Reaction Details |
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Target | Presenilin-1 |
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Ligand | BDBM50498595 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1512247 (CHEMBL3611643) |
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IC50 | 3080±n/a nM |
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Citation | Fischer, C; Zultanski, SL; Zhou, H; Methot, JL; Shah, S; Hayashi, I; Hughes, BL; Moxham, CM; Bays, NW; Smotrov, N; Hill, AD; Pan, BS; Wu, Z; Moy, LY; Tanga, F; Kenific, C; Cruz, JC; Walker, D; Bouthillette, M; Nikov, GN; Deshmukh, SV; Jeliazkova-Mecheva, VV; Diaz, D; Michener, MS; Cook, JJ; Munoz, B; Shearman, MS Discovery of novel triazolobenzazepinones as ?-secretase modulators with central A?42 lowering in rodents and rhesus monkeys. Bioorg Med Chem Lett25:3488-94 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Presenilin-1 |
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Name: | Presenilin-1 |
Synonyms: | 3.4.23.- | AD3 | Gamma-Secretase Subunit Presenilin-1 | PS-1 | PS1 | PS1-CTF12 | PSEN1 | PSN1_HUMAN | PSNL1 | Presenilin-1 CTF subunit | Presenilin-1 CTF12 | Presenilin-1 NTF subunit | Protein S182 |
Type: | n/a |
Mol. Mass.: | 52657.13 |
Organism: | Homo sapiens (Human) |
Description: | P49768 |
Residue: | 467 |
Sequence: | MTELPAPLSYFQNAQMSEDNHLSNTVRSQNDNRERQEHNDRRSLGHPEPLSNGRPQGNSR
QVVEQDEEEDEELTLKYGAKHVIMLFVPVTLCMVVVVATIKSVSFYTRKDGQLIYTPFTE
DTETVGQRALHSILNAAIMISVIVVMTILLVVLYKYRCYKVIHAWLIISSLLLLFFFSFI
YLGEVFKTYNVAVDYITVALLIWNFGVVGMISIHWKGPLRLQQAYLIMISALMALVFIKY
LPEWTAWLILAVISVYDLVAVLCPKGPLRMLVETAQERNETLFPALIYSSTMVWLVNMAE
GDPEAQRRVSKNSKYNAESTERESQDTVAENDDGGFSEEWEAQRDSHLGPHRSTPESRAA
VQELSSSILAGEDPEERGVKLGLGDFIFYSVLVGKASATASGDWNTTIACFVAILIGLCL
TLLLLAIFKKALPALPISITFGLVFYFATDYLVQPFMDQLAFHQFYI
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BDBM50498595 |
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n/a |
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Name | BDBM50498595 |
Synonyms: | CHEMBL3609623 |
Type | Small organic molecule |
Emp. Form. | C24H24N6O2 |
Mol. Mass. | 428.4864 |
SMILES | COc1cc(ccc1-n1cnc(C)c1)-c1cn(nn1)C1CCc2ccccc2N(C)C1=O |
Structure |
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