Reaction Details |
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Target | Presenilin-1 |
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Ligand | BDBM50577496 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2130375 (CHEMBL4839804) |
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EC50 | 97±n/a nM |
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Citation | Bursavich, MG; Harrison, BA; Acharya, R; Costa, DE; Freeman, EA; Hrdlicka, LA; Jin, H; Kapadnis, S; Moffit, JS; Murphy, D; Nolan, SJ; Patzke, H; Tang, C; Van Voorhies, HE; Wen, M; Koenig, G; Blain, JF; Burnett, DA Discovery of the Oxadiazine FRM-024: A Potent CNS-Penetrant Gamma Secretase Modulator. J Med Chem64:14426-14447 (2021) [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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BDBM50577496 |
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n/a |
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Name | BDBM50577496 |
Synonyms: | CHEMBL4859045 |
Type | Small organic molecule |
Emp. Form. | C20H21N5O3 |
Mol. Mass. | 379.4124 |
SMILES | COc1ccc(cc1)C1CON=C(N1)c1ccc(c(OC)n1)-n1cnc(C)c1 |c:12| |
Structure |
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