Ki Summary new BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetGamma-Secretase
LigandBDBM28960
Substrate/CompetitorBeta amyloid A4 protein
Meas. Tech.Cell-Based Assay for Amyloid-beta Accumulation
EC50 10±n/a nM
Citation Bergstrom CPSloan CPLau WYSmith DWZheng MHansel SBPolson CTCorsa JABarten DMFelsenstein KMRoberts SB Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase. Bioorg Med Chem Lett 18:464-8 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Gamma-Secretase
Name:Gamma-Secretase
Synonyms:n/a
Type:Multi-subunit protease complex
Mol. Mass.:n/a
Description:A complex composed of a presenilin homodimer, nicastrin, APH1 and PEN2. It is the minimal complex sufficient for secretase activity.
Components:This complex has 4 components.
Component 1
Name:Gamma-Secretase Subunit APH-1A
Synonyms:APH-1a | Aph-1alpha | Presenilin-stabilization factor
Type:Enzyme subunit; multi-pass membrane protein
Mol. Mass.:28998.73
Organism:Homo sapiens (Human)
Description:n/a
Residue:265
Sequence:
MGAAVFFGCTFVAFGPAFALFLITVAGDPLRVIILVAGAFFWLVSLLLASVVWFILVHVT
DRSDARLQYGLLIFGAAVSVLLQEVFRFAYYKLLKKADEGLASLSEDGRSPISIRQMAYV
SGLSFGIISGVFSVINILADALGPGVVGIHGDSPYYFLTSAFLTAAIILLHTFWGVVFFD
ACERRRYWALGLVVGSHLLTSGLTFLNPWYEASLLPIYAVTVSMGLWAFITAGGSLRSIQ
RSLLCRRQEDSRVMVYSALRIPPED
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
Component 2
Name:Gamma-secretase
Synonyms:Gamma-Secretase Subunit PEN-2 | Presenilin enhancer protein 2
Type:Enzyme subunit; multi-pass membrane protein
Mol. Mass.:12031.98
Organism:Homo sapiens (Human)
Description:n/a
Residue:101
Sequence:
MNLERVSNEEKLNLCRKYYLGGFAFLPFLWLVNIFWFFREAFLVPAYTEQSQIKGYVWRS
AVGFLFWVIVLTSWITIFQIYRPRWGALGDYLSFTIPLGTP
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
Component 3
Name:Gamma-Secretase Subunit Nicastrin
Synonyms:n/a
Type:Single-pass type I membrane protein
Mol. Mass.:75243.23
Organism:Homo sapiens (Human)
Description:n/a
Residue:676
Sequence:
NSVERKIYIPLNKTAPCVRLLNATHQIGCQSSISGDTGVIHVVEKEEDLQWVLTDGPNPP
YMVLLESKHFTRDLMEKLKGRTSRIAGLAVSLTKPSPASGFSPSVQCPNDGFGVYSNSYG
PEFAHCREIQWNSLGNGLAYEDFSFPIFLLEDENETKVIKQCYQDHNLSQNGSAPTFPLC
AMQLFSHMHAVISTATCMRRSSIQSTFSINPEIVCDPLSDYNVWSMLKPINTTGTLKPDD
RVVVAATRLDSRSFFWNVAPGAESAVASFVTQLAAAEALQKAPDVTTLPRNVMFVFFQGE
TFDYIGSSRMVYDMEKGKFPVQLENVDSFVELGQVALRTSLELWMHTDPVSQKNESVRNQ
VEDLLATLEKSGAGVPAVILRRPNQSQPLPPSSLQRFLRARNISGVVLADHSGAFHNKYY
QSIYDTAENINVSYPEWLSPEEDLNFVTDTAKALADVATVLGRALYELAGGTNFSDTVQA
DPQTVTRLLYGFLIKANNSWFQSILRQDLRSYLGDGPLQHYIAVSSPTNTTYVVQYALAN
LTGTVVNLTREQCQDPSKVPSENKDLYEYSWVQGPLHSNETDRLPRCVRSTARLARALSP
AFELSQWSSTEYSTWTESRWKDIRARIFLIASKELELITLTVGFGILIFSLIVTYCINAK
ADVLFIAPREPGAVSY
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
Component 4
Name:Presenilin-1
Synonyms:3.4.23.- | AD3 | AD3 | Gamma-Secretase Subunit Presenilin-1 | PS-1 | PS1 | PS1-CTF12 | PSEN1 | 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:
BDBM28960
Beta amyloid A4 protein
Name:Beta amyloid A4 protein
Synonyms:ABPP | 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) | 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:n/a
Residue:770
Sequence:
MLPGLALLLLAAWTARALEVPTDGNAGLLAEPQIAMFCGRLNMHMNVQNGKWDSDPSGTK
TCIDTKEGILQYCQEVYPELQITNVVEANQPVTIQNWCKRGRKQCKTHPHFVIPYRCLVG
EFVSDALLVPDKCKFLHQERMDVCETHLHWHTVAKETCSEKSTNLHDYGMLLPCGIDKFR
GVEFVCCPLAEESDNVDSADAEEDDSDVWWGGADTDYADGSEDKVVEVAEEEEVAEVEEE
EADDDEDDEDGDEVEEEAEEPYEEATERTTSIATTTTTTTESVEEVVREVCSEQAETGPC
RAMISRWYFDVTEGKCAPFFYGGCGGNRNNFDTEEYCMAVCGSAMSQSLLKTTQEPLARD
PVKLPTTAASTPDAVDKYLETPGDENEHAHFQKAKERLEAKHRERMSQVMREWEEAERQA
KNLPKADKKAVIQHFQEKVESLEQEAANERQQLVETHMARVEAMLNDRRRLALENYITAL
QAVPPRPRHVFNMLKKYVRAEQKDRQHTLKHFEHVRMVDPKKAAQIRSQVMTHLRVIYER
MNQSLSLLYNVPAVAEEIQDEVDELLQKEQNYSDDVLANMISEPRISYGNDALMPSLTET
KTTVELLPVNGEFSLDDLQPWHSFGADSVPANTENEVEPVDARPAADRGLTTRPGSGLTN
IKTEEISEVKMDAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIATVIVITL
VMLKKKQYTSIHHGVVEVDAAVTPEERHLSKMQQNGYENPTYKFFEQMQN
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff: