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TargetPresenilin-1
LigandBDBM50481053
Substrate/Competitorn/a
Meas. Tech.ChEMBL_599754 (CHEMBL1048198)
IC50 2.4±n/a nM
Citation Truong, APAubele, DLProbst, GDNeitzel, MLSemko, CMBowers, SDressen, DHom, RKKonradi, AWSham, HLGarofalo, AWKeim, PSWu, JDappen, MSWong, KGoldbach, EQuinn, KPSauer, JMBrigham, EFWallace, WNguyen, LHemphill, SSBova, MPBard, FYednock, TABasi, 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
More Info.:Get all data from this article,  Assay Method
 
Presenilin-1
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50481053
n/a
NameBDBM50481053
Synonyms:CHEMBL571604
TypeSmall 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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