Reaction Details |
| Report a problem with these data |
Target | Gamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2 |
---|
Ligand | BDBM50172473 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1462983 (CHEMBL3398727) |
---|
IC50 | 307000±n/a nM |
---|
Citation | Flesch, D; Ness, J; Lamers, C; Dehm, F; Popella, S; Steri, R; Ogorek, I; Hieke, M; Dannhardt, G; Werz, O; Weggen, S; Schubert-Zsilavecz, M SAR-studies of¿-secretase modulators with PPAR¿-agonistic and 5-lipoxygenase-inhibitory activity for Alzheimer's disease. Bioorg Med Chem Lett25:841-6 (2015) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Gamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2 |
---|
Name: | Gamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2 |
Synonyms: | Gamma-Secretase Subunit APH-1A/Gamma-Secretase Subunit PEN-2/Gamma-Secretase Subunit Presenilin-1/Gamma-secretase subunit APH-1B/Nicastrin /Presenilin 2 | Gamma-secretase | Gamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin /Presenilin 1/Presenilin 2 |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 68900 |
Components: | This complex has 6 components. |
Component 1 |
Name: | Gamma-secretase subunit APH-1B |
Synonyms: | APH-1b | APH1B | APH1B_HUMAN | Aph-1beta | Gamma-secretase | Gamma-secretase subunit APH-1B | PSFL | Presenilin-stabilization factor-like |
Type: | PROTEIN |
Mol. Mass.: | 28468.17 |
Organism: | Homo sapiens (Human) |
Description: | EBI_10231 |
Residue: | 257 |
Sequence: | MTAAVFFGCAFIAFGPALALYVFTIATEPLRIIFLIAGAFFWLVSLLISSLVWFMARVII
DNKDGPTQKYLLIFGAFVSVYIQEMFRFAYYKLLKKASEGLKSINPGETAPSMRLLAYVS
GLGFGIMSGVFSFVNTLSDSLGPGTVGIHGDSPQFFLYSAFMTLVIILLHVFWGIVFFDG
CEKKKWGILLIVLLTHLLVSAQTFISSYYGINLASAFIILVLMGTWAFLAAGGSCRSLKL
CLLCQDKNFLLYNQRSR
|
|
|
Component 2 |
Name: | Presenilin-2 |
Synonyms: | AD3LP | AD4 | AD5 | E5-1 | Gamma-secretase | PS-2 | PS2 | PSEN2 | PSN2_HUMAN | PSNL2 | Presenilin 2 | Presenilin-2 | Presenilin-2 CTF subunit | Presenilin-2 NTF subunit | STM-2 | STM2 |
Type: | PROTEIN |
Mol. Mass.: | 50116.65 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_855576 |
Residue: | 448 |
Sequence: | MLTFMASDSEEEVCDERTSLMSAESPTPRSCQEGRQGPEDGENTAQWRSQENEEDGEEDP
DRYVCSGVPGRPPGLEEELTLKYGAKHVIMLFVPVTLCMIVVVATIKSVRFYTEKNGQLI
YTPFTEDTPSVGQRLLNSVLNTLIMISVIVVMTIFLVVLYKYRCYKFIHGWLIMSSLMLL
FLFTYIYLGEVLKTYNVAMDYPTLLLTVWNFGAVGMVCIHWKGPLVLQQAYLIMISALMA
LVFIKYLPEWSAWVILGAISVYDLVAVLCPKGPLRMLVETAQERNEPIFPALIYSSAMVW
TVGMAKLDPSSQGALQLPYDPEMEEDSYDSFGEPSYPEVFEPPLTGYPGEELEEEEERGV
KLGLGDFIFYSVLVGKAAATGSGDWNTTLACFVAILIGLCLTLLLLAVFKKALPALPISI
TFGLIFYFSTDNLVRPFMDTLASHQLYI
|
|
|
Component 3 |
Name: | Gamma-secretase subunit APH-1A |
Synonyms: | APH-1a | APH1A | APH1A_HUMAN | Aph-1alpha | Gamma-Secretase Subunit APH-1A | PSF | 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
|
|
|
Component 4 |
Name: | Nicastrin |
Synonyms: | Gamma-secretase | KIAA0253 | NCSTN | NICA_HUMAN | Nicastrin |
Type: | PROTEIN |
Mol. Mass.: | 78404.96 |
Organism: | Homo sapiens (Human) |
Description: | EBI_10683 |
Residue: | 709 |
Sequence: | MATAGGGSGADPGSRGLLRLLSFCVLLAGLCRGNSVERKIYIPLNKTAPCVRLLNATHQI
GCQSSISGDTGVIHVVEKEEDLQWVLTDGPNPPYMVLLESKHFTRDLMEKLKGRTSRIAG
LAVSLTKPSPASGFSPSVQCPNDGFGVYSNSYGPEFAHCREIQWNSLGNGLAYEDFSFPI
FLLEDENETKVIKQCYQDHNLSQNGSAPTFPLCAMQLFSHMHAVISTATCMRRSSIQSTF
SINPEIVCDPLSDYNVWSMLKPINTTGTLKPDDRVVVAATRLDSRSFFWNVAPGAESAVA
SFVTQLAAAEALQKAPDVTTLPRNVMFVFFQGETFDYIGSSRMVYDMEKGKFPVQLENVD
SFVELGQVALRTSLELWMHTDPVSQKNESVRNQVEDLLATLEKSGAGVPAVILRRPNQSQ
PLPPSSLQRFLRARNISGVVLADHSGAFHNKYYQSIYDTAENINVSYPEWLSPEEDLNFV
TDTAKALADVATVLGRALYELAGGTNFSDTVQADPQTVTRLLYGFLIKANNSWFQSILRQ
DLRSYLGDGPLQHYIAVSSPTNTTYVVQYALANLTGTVVNLTREQCQDPSKVPSENKDLY
EYSWVQGPLHSNETDRLPRCVRSTARLARALSPAFELSQWSSTEYSTWTESRWKDIRARI
FLIASKELELITLTVGFGILIFSLIVTYCINAKADVLFIAPREPGAVSY
|
|
|
Component 5 |
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
|
|
|
Component 6 |
Name: | Gamma-secretase subunit PEN-2 |
Synonyms: | Gamma-Secretase Subunit PEN-2 | Gamma-secretase | PEN2 | PEN2_HUMAN | PSENEN | 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
|
|
|
BDBM50172473 |
---|
n/a |
---|
Name | BDBM50172473 |
Synonyms: | (-)-(2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid | (2R)-2-(2-fluoro-[1,1'-biphenyl-4-yl])propanoic acid | (2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid | (R)-2-fluoro-alpha-methyl(1,1'-biphenyl)-4-acetic acid | (R)-FLURBIPROFEN | CHEMBL190083 | Flurizan | Tarenflurbil |
Type | Small organic molecule |
Emp. Form. | C15H13FO2 |
Mol. Mass. | 244.2609 |
SMILES | C[C@@H](C(O)=O)c1ccc(c(F)c1)-c1ccccc1 |
Structure |
|