Target
Amyloid-beta precursor protein
Ligand
BDBM455356
Substrate
n/a
Meas. Tech.
Cellular gamma-Secretase Assay
EC50
35.0±n/a nM
Citation
 Bartels, BJakob-Roetne, RLimberg, ANeidhart, WRatni, HReutlinger, MSteiner, S Fused pyrimidine derivatives US Patent  US10730881 Publication Date 8/4/2020 
Target
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:
MLPGLALLLLAAWTARALEVPTDGNAGLLAEPQIAMFCGRLNMHMNVQNGKWDSDPSGTKTCIDTKEGILQYCQEVYPELQITNVVEANQPVTIQNWCKRGRKQCKTHPHFVIPYRCLVGEFVSDALLVPDKCKFLHQERMDVCETHLHWHTVAKETCSEKSTNLHDYGMLLPCGIDKFRGVEFVCCPLAEESDNVDSADAEEDDSDVWWGGADTDYADGSEDKVVEVAEEEEVAEVEEEEADDDEDDEDGDEVEEEAEEPYEEATERTTSIATTTTTTTESVEEVVREVCSEQAETGPCRAMISRWYFDVTEGKCAPFFYGGCGGNRNNFDTEEYCMAVCGSAMSQSLLKTTQEPLARDPVKLPTTAASTPDAVDKYLETPGDENEHAHFQKAKERLEAKHRERMSQVMREWEEAERQAKNLPKADKKAVIQHFQEKVESLEQEAANERQQLVETHMARVEAMLNDRRRLALENYITALQAVPPRPRHVFNMLKKYVRAEQKDRQHTLKHFEHVRMVDPKKAAQIRSQVMTHLRVIYERMNQSLSLLYNVPAVAEEIQDEVDELLQKEQNYSDDVLANMISEPRISYGNDALMPSLTETKTTVELLPVNGEFSLDDLQPWHSFGADSVPANTENEVEPVDARPAADRGLTTRPGSGLTNIKTEEISEVKMDAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIATVIVITLVMLKKKQYTSIHHGVVEVDAAVTPEERHLSKMQQNGYENPTYKFFEQMQN
  
Inhibitor
Name:
BDBM455356
Synonyms:
8-(4-Fluorophenyl)-N4,5,5-trimethyl-N2-((1R,5S,8s)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diamine | US10730881, Example 22
Type:
Small organic molecule
Emp. Form.:
C28H35FN8
Mol. Mass.:
502.6295
SMILES:
CNc1nc(NC2C3CCC2CN(C3)c2cc(C)ncn2)nc2N(CCC(C)(C)c12)c1ccc(F)cc1 |TLB:14:12:6:8.9,5:6:12.11.13:8.9|
Structure:
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