
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Km | 22000±2000 nM |
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Comments | kcat/Km= 120000 M-1s-1 |
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Citation | Asante-Appiah, E; Patel, S; Desponts, C; Taylor, JM; Lau, C; Dufresne, C; Therien, M; Friesen, R; Becker, JW; Leblanc, Y; Kennedy, BP; Scapin, G Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase. J Biol Chem281:8010-5 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Tyrosine-protein phosphatase non-receptor type 1 [M114V] |
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Name: | Tyrosine-protein phosphatase non-receptor type 1 [M114V] |
Synonyms: | PTN1_HUMAN | PTP-1B | PTP1B | PTPN1 | PTPase 1B | Protein-Tyrosine Phosphatase 1B (PTP1B) Mutant (M114V) | Tyrosine-protein phosphatase, non-receptor type 1 |
Type: | Enzyme |
Mol. Mass.: | 34638.59 |
Organism: | Homo sapiens (Human) |
Description: | P18031[M114V] |
Residue: | 298 |
Sequence: | MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLH
QEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVVEKGSLK
CAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWP
DFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKD
PSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHED
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BDBM13814 |
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BDBM13594 |
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Name | BDBM13814 |
Synonyms: | ({4-[(4E)-2-(1H-1,2,3-benzotriazol-1-yl)-2-[4-(methoxycarbonyl)phenyl]-5-phenylpent-4-en-1-yl]phenyl}difluoromethyl)phosphonic acid | benzotriazole phenyldifluoromethylphosphonic acid compound 1 |
Type | Small organic molecule |
Emp. Form. | C32H28F2N3O5P |
Mol. Mass. | 603.5524 |
SMILES | COC(=O)c1ccc(cc1)C(C\C=C\c1ccccc1)(Cc1ccc(cc1)C(F)(F)P(O)(O)=O)n1nnc2ccccc12 |
Structure |
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