Reaction Details |
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Target | Presenilin-1 |
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Ligand | BDBM50481053 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_599754 (CHEMBL1048198) |
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IC50 | 2.4±n/a nM |
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Citation | Truong, AP; Aubele, DL; Probst, GD; Neitzel, ML; Semko, CM; Bowers, S; Dressen, D; Hom, RK; Konradi, AW; Sham, HL; Garofalo, AW; Keim, PS; Wu, J; Dappen, MS; Wong, K; Goldbach, E; Quinn, KP; Sauer, JM; Brigham, EF; Wallace, W; Nguyen, L; Hemphill, SS; Bova, MP; Bard, F; Yednock, TA; Basi, G Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors. Bioorg Med Chem Lett19:4920-3 (2009) [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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BDBM50481053 |
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n/a |
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Name | BDBM50481053 |
Synonyms: | CHEMBL571604 |
Type | Small organic molecule |
Emp. Form. | C19H15F3N4O3S |
Mol. Mass. | 436.408 |
SMILES | [O-][n+]1ccc2-c3n[nH]cc3C(C3CC3)N(c2c1)S(=O)(=O)c1ccc(cc1)C(F)(F)F |
Structure |
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