Reaction Details |
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Target | Amyloid-beta precursor protein |
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Ligand | BDBM50220284 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_449193 (CHEMBL899458) |
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IC50 | 3.5±n/a nM |
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Citation | Josien, H; Bara, T; Rajagopalan, M; Asberom, T; Clader, JW; Favreau, L; Greenlee, WJ; Hyde, LA; Nomeir, AA; Parker, EM; Pissarnitski, DA; Song, L; Wong, GT; Zhang, L; Zhang, Q; Zhao, Z Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors. Bioorg Med Chem Lett17:5330-5 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Amyloid-beta precursor protein |
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Name: | Amyloid-beta precursor protein |
Synonyms: | A4 | A4_HUMAN | ABPP | AD1 | AICD-50 | AICD-57 | AICD-59 | AID(50) | AID(57) | AID(59) | APP | APPI | Alzheimer disease amyloid protein | Amyloid beta A4 protein | Amyloid beta Protein | Amyloid beta protein (sAPPbeta) | Amyloid beta protein Abeta(1-42) | Amyloid intracellular domain 50 | Amyloid intracellular domain 57 | Amyloid intracellular domain 59 | Amyloid protein (Abeta42b) | Amyloid β-protein (Aβ42) | Beta amyloid A4 protein | Beta-APP40 | Beta-APP42 | Beta-amyloid protein 40 | Beta-amyloid protein 42 | C31 | C83 | C99 | CVAP | Cerebral vascular amyloid peptide | Gamma Secretase | Gamma-CTF(50) | Gamma-CTF(57) | Gamma-CTF(59) | Gamma-secretase | Gamma-secretase C-terminal fragment 50 | Gamma-secretase C-terminal fragment 57 | Gamma-secretase C-terminal fragment 59 | P3(40) | P3(42) | PN-II | PreA4 | Protease nexin-II | S-APP-alpha | S-APP-beta | Soluble APP-alpha | Soluble APP-beta | beta-Amyloid Precursor Protein (APP) |
Type: | Single-pass type I membrane protein |
Mol. Mass.: | 86890.41 |
Organism: | Homo sapiens (Human) |
Description: | P05067 |
Residue: | 770 |
Sequence: | MLPGLALLLLAAWTARALEVPTDGNAGLLAEPQIAMFCGRLNMHMNVQNGKWDSDPSGTK
TCIDTKEGILQYCQEVYPELQITNVVEANQPVTIQNWCKRGRKQCKTHPHFVIPYRCLVG
EFVSDALLVPDKCKFLHQERMDVCETHLHWHTVAKETCSEKSTNLHDYGMLLPCGIDKFR
GVEFVCCPLAEESDNVDSADAEEDDSDVWWGGADTDYADGSEDKVVEVAEEEEVAEVEEE
EADDDEDDEDGDEVEEEAEEPYEEATERTTSIATTTTTTTESVEEVVREVCSEQAETGPC
RAMISRWYFDVTEGKCAPFFYGGCGGNRNNFDTEEYCMAVCGSAMSQSLLKTTQEPLARD
PVKLPTTAASTPDAVDKYLETPGDENEHAHFQKAKERLEAKHRERMSQVMREWEEAERQA
KNLPKADKKAVIQHFQEKVESLEQEAANERQQLVETHMARVEAMLNDRRRLALENYITAL
QAVPPRPRHVFNMLKKYVRAEQKDRQHTLKHFEHVRMVDPKKAAQIRSQVMTHLRVIYER
MNQSLSLLYNVPAVAEEIQDEVDELLQKEQNYSDDVLANMISEPRISYGNDALMPSLTET
KTTVELLPVNGEFSLDDLQPWHSFGADSVPANTENEVEPVDARPAADRGLTTRPGSGLTN
IKTEEISEVKMDAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIATVIVITL
VMLKKKQYTSIHHGVVEVDAAVTPEERHLSKMQQNGYENPTYKFFEQMQN
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BDBM50220284 |
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n/a |
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Name | BDBM50220284 |
Synonyms: | 1-((2R,6R)-1-(4-chlorophenylsulfonyl)-6-ethylpiperidin-2-yl)cyclopropyl 4-(piperidin-1-yl)piperidine-1-carboxylate | CHEMBL239859 |
Type | Small organic molecule |
Emp. Form. | C27H40ClN3O4S |
Mol. Mass. | 538.142 |
SMILES | CC[C@@H]1CCC[C@@H](N1S(=O)(=O)c1ccc(Cl)cc1)C1(CC1)OC(=O)N1CCC(CC1)N1CCCCC1 |
Structure |
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