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Target
Isoform APP695 of Amyloid-beta precursor protein [K595N,M596L]
Ligand
BDBM476539
Substrate
n/a
Meas. Tech.
Cellular gamma-Secretase Assay
EC50
38.5±n/a nM
Citation
 Bartels, B; Jakob-Roetne, R; Limberg, A; Neidhart, W; Ratni, H; Rodriguez Sarmiento, RM Triazolopyridines US Patent  US10875854 Publication Date 12/29/2020 
Target
Name:
Isoform APP695 of Amyloid-beta precursor protein [K595N,M596L]
Synonyms:
A4 | A4_HUMAN | AD1 | APP | Amyloid-beta precursor protein | Amyloid-beta precursor protein (PreA4 695) [K595N,M596L] | Isoform APP695 (K595N,M596L)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
78580.06
Organism:
Homo sapiens (Human)
Description:
P05067-4(K595N,M596L)
Residue:
695
Sequence:
MLPGLALLLLAAWTARALEVPTDGNAGLLAEPQIAMFCGRLNMHMNVQNGKWDSDPSGTKTCIDTKEGILQYCQEVYPELQITNVVEANQPVTIQNWCKRGRKQCKTHPHFVIPYRCLVGEFVSDALLVPDKCKFLHQERMDVCETHLHWHTVAKETCSEKSTNLHDYGMLLPCGIDKFRGVEFVCCPLAEESDNVDSADAEEDDSDVWWGGADTDYADGSEDKVVEVAEEEEVAEVEEEEADDDEDDEDGDEVEEEAEEPYEEATERTTSIATTTTTTTESVEEVVRVPTTAASTPDAVDKYLETPGDENEHAHFQKAKERLEAKHRERMSQVMREWEEAERQAKNLPKADKKAVIQHFQEKVESLEQEAANERQQLVETHMARVEAMLNDRRRLALENYITALQAVPPRPRHVFNMLKKYVRAEQKDRQHTLKHFEHVRMVDPKKAAQIRSQVMTHLRVIYERMNQSLSLLYNVPAVAEEIQDEVDELLQKEQNYSDDVLANMISEPRISYGNDALMPSLTETKTTVELLPVNGEFSLDDLQPWHSFGADSVPANTENEVEPVDARPAADRGLTTRPGSGLTNIKTEEISEVNLDAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIATVIVITLVMLKKKQYTSIHHGVVEVDAAVTPEERHLSKMQQNGYENPTYKFFEQMQN
  
Inhibitor
Name:
BDBM476539
Synonyms:
US10875854, Example 12
Type:
Small organic molecule
Emp. Form.:
C23H28F3N7O
Mol. Mass.:
475.5099
SMILES:
CC(C)c1ccc(OCC(F)(F)F)n2nc(N[C@H]3[C@H]4CC[C@@H]3CN(C4)c3cc(C)ncn3)nc12 |r,TLB:16:17:23.24.22:19.20,THB:25:23:17:19.20|
Structure:
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