mrk 560 profile

MRK 560: a gamma-secretase inhibitor; MRK-560 is the (cis)-isomer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	11577204
CHEMBL ID	372199
CHEMBL ID	1091513
SCHEMBL ID	237758
SCHEMBL ID	237759
SCHEMBL ID	237760
MeSH ID	M0498682

Synonym
cyclohexyl sulfone-based compound, 32
n-{4-[(4-chlorobenzene)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl}trifluoromethanesulfonamide
bdbm28986
CHEMBL372199
CHEMBL1091513
mrk-560
SCHEMBL237758
SCHEMBL237759
SCHEMBL237760
trifluoromethanesulfonic acid, n-[4-(4-chlorobenzenesulfonyl)-4-(2,5-difluorophenyl)-cyclohexyl]-amide
mrk 560
n-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide
677772-84-8
AKOS024457922
MRF-0000011
NCGC00371101-01
n-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide
n-((1s,4s)-4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)-1,1,1-trifluoromethanesulfonamide
HY-14174
SB19628
CS-0003248
EX-A5360
MS-29608
wdzvwdxoigqjio-ujkqegagsa-n
IGD ,

Excerpt	Reference	Relevance
"We treated T-ALL cell lines in vitro and T-ALL patient-derived xenograft (PDX) models in vivo with MRK-560 alone or in combination with other targeted inhibitors (ruxolitinib, imatinib or KPT-8602/eltanexor)."	( PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia. Boeckx, N; Cools, J; De Keersmaecker, K; Gielen, O; Govaerts, I; Jacobs, K; Maertens, J; Nittner, D; Prieto, C; Provost, S; Segers, H; Vandersmissen, C, 2021)	0.62
"All NOTCH1-signaling-dependent T-ALL cell lines were sensitive to MRK-560 and its combination with ruxolitinib or imatinib in JAK1- or ABL1-dependent cell lines synergistically inhibited leukemia proliferation."	( PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia. Boeckx, N; Cools, J; De Keersmaecker, K; Gielen, O; Govaerts, I; Jacobs, K; Maertens, J; Nittner, D; Prieto, C; Provost, S; Segers, H; Vandersmissen, C, 2021)	0.62

Excerpt	Reference	Relevance
" These results demonstrate that MRK-560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo."	( In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat. Atack, JR; Best, JD; Churcher, I; Harrison, T; Jay, MT; Morentin-Gutierrez, P; Otu, F; Pattison, C; Reilly, M; Shearman, MS, 2006)	0.33
" We demonstrate here that chronic treatment for 3 months with 3 mg/kg of the potent, orally bioavailable and brain-penetrant gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)-sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) attenuates the appearance of amyloid plaques in the Tg2576 mouse."	( The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse. Atack, JR; Best, JD; Boussiquet-Leroux, C; Churcher, I; Ellis, S; Harrison, T; Laroque, PA; Lewis, HD; O'Donnell, R; Reilly, MA; Rosahl, TW; Shearman, MS; Smith, DW; Wilkie, N, 2007)	0.34
" We studied the in vivo effects of the potent, orally bioavailable and brain penetrant γ-secretase inhibitor (GSI), MRK-560, on both Aβx-40 and Aβx-42 in multiple compartments (plasma, the brain and cerebrospinal fluid) of rat."	( Quantitative assessment of Aβ peptide in brain, cerebrospinal fluid and plasma following oral administration of γ-secretase inhibitor MRK-560 in rats. Hershey, JC; Na, S; Wu, G; Wu, Z, 2015)	0.42
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" This relationship between the brain and CSF Abeta was maintained when MRK-560 was dosed once a day for 2 weeks, and accordingly, when all the data for the dose-response curve and time courses were correlated, a strong association was observed between the brain and CSF Abeta levels."	( In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat. Atack, JR; Best, JD; Churcher, I; Harrison, T; Jay, MT; Morentin-Gutierrez, P; Otu, F; Pattison, C; Reilly, M; Shearman, MS, 2006)	0.33
" These results suggest that central Aβ changes that occur following acute dosing with MRK-560 can be predicted based on plasma Aβ changes and could thus serve as a useful biomarker to help accelerate decision-making during early clinical development."	( Quantitative assessment of Aβ peptide in brain, cerebrospinal fluid and plasma following oral administration of γ-secretase inhibitor MRK-560 in rats. Hershey, JC; Na, S; Wu, G; Wu, Z, 2015)	0.42

Protein Targets (19)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	4.2534	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	0.4253	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	18.9991	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	0.4253	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	0.4253	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	0.4253	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	0.4253	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Amyloid-beta precursor protein	Homo sapiens (human)	IC50 (µMol)	0.0006	0.0005	3.8895	10.0000	AID1790891; AID1790892; AID1790893
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	12.9500	0.0001	1.7536	10.0000	AID1254132; AID1254133
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	30.0000	0.0000	2.0151	10.0000	AID1254134; AID1254135
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	0.3000	0.0000	2.8005	10.0000	AID1254136; AID1254137
Presenilin-1	Homo sapiens (human)	IC50 (µMol)	0.0144	0.0001	0.2378	5.6800	AID1254120; AID1254121; AID1254122; AID1628295; AID1912794; AID1913255; AID258050
Presenilin-2	Homo sapiens (human)	IC50 (µMol)	0.0200	0.0001	0.2435	5.6800	AID1254120; AID1254121; AID1254122; AID1628295; AID258050
Sodium-dependent dopamine transporter	Homo sapiens (human)	Ki	3.1454	0.0002	1.1115	8.0280	AID1794421; AID1914651
Synaptic vesicular amine transporter	Homo sapiens (human)	IC50 (µMol)	0.2130	0.0132	0.4859	4.2000	AID1914650
Gamma-secretase subunit APH-1B	Homo sapiens (human)	IC50 (µMol)	0.0200	0.0001	0.2435	5.6800	AID1254120; AID1254121; AID1254122; AID1628295; AID258050
Nicastrin	Homo sapiens (human)	IC50 (µMol)	0.0200	0.0001	0.2435	5.6800	AID1254120; AID1254121; AID1254122; AID1628295; AID258050
Gamma-secretase subunit APH-1A	Homo sapiens (human)	IC50 (µMol)	0.0200	0.0001	0.2435	5.6800	AID1254120; AID1254121; AID1254122; AID1628295; AID258050
Gamma-secretase subunit PEN-2	Homo sapiens (human)	IC50 (µMol)	0.0200	0.0001	0.2442	5.6800	AID1254120; AID1254121; AID1254122; AID1628295; AID258050
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Presenilin-1	Homo sapiens (human)	EC50 (µMol)	0.0007	0.0001	0.6857	5.7000	AID1798949
Nicastrin	Homo sapiens (human)	EC50 (µMol)	0.0007	0.0001	0.7999	5.7000	AID1798949
Gamma-secretase subunit APH-1A	Homo sapiens (human)	EC50 (µMol)	0.0007	0.0001	0.7999	5.7000	AID1798949
Gamma-secretase subunit PEN-2	Homo sapiens (human)	EC50 (µMol)	0.0007	0.0001	0.7999	5.7000	AID1798949
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (277)

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of gene expression	Amyloid-beta precursor protein	Homo sapiens (human)
cognition	Amyloid-beta precursor protein	Homo sapiens (human)
G2/M transition of mitotic cell cycle	Amyloid-beta precursor protein	Homo sapiens (human)
microglial cell activation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of protein phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
suckling behavior	Amyloid-beta precursor protein	Homo sapiens (human)
astrocyte activation involved in immune response	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of translation	Amyloid-beta precursor protein	Homo sapiens (human)
protein phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
intracellular copper ion homeostasis	Amyloid-beta precursor protein	Homo sapiens (human)
endocytosis	Amyloid-beta precursor protein	Homo sapiens (human)
response to oxidative stress	Amyloid-beta precursor protein	Homo sapiens (human)
cell adhesion	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of epidermal growth factor-activated receptor activity	Amyloid-beta precursor protein	Homo sapiens (human)
Notch signaling pathway	Amyloid-beta precursor protein	Homo sapiens (human)
axonogenesis	Amyloid-beta precursor protein	Homo sapiens (human)
learning or memory	Amyloid-beta precursor protein	Homo sapiens (human)
learning	Amyloid-beta precursor protein	Homo sapiens (human)
mating behavior	Amyloid-beta precursor protein	Homo sapiens (human)
locomotory behavior	Amyloid-beta precursor protein	Homo sapiens (human)
axo-dendritic transport	Amyloid-beta precursor protein	Homo sapiens (human)
cholesterol metabolic process	Amyloid-beta precursor protein	Homo sapiens (human)
negative regulation of cell population proliferation	Amyloid-beta precursor protein	Homo sapiens (human)
adult locomotory behavior	Amyloid-beta precursor protein	Homo sapiens (human)
visual learning	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of gene expression	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of gene expression	Amyloid-beta precursor protein	Homo sapiens (human)
negative regulation of gene expression	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycle	Amyloid-beta precursor protein	Homo sapiens (human)
microglia development	Amyloid-beta precursor protein	Homo sapiens (human)
axon midline choice point recognition	Amyloid-beta precursor protein	Homo sapiens (human)
neuron remodeling	Amyloid-beta precursor protein	Homo sapiens (human)
dendrite development	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of Wnt signaling pathway	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular matrix organization	Amyloid-beta precursor protein	Homo sapiens (human)
forebrain development	Amyloid-beta precursor protein	Homo sapiens (human)
neuron projection development	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of chemokine production	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of interleukin-1 beta production	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of interleukin-6 production	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of tumor necrosis factor production	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of multicellular organism growth	Amyloid-beta precursor protein	Homo sapiens (human)
negative regulation of neuron differentiation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of glycolytic process	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of mitotic cell cycle	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of JNK cascade	Amyloid-beta precursor protein	Homo sapiens (human)
astrocyte activation	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of long-term neuronal synaptic plasticity	Amyloid-beta precursor protein	Homo sapiens (human)
collateral sprouting in absence of injury	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of inflammatory response	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of peptidyl-tyrosine phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of synapse structure or activity	Amyloid-beta precursor protein	Homo sapiens (human)
synapse organization	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of calcium-mediated signaling	Amyloid-beta precursor protein	Homo sapiens (human)
neuromuscular process controlling balance	Amyloid-beta precursor protein	Homo sapiens (human)
synaptic assembly at neuromuscular junction	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of protein metabolic process	Amyloid-beta precursor protein	Homo sapiens (human)
neuron apoptotic process	Amyloid-beta precursor protein	Homo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasis	Amyloid-beta precursor protein	Homo sapiens (human)
neuron cellular homeostasis	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Amyloid-beta precursor protein	Homo sapiens (human)
response to interleukin-1	Amyloid-beta precursor protein	Homo sapiens (human)
modulation of excitatory postsynaptic potential	Amyloid-beta precursor protein	Homo sapiens (human)
NMDA selective glutamate receptor signaling pathway	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of spontaneous synaptic transmission	Amyloid-beta precursor protein	Homo sapiens (human)
cytosolic mRNA polyadenylation	Amyloid-beta precursor protein	Homo sapiens (human)
negative regulation of long-term synaptic potentiation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of long-term synaptic potentiation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transduction	Amyloid-beta precursor protein	Homo sapiens (human)
cellular response to amyloid-beta	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of presynapse assembly	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of amyloid fibril formation	Amyloid-beta precursor protein	Homo sapiens (human)
amyloid fibril formation	Amyloid-beta precursor protein	Homo sapiens (human)
neuron projection maintenance	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of T cell migration	Amyloid-beta precursor protein	Homo sapiens (human)
central nervous system development	Amyloid-beta precursor protein	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
negative regulation of low-density lipoprotein receptor activity	Presenilin-1	Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasis	Presenilin-1	Homo sapiens (human)
cell-cell adhesion	Presenilin-1	Homo sapiens (human)
autophagosome assembly	Presenilin-1	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Presenilin-1	Homo sapiens (human)
blood vessel development	Presenilin-1	Homo sapiens (human)
cell fate specification	Presenilin-1	Homo sapiens (human)
somitogenesis	Presenilin-1	Homo sapiens (human)
neuron migration	Presenilin-1	Homo sapiens (human)
positive regulation of receptor recycling	Presenilin-1	Homo sapiens (human)
negative regulation of protein phosphorylation	Presenilin-1	Homo sapiens (human)
positive regulation of protein phosphorylation	Presenilin-1	Homo sapiens (human)
heart looping	Presenilin-1	Homo sapiens (human)
positive regulation of L-glutamate import across plasma membrane	Presenilin-1	Homo sapiens (human)
hematopoietic progenitor cell differentiation	Presenilin-1	Homo sapiens (human)
astrocyte activation involved in immune response	Presenilin-1	Homo sapiens (human)
T cell activation involved in immune response	Presenilin-1	Homo sapiens (human)
neural retina development	Presenilin-1	Homo sapiens (human)
protein glycosylation	Presenilin-1	Homo sapiens (human)
membrane protein ectodomain proteolysis	Presenilin-1	Homo sapiens (human)
mitochondrial transport	Presenilin-1	Homo sapiens (human)
DNA damage response	Presenilin-1	Homo sapiens (human)
response to oxidative stress	Presenilin-1	Homo sapiens (human)
Notch receptor processing	Presenilin-1	Homo sapiens (human)
learning or memory	Presenilin-1	Homo sapiens (human)
memory	Presenilin-1	Homo sapiens (human)
post-embryonic development	Presenilin-1	Homo sapiens (human)
regulation of gene expression	Presenilin-1	Homo sapiens (human)
positive regulation of gene expression	Presenilin-1	Homo sapiens (human)
negative regulation of gene expression	Presenilin-1	Homo sapiens (human)
regulation of neuron projection development	Presenilin-1	Homo sapiens (human)
protein transport	Presenilin-1	Homo sapiens (human)
choline transport	Presenilin-1	Homo sapiens (human)
synaptic vesicle targeting	Presenilin-1	Homo sapiens (human)
protein processing	Presenilin-1	Homo sapiens (human)
cerebellum development	Presenilin-1	Homo sapiens (human)
cerebral cortex cell migration	Presenilin-1	Homo sapiens (human)
Cajal-Retzius cell differentiation	Presenilin-1	Homo sapiens (human)
dorsal/ventral neural tube patterning	Presenilin-1	Homo sapiens (human)
embryonic limb morphogenesis	Presenilin-1	Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic process	Presenilin-1	Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasis	Presenilin-1	Homo sapiens (human)
positive regulation of tumor necrosis factor production	Presenilin-1	Homo sapiens (human)
amyloid-beta formation	Presenilin-1	Homo sapiens (human)
intracellular signal transduction	Presenilin-1	Homo sapiens (human)
locomotion	Presenilin-1	Homo sapiens (human)
positive regulation of protein import into nucleus	Presenilin-1	Homo sapiens (human)
regulation of phosphorylation	Presenilin-1	Homo sapiens (human)
amyloid precursor protein metabolic process	Presenilin-1	Homo sapiens (human)
amyloid precursor protein catabolic process	Presenilin-1	Homo sapiens (human)
myeloid dendritic cell differentiation	Presenilin-1	Homo sapiens (human)
positive regulation of apoptotic process	Presenilin-1	Homo sapiens (human)
negative regulation of apoptotic process	Presenilin-1	Homo sapiens (human)
negative regulation of neuron apoptotic process	Presenilin-1	Homo sapiens (human)
skin morphogenesis	Presenilin-1	Homo sapiens (human)
positive regulation of glycolytic process	Presenilin-1	Homo sapiens (human)
positive regulation of DNA-templated transcription	Presenilin-1	Homo sapiens (human)
astrocyte activation	Presenilin-1	Homo sapiens (human)
regulation of synaptic plasticity	Presenilin-1	Homo sapiens (human)
thymus development	Presenilin-1	Homo sapiens (human)
neuron development	Presenilin-1	Homo sapiens (human)
skeletal system morphogenesis	Presenilin-1	Homo sapiens (human)
brain morphogenesis	Presenilin-1	Homo sapiens (human)
epithelial cell proliferation	Presenilin-1	Homo sapiens (human)
negative regulation of axonogenesis	Presenilin-1	Homo sapiens (human)
synapse organization	Presenilin-1	Homo sapiens (human)
positive regulation of coagulation	Presenilin-1	Homo sapiens (human)
T cell receptor signaling pathway	Presenilin-1	Homo sapiens (human)
sequestering of calcium ion	Presenilin-1	Homo sapiens (human)
neuron apoptotic process	Presenilin-1	Homo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasis	Presenilin-1	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Presenilin-1	Homo sapiens (human)
regulation of resting membrane potential	Presenilin-1	Homo sapiens (human)
regulation of canonical Wnt signaling pathway	Presenilin-1	Homo sapiens (human)
positive regulation of dendritic spine development	Presenilin-1	Homo sapiens (human)
neuron cellular homeostasis	Presenilin-1	Homo sapiens (human)
calcium ion transmembrane transport	Presenilin-1	Homo sapiens (human)
apoptotic signaling pathway	Presenilin-1	Homo sapiens (human)
regulation of synaptic vesicle cycle	Presenilin-1	Homo sapiens (human)
L-glutamate import across plasma membrane	Presenilin-1	Homo sapiens (human)
regulation of postsynapse organization	Presenilin-1	Homo sapiens (human)
protein catabolic process at postsynapse	Presenilin-1	Homo sapiens (human)
cellular response to amyloid-beta	Presenilin-1	Homo sapiens (human)
negative regulation of core promoter binding	Presenilin-1	Homo sapiens (human)
positive regulation of amyloid fibril formation	Presenilin-1	Homo sapiens (human)
neuron projection maintenance	Presenilin-1	Homo sapiens (human)
negative regulation of ubiquitin-dependent protein catabolic process	Presenilin-1	Homo sapiens (human)
negative regulation of apoptotic signaling pathway	Presenilin-1	Homo sapiens (human)
calcium ion homeostasis	Presenilin-1	Homo sapiens (human)
Notch signaling pathway	Presenilin-1	Homo sapiens (human)
response to hypoxia	Presenilin-2	Homo sapiens (human)
membrane protein ectodomain proteolysis	Presenilin-2	Homo sapiens (human)
Notch receptor processing	Presenilin-2	Homo sapiens (human)
protein processing	Presenilin-2	Homo sapiens (human)
amyloid-beta formation	Presenilin-2	Homo sapiens (human)
intracellular signal transduction	Presenilin-2	Homo sapiens (human)
amyloid precursor protein catabolic process	Presenilin-2	Homo sapiens (human)
regulation of calcium import into the mitochondrion	Presenilin-2	Homo sapiens (human)
mitochondrion-endoplasmic reticulum membrane tethering	Presenilin-2	Homo sapiens (human)
calcium ion homeostasis	Presenilin-2	Homo sapiens (human)
Notch signaling pathway	Presenilin-2	Homo sapiens (human)
monoamine transport	Sodium-dependent dopamine transporter	Homo sapiens (human)
neurotransmitter transport	Sodium-dependent dopamine transporter	Homo sapiens (human)
lactation	Sodium-dependent dopamine transporter	Homo sapiens (human)
sensory perception of smell	Sodium-dependent dopamine transporter	Homo sapiens (human)
locomotory behavior	Sodium-dependent dopamine transporter	Homo sapiens (human)
response to xenobiotic stimulus	Sodium-dependent dopamine transporter	Homo sapiens (human)
response to iron ion	Sodium-dependent dopamine transporter	Homo sapiens (human)
dopamine transport	Sodium-dependent dopamine transporter	Homo sapiens (human)
adenohypophysis development	Sodium-dependent dopamine transporter	Homo sapiens (human)
response to nicotine	Sodium-dependent dopamine transporter	Homo sapiens (human)
positive regulation of multicellular organism growth	Sodium-dependent dopamine transporter	Homo sapiens (human)
regulation of dopamine metabolic process	Sodium-dependent dopamine transporter	Homo sapiens (human)
response to cocaine	Sodium-dependent dopamine transporter	Homo sapiens (human)
dopamine biosynthetic process	Sodium-dependent dopamine transporter	Homo sapiens (human)
dopamine catabolic process	Sodium-dependent dopamine transporter	Homo sapiens (human)
response to ethanol	Sodium-dependent dopamine transporter	Homo sapiens (human)
cognition	Sodium-dependent dopamine transporter	Homo sapiens (human)
dopamine uptake involved in synaptic transmission	Sodium-dependent dopamine transporter	Homo sapiens (human)
response to cAMP	Sodium-dependent dopamine transporter	Homo sapiens (human)
norepinephrine uptake	Sodium-dependent dopamine transporter	Homo sapiens (human)
prepulse inhibition	Sodium-dependent dopamine transporter	Homo sapiens (human)
dopamine uptake	Sodium-dependent dopamine transporter	Homo sapiens (human)
hyaloid vascular plexus regression	Sodium-dependent dopamine transporter	Homo sapiens (human)
amino acid transport	Sodium-dependent dopamine transporter	Homo sapiens (human)
norepinephrine transport	Sodium-dependent dopamine transporter	Homo sapiens (human)
sodium ion transmembrane transport	Sodium-dependent dopamine transporter	Homo sapiens (human)
response to amphetamine	Synaptic vesicular amine transporter	Homo sapiens (human)
serotonin secretion by mast cell	Synaptic vesicular amine transporter	Homo sapiens (human)
histamine secretion by mast cell	Synaptic vesicular amine transporter	Homo sapiens (human)
neurotransmitter transport	Synaptic vesicular amine transporter	Homo sapiens (human)
chemical synaptic transmission	Synaptic vesicular amine transporter	Homo sapiens (human)
locomotory behavior	Synaptic vesicular amine transporter	Homo sapiens (human)
response to toxic substance	Synaptic vesicular amine transporter	Homo sapiens (human)
post-embryonic development	Synaptic vesicular amine transporter	Homo sapiens (human)
monoamine transport	Synaptic vesicular amine transporter	Homo sapiens (human)
dopamine transport	Synaptic vesicular amine transporter	Homo sapiens (human)
sequestering of neurotransmitter	Synaptic vesicular amine transporter	Homo sapiens (human)
serotonin uptake	Synaptic vesicular amine transporter	Homo sapiens (human)
histamine uptake	Synaptic vesicular amine transporter	Homo sapiens (human)
neurotransmitter loading into synaptic vesicle	Synaptic vesicular amine transporter	Homo sapiens (human)
somato-dendritic dopamine secretion	Synaptic vesicular amine transporter	Homo sapiens (human)
proton transmembrane transport	Synaptic vesicular amine transporter	Homo sapiens (human)
negative regulation of reactive oxygen species biosynthetic process	Synaptic vesicular amine transporter	Homo sapiens (human)
aminergic neurotransmitter loading into synaptic vesicle	Synaptic vesicular amine transporter	Homo sapiens (human)
protein processing	Gamma-secretase subunit APH-1B	Homo sapiens (human)
Notch receptor processing	Gamma-secretase subunit APH-1B	Homo sapiens (human)
positive regulation of endopeptidase activity	Gamma-secretase subunit APH-1B	Homo sapiens (human)
protein processing	Gamma-secretase subunit APH-1B	Homo sapiens (human)
membrane protein intracellular domain proteolysis	Gamma-secretase subunit APH-1B	Homo sapiens (human)
amyloid-beta formation	Gamma-secretase subunit APH-1B	Homo sapiens (human)
amyloid precursor protein catabolic process	Gamma-secretase subunit APH-1B	Homo sapiens (human)
Notch signaling pathway	Gamma-secretase subunit APH-1B	Homo sapiens (human)
myeloid cell homeostasis	Nicastrin	Homo sapiens (human)
proteolysis	Nicastrin	Homo sapiens (human)
membrane protein ectodomain proteolysis	Nicastrin	Homo sapiens (human)
dopamine receptor signaling pathway	Nicastrin	Homo sapiens (human)
glutamate receptor signaling pathway	Nicastrin	Homo sapiens (human)
Notch signaling pathway	Nicastrin	Homo sapiens (human)
Notch receptor processing	Nicastrin	Homo sapiens (human)
learning or memory	Nicastrin	Homo sapiens (human)
positive regulation of endopeptidase activity	Nicastrin	Homo sapiens (human)
protein processing	Nicastrin	Homo sapiens (human)
cerebellum development	Nicastrin	Homo sapiens (human)
central nervous system myelination	Nicastrin	Homo sapiens (human)
adult behavior	Nicastrin	Homo sapiens (human)
membrane protein intracellular domain proteolysis	Nicastrin	Homo sapiens (human)
amyloid-beta formation	Nicastrin	Homo sapiens (human)
T cell proliferation	Nicastrin	Homo sapiens (human)
amyloid precursor protein metabolic process	Nicastrin	Homo sapiens (human)
amyloid precursor protein biosynthetic process	Nicastrin	Homo sapiens (human)
positive regulation of amyloid precursor protein biosynthetic process	Nicastrin	Homo sapiens (human)
amyloid precursor protein catabolic process	Nicastrin	Homo sapiens (human)
epithelial cell proliferation	Nicastrin	Homo sapiens (human)
neuron apoptotic process	Nicastrin	Homo sapiens (human)
cellular response to calcium ion	Nicastrin	Homo sapiens (human)
regulation of long-term synaptic potentiation	Nicastrin	Homo sapiens (human)
short-term synaptic potentiation	Nicastrin	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
metanephros development	Gamma-secretase subunit APH-1A	Homo sapiens (human)
membrane protein ectodomain proteolysis	Gamma-secretase subunit APH-1A	Homo sapiens (human)
Notch receptor processing	Gamma-secretase subunit APH-1A	Homo sapiens (human)
positive regulation of endopeptidase activity	Gamma-secretase subunit APH-1A	Homo sapiens (human)
protein processing	Gamma-secretase subunit APH-1A	Homo sapiens (human)
membrane protein intracellular domain proteolysis	Gamma-secretase subunit APH-1A	Homo sapiens (human)
amyloid-beta formation	Gamma-secretase subunit APH-1A	Homo sapiens (human)
amyloid precursor protein metabolic process	Gamma-secretase subunit APH-1A	Homo sapiens (human)
amyloid precursor protein catabolic process	Gamma-secretase subunit APH-1A	Homo sapiens (human)
Notch signaling pathway	Gamma-secretase subunit APH-1A	Homo sapiens (human)
membrane protein ectodomain proteolysis	Gamma-secretase subunit PEN-2	Homo sapiens (human)
Notch signaling pathway	Gamma-secretase subunit PEN-2	Homo sapiens (human)
Notch receptor processing	Gamma-secretase subunit PEN-2	Homo sapiens (human)
positive regulation of endopeptidase activity	Gamma-secretase subunit PEN-2	Homo sapiens (human)
protein processing	Gamma-secretase subunit PEN-2	Homo sapiens (human)
membrane protein intracellular domain proteolysis	Gamma-secretase subunit PEN-2	Homo sapiens (human)
amyloid-beta formation	Gamma-secretase subunit PEN-2	Homo sapiens (human)
amyloid precursor protein metabolic process	Gamma-secretase subunit PEN-2	Homo sapiens (human)
amyloid precursor protein catabolic process	Gamma-secretase subunit PEN-2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (81)

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Amyloid-beta precursor protein	Homo sapiens (human)
DNA binding	Amyloid-beta precursor protein	Homo sapiens (human)
serine-type endopeptidase inhibitor activity	Amyloid-beta precursor protein	Homo sapiens (human)
signaling receptor binding	Amyloid-beta precursor protein	Homo sapiens (human)
protein binding	Amyloid-beta precursor protein	Homo sapiens (human)
heparin binding	Amyloid-beta precursor protein	Homo sapiens (human)
enzyme binding	Amyloid-beta precursor protein	Homo sapiens (human)
identical protein binding	Amyloid-beta precursor protein	Homo sapiens (human)
transition metal ion binding	Amyloid-beta precursor protein	Homo sapiens (human)
receptor ligand activity	Amyloid-beta precursor protein	Homo sapiens (human)
PTB domain binding	Amyloid-beta precursor protein	Homo sapiens (human)
protein serine/threonine kinase binding	Amyloid-beta precursor protein	Homo sapiens (human)
signaling receptor activator activity	Amyloid-beta precursor protein	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
endopeptidase activity	Presenilin-1	Homo sapiens (human)
aspartic-type endopeptidase activity	Presenilin-1	Homo sapiens (human)
calcium channel activity	Presenilin-1	Homo sapiens (human)
protein binding	Presenilin-1	Homo sapiens (human)
beta-catenin binding	Presenilin-1	Homo sapiens (human)
PDZ domain binding	Presenilin-1	Homo sapiens (human)
aspartic endopeptidase activity, intramembrane cleaving	Presenilin-1	Homo sapiens (human)
cadherin binding	Presenilin-1	Homo sapiens (human)
ATPase binding	Presenilin-1	Homo sapiens (human)
growth factor receptor binding	Presenilin-1	Homo sapiens (human)
protein binding	Presenilin-2	Homo sapiens (human)
aspartic endopeptidase activity, intramembrane cleaving	Presenilin-2	Homo sapiens (human)
protease binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
signaling receptor binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Sodium-dependent dopamine transporter	Homo sapiens (human)
dopamine:sodium symporter activity	Sodium-dependent dopamine transporter	Homo sapiens (human)
protein binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
monoamine transmembrane transporter activity	Sodium-dependent dopamine transporter	Homo sapiens (human)
dopamine binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
amine binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
protein-containing complex binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
metal ion binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
protein phosphatase 2A binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
heterocyclic compound binding	Sodium-dependent dopamine transporter	Homo sapiens (human)
norepinephrine:sodium symporter activity	Sodium-dependent dopamine transporter	Homo sapiens (human)
protein binding	Synaptic vesicular amine transporter	Homo sapiens (human)
monoamine transmembrane transporter activity	Synaptic vesicular amine transporter	Homo sapiens (human)
monoamine:proton antiporter activity	Synaptic vesicular amine transporter	Homo sapiens (human)
serotonin:sodium:chloride symporter activity	Synaptic vesicular amine transporter	Homo sapiens (human)
protein binding	Gamma-secretase subunit APH-1B	Homo sapiens (human)
protein-macromolecule adaptor activity	Gamma-secretase subunit APH-1B	Homo sapiens (human)
endopeptidase activator activity	Gamma-secretase subunit APH-1B	Homo sapiens (human)
protein binding	Nicastrin	Homo sapiens (human)
protein-macromolecule adaptor activity	Nicastrin	Homo sapiens (human)
aspartic endopeptidase activity, intramembrane cleaving	Nicastrin	Homo sapiens (human)
ATPase binding	Nicastrin	Homo sapiens (human)
growth factor receptor binding	Nicastrin	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Gamma-secretase subunit APH-1A	Homo sapiens (human)
enzyme binding	Gamma-secretase subunit APH-1A	Homo sapiens (human)
protein-macromolecule adaptor activity	Gamma-secretase subunit APH-1A	Homo sapiens (human)
endopeptidase activator activity	Gamma-secretase subunit APH-1A	Homo sapiens (human)
protein binding	Gamma-secretase subunit PEN-2	Homo sapiens (human)
enzyme binding	Gamma-secretase subunit PEN-2	Homo sapiens (human)
endopeptidase activator activity	Gamma-secretase subunit PEN-2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (88)

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	Amyloid-beta precursor protein	Homo sapiens (human)
dendrite	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular region	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular space	Amyloid-beta precursor protein	Homo sapiens (human)
nuclear envelope lumen	Amyloid-beta precursor protein	Homo sapiens (human)
cytoplasm	Amyloid-beta precursor protein	Homo sapiens (human)
mitochondrial inner membrane	Amyloid-beta precursor protein	Homo sapiens (human)
endosome	Amyloid-beta precursor protein	Homo sapiens (human)
early endosome	Amyloid-beta precursor protein	Homo sapiens (human)
endoplasmic reticulum	Amyloid-beta precursor protein	Homo sapiens (human)
endoplasmic reticulum lumen	Amyloid-beta precursor protein	Homo sapiens (human)
smooth endoplasmic reticulum	Amyloid-beta precursor protein	Homo sapiens (human)
Golgi apparatus	Amyloid-beta precursor protein	Homo sapiens (human)
Golgi lumen	Amyloid-beta precursor protein	Homo sapiens (human)
Golgi-associated vesicle	Amyloid-beta precursor protein	Homo sapiens (human)
cytosol	Amyloid-beta precursor protein	Homo sapiens (human)
plasma membrane	Amyloid-beta precursor protein	Homo sapiens (human)
clathrin-coated pit	Amyloid-beta precursor protein	Homo sapiens (human)
cell-cell junction	Amyloid-beta precursor protein	Homo sapiens (human)
synaptic vesicle	Amyloid-beta precursor protein	Homo sapiens (human)
cell surface	Amyloid-beta precursor protein	Homo sapiens (human)
membrane	Amyloid-beta precursor protein	Homo sapiens (human)
COPII-coated ER to Golgi transport vesicle	Amyloid-beta precursor protein	Homo sapiens (human)
axon	Amyloid-beta precursor protein	Homo sapiens (human)
growth cone	Amyloid-beta precursor protein	Homo sapiens (human)
platelet alpha granule lumen	Amyloid-beta precursor protein	Homo sapiens (human)
neuromuscular junction	Amyloid-beta precursor protein	Homo sapiens (human)
endosome lumen	Amyloid-beta precursor protein	Homo sapiens (human)
trans-Golgi network membrane	Amyloid-beta precursor protein	Homo sapiens (human)
ciliary rootlet	Amyloid-beta precursor protein	Homo sapiens (human)
dendritic spine	Amyloid-beta precursor protein	Homo sapiens (human)
dendritic shaft	Amyloid-beta precursor protein	Homo sapiens (human)
perikaryon	Amyloid-beta precursor protein	Homo sapiens (human)
membrane raft	Amyloid-beta precursor protein	Homo sapiens (human)
apical part of cell	Amyloid-beta precursor protein	Homo sapiens (human)
synapse	Amyloid-beta precursor protein	Homo sapiens (human)
perinuclear region of cytoplasm	Amyloid-beta precursor protein	Homo sapiens (human)
presynaptic active zone	Amyloid-beta precursor protein	Homo sapiens (human)
spindle midzone	Amyloid-beta precursor protein	Homo sapiens (human)
recycling endosome	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular exosome	Amyloid-beta precursor protein	Homo sapiens (human)
receptor complex	Amyloid-beta precursor protein	Homo sapiens (human)
early endosome	Amyloid-beta precursor protein	Homo sapiens (human)
membrane raft	Amyloid-beta precursor protein	Homo sapiens (human)
cell surface	Amyloid-beta precursor protein	Homo sapiens (human)
Golgi apparatus	Amyloid-beta precursor protein	Homo sapiens (human)
plasma membrane	Amyloid-beta precursor protein	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
smooth endoplasmic reticulum	Presenilin-1	Homo sapiens (human)
dendrite	Presenilin-1	Homo sapiens (human)
Golgi membrane	Presenilin-1	Homo sapiens (human)
kinetochore	Presenilin-1	Homo sapiens (human)
nucleus	Presenilin-1	Homo sapiens (human)
nuclear outer membrane	Presenilin-1	Homo sapiens (human)
nucleoplasm	Presenilin-1	Homo sapiens (human)
mitochondrion	Presenilin-1	Homo sapiens (human)
mitochondrial inner membrane	Presenilin-1	Homo sapiens (human)
endoplasmic reticulum	Presenilin-1	Homo sapiens (human)
endoplasmic reticulum membrane	Presenilin-1	Homo sapiens (human)
smooth endoplasmic reticulum	Presenilin-1	Homo sapiens (human)
rough endoplasmic reticulum	Presenilin-1	Homo sapiens (human)
Golgi apparatus	Presenilin-1	Homo sapiens (human)
centrosome	Presenilin-1	Homo sapiens (human)
plasma membrane	Presenilin-1	Homo sapiens (human)
cell cortex	Presenilin-1	Homo sapiens (human)
synaptic vesicle	Presenilin-1	Homo sapiens (human)
cell surface	Presenilin-1	Homo sapiens (human)
membrane	Presenilin-1	Homo sapiens (human)
aggresome	Presenilin-1	Homo sapiens (human)
cell junction	Presenilin-1	Homo sapiens (human)
growth cone	Presenilin-1	Homo sapiens (human)
neuromuscular junction	Presenilin-1	Homo sapiens (human)
early endosome membrane	Presenilin-1	Homo sapiens (human)
nuclear membrane	Presenilin-1	Homo sapiens (human)
ciliary rootlet	Presenilin-1	Homo sapiens (human)
azurophil granule membrane	Presenilin-1	Homo sapiens (human)
sarcolemma	Presenilin-1	Homo sapiens (human)
presynaptic membrane	Presenilin-1	Homo sapiens (human)
neuron projection	Presenilin-1	Homo sapiens (human)
neuronal cell body	Presenilin-1	Homo sapiens (human)
dendritic shaft	Presenilin-1	Homo sapiens (human)
membrane raft	Presenilin-1	Homo sapiens (human)
postsynapse	Presenilin-1	Homo sapiens (human)
glutamatergic synapse	Presenilin-1	Homo sapiens (human)
protein-containing complex	Presenilin-1	Homo sapiens (human)
gamma-secretase complex	Presenilin-1	Homo sapiens (human)
Golgi membrane	Presenilin-2	Homo sapiens (human)
kinetochore	Presenilin-2	Homo sapiens (human)
nuclear inner membrane	Presenilin-2	Homo sapiens (human)
early endosome	Presenilin-2	Homo sapiens (human)
endoplasmic reticulum	Presenilin-2	Homo sapiens (human)
endoplasmic reticulum membrane	Presenilin-2	Homo sapiens (human)
Golgi apparatus	Presenilin-2	Homo sapiens (human)
centrosome	Presenilin-2	Homo sapiens (human)
plasma membrane	Presenilin-2	Homo sapiens (human)
synaptic vesicle	Presenilin-2	Homo sapiens (human)
membrane	Presenilin-2	Homo sapiens (human)
presynaptic membrane	Presenilin-2	Homo sapiens (human)
protein-containing complex	Presenilin-2	Homo sapiens (human)
gamma-secretase complex	Presenilin-2	Homo sapiens (human)
cytoplasm	Sodium-dependent dopamine transporter	Homo sapiens (human)
plasma membrane	Sodium-dependent dopamine transporter	Homo sapiens (human)
cell surface	Sodium-dependent dopamine transporter	Homo sapiens (human)
membrane	Sodium-dependent dopamine transporter	Homo sapiens (human)
axon	Sodium-dependent dopamine transporter	Homo sapiens (human)
neuron projection	Sodium-dependent dopamine transporter	Homo sapiens (human)
neuronal cell body	Sodium-dependent dopamine transporter	Homo sapiens (human)
axon terminus	Sodium-dependent dopamine transporter	Homo sapiens (human)
membrane raft	Sodium-dependent dopamine transporter	Homo sapiens (human)
postsynaptic membrane	Sodium-dependent dopamine transporter	Homo sapiens (human)
dopaminergic synapse	Sodium-dependent dopamine transporter	Homo sapiens (human)
flotillin complex	Sodium-dependent dopamine transporter	Homo sapiens (human)
axon	Sodium-dependent dopamine transporter	Homo sapiens (human)
presynaptic membrane	Sodium-dependent dopamine transporter	Homo sapiens (human)
plasma membrane	Sodium-dependent dopamine transporter	Homo sapiens (human)
neuronal cell body membrane	Sodium-dependent dopamine transporter	Homo sapiens (human)
centrosome	Synaptic vesicular amine transporter	Homo sapiens (human)
plasma membrane	Synaptic vesicular amine transporter	Homo sapiens (human)
synaptic vesicle	Synaptic vesicular amine transporter	Homo sapiens (human)
membrane	Synaptic vesicular amine transporter	Homo sapiens (human)
axon	Synaptic vesicular amine transporter	Homo sapiens (human)
dendrite	Synaptic vesicular amine transporter	Homo sapiens (human)
secretory granule membrane	Synaptic vesicular amine transporter	Homo sapiens (human)
synaptic vesicle membrane	Synaptic vesicular amine transporter	Homo sapiens (human)
intracellular membrane-bounded organelle	Synaptic vesicular amine transporter	Homo sapiens (human)
clathrin-sculpted monoamine transport vesicle membrane	Synaptic vesicular amine transporter	Homo sapiens (human)
dopaminergic synapse	Synaptic vesicular amine transporter	Homo sapiens (human)
terminal bouton	Synaptic vesicular amine transporter	Homo sapiens (human)
synaptic vesicle membrane	Synaptic vesicular amine transporter	Homo sapiens (human)
Golgi membrane	Gamma-secretase subunit APH-1B	Homo sapiens (human)
endoplasmic reticulum membrane	Gamma-secretase subunit APH-1B	Homo sapiens (human)
plasma membrane	Gamma-secretase subunit APH-1B	Homo sapiens (human)
endosome membrane	Gamma-secretase subunit APH-1B	Homo sapiens (human)
membrane	Gamma-secretase subunit APH-1B	Homo sapiens (human)
transport vesicle	Gamma-secretase subunit APH-1B	Homo sapiens (human)
gamma-secretase complex	Gamma-secretase subunit APH-1B	Homo sapiens (human)
endoplasmic reticulum	Gamma-secretase subunit APH-1B	Homo sapiens (human)
Golgi membrane	Nicastrin	Homo sapiens (human)
lysosomal membrane	Nicastrin	Homo sapiens (human)
early endosome	Nicastrin	Homo sapiens (human)
endoplasmic reticulum	Nicastrin	Homo sapiens (human)
endoplasmic reticulum membrane	Nicastrin	Homo sapiens (human)
Golgi apparatus	Nicastrin	Homo sapiens (human)
plasma membrane	Nicastrin	Homo sapiens (human)
focal adhesion	Nicastrin	Homo sapiens (human)
synaptic vesicle	Nicastrin	Homo sapiens (human)
endosome membrane	Nicastrin	Homo sapiens (human)
membrane	Nicastrin	Homo sapiens (human)
azurophil granule membrane	Nicastrin	Homo sapiens (human)
sarcolemma	Nicastrin	Homo sapiens (human)
melanosome	Nicastrin	Homo sapiens (human)
presynaptic membrane	Nicastrin	Homo sapiens (human)
extracellular exosome	Nicastrin	Homo sapiens (human)
gamma-secretase complex	Nicastrin	Homo sapiens (human)
plasma membrane	Nicastrin	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
Golgi membrane	Gamma-secretase subunit APH-1A	Homo sapiens (human)
early endosome	Gamma-secretase subunit APH-1A	Homo sapiens (human)
endoplasmic reticulum	Gamma-secretase subunit APH-1A	Homo sapiens (human)
endoplasmic reticulum membrane	Gamma-secretase subunit APH-1A	Homo sapiens (human)
Golgi apparatus	Gamma-secretase subunit APH-1A	Homo sapiens (human)
plasma membrane	Gamma-secretase subunit APH-1A	Homo sapiens (human)
synaptic vesicle	Gamma-secretase subunit APH-1A	Homo sapiens (human)
endosome membrane	Gamma-secretase subunit APH-1A	Homo sapiens (human)
membrane	Gamma-secretase subunit APH-1A	Homo sapiens (human)
Golgi cisterna membrane	Gamma-secretase subunit APH-1A	Homo sapiens (human)
presynaptic membrane	Gamma-secretase subunit APH-1A	Homo sapiens (human)
gamma-secretase complex	Gamma-secretase subunit APH-1A	Homo sapiens (human)
endoplasmic reticulum	Gamma-secretase subunit APH-1A	Homo sapiens (human)
Golgi membrane	Gamma-secretase subunit PEN-2	Homo sapiens (human)
endoplasmic reticulum	Gamma-secretase subunit PEN-2	Homo sapiens (human)
endoplasmic reticulum membrane	Gamma-secretase subunit PEN-2	Homo sapiens (human)
Golgi apparatus	Gamma-secretase subunit PEN-2	Homo sapiens (human)
plasma membrane	Gamma-secretase subunit PEN-2	Homo sapiens (human)
endosome membrane	Gamma-secretase subunit PEN-2	Homo sapiens (human)
membrane	Gamma-secretase subunit PEN-2	Homo sapiens (human)
Golgi cisterna membrane	Gamma-secretase subunit PEN-2	Homo sapiens (human)
presynaptic membrane	Gamma-secretase subunit PEN-2	Homo sapiens (human)
gamma-secretase complex	Gamma-secretase subunit PEN-2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (30)

Assay ID	Title	Year	Journal	Article
AID475533	Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in transgenic 2576 mouse brain at 3 mg/kg, po	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
AID475536	Bioavailability in rat	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
AID475517	Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
AID475532	Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in brain of po dosed human APP transgenic YAC mouse assessed as minimum effective dose	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
AID475535	Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in CSF of po dosed Sprague-Dawley rat	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
AID475537	Half life in rat	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
AID475534	Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in brain of po dosed Sprague-Dawley rat	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1254133	Inhibition of CYP3A4 (unknown origin) preincubated with protein for 30 mins followed by substrate addition	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1254137	Inhibition of CYP2C9 (unknown origin) preincubated with protein for 30 mins followed by substrate addition	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1254120	Inhibition of gamma-secretase in HEK293 cell membranes using SPC99-Lon as substrate assessed as formation of amyloid beta 40 after 1 hr by electrochemiluminescence-based immunoassay	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1254124	Ratio of drug level in brain to plasma in Sprague-Dawley rat at 10 mg/kg, po	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1254123	AUC (0 to 6 hrs) in Sprague-Dawley rat at 10 mg/kg, po by LC-MS/MS analysis	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1254122	Inhibition of gamma-secretase in HEK293 cells using human APP Swedish/London double mutant as substrate assessed as formation of amyloid beta 42 after 5 to 6 hrs by sandwich immunoassay	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1661513	In vivo modulation of gamma secretase in APP-Swedish transgenic mouse assessed as reduction in Abeta42 production by measuring remaining Abeta42 level at 10 mg/kg, po measured after 4 hrs by ELISA or AlphaLISA assay relative to control	2020	Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15	Stepwise Design of γ-Secretase Modulators with an Advanced Profile by Judicious Coordinated Structural Replacements and an Unconventional Phenyl Ring Bioisostere.
AID1254125	Selectivity ratio of IC50 for human presenilin-2 to IC50 for human presenilin-1	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1628295	Inhibition of gamma secretase in HEK293 cells expressing APP assessed as reduction in amyloid beta levels	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases.
AID1254134	Inhibition of CYP2D6 (unknown origin) co-incubated with substrate and protein	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID258051	DEA-extractable brain Abeta(40) lowering 4 hrs after oral dosing in APP-YAC mice	2006	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2	4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
AID1254121	Inhibition of gamma-secretase in HEK293 cells using human APP Swedish/London double mutant as substrate assessed as formation of amyloid beta 40 after 5 to 6 hrs by sandwich immunoassay	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1254126	Antialzheimer activity in Sprague-Dawley rat assessed as reduction of total amylod beta level in plasma at 10 mg/kg, po after 3 hrs by immunoassay relative to vehicle-treated control	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1254136	Inhibition of CYP2C9 (unknown origin) co-incubated with substrate and protein	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1254135	Inhibition of CYP2D6 (unknown origin) preincubated with protein for 30 mins followed by substrate addition	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID258050	Inhibition of human gamma-secretase in SHSY5Y neuroblastoma cells	2006	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2	4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
AID1254132	Inhibition of CYP3A4 (unknown origin) co-incubated with substrate and protein	2015	Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22	Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
AID1798949	Cell-Based Assay for Amyloid-beta Accumulation from Article 10.1016/j.bmcl.2005.10.009: \\4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.\\	2006	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2	4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	4 (20.00)	29.6817
2010's	11 (55.00)	24.3611
2020's	5 (25.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (5.00%)	5.53%
Reviews	2 (10.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	17 (85.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
carbamates [no description available]	2.07	1	amino-acid anion
flurbiprofen Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.	2.07	1	fluorobiphenyl; monocarboxylic acid	antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug
7-amino-4-chloro-3-methoxy-2-benzopyran-1-one [no description available]	3.23	1	isocoumarins
alanine Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.	2.07	1	alanine zwitterion; alanine; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid	EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor; fundamental metabolite
manganese Manganese: A trace element with atomic symbol Mn, atomic number 25, and atomic weight 54.94. It is concentrated in cell mitochondria, mostly in the pituitary gland, liver, pancreas, kidney, and bone, influences the synthesis of mucopolysaccharides, stimulates hepatic synthesis of cholesterol and fatty acids, and is a cofactor in many enzymes, including arginase and alkaline phosphatase in the liver. (From AMA Drug Evaluations Annual 1992, p2035). manganese(4+) : A manganese cation that is monoatomic and has a formal charge of +4.	2.07	1	elemental manganese; manganese group element atom	Escherichia coli metabolite; micronutrient
tarenflurbil tarenflurbil: R-enantiomer of flurbiprofen but not a COX inhibitor; modulates NF-kB, gamma-secretase, amyloid beta-protein;	4.09	2	flurbiprofen
imatinib mesylate imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.	2.31	1	methanesulfonate salt	anticoronaviral agent; antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor
sulindac Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.	2.07	1	monocarboxylic acid; organofluorine compound; sulfoxide	analgesic; antineoplastic agent; antipyretic; apoptosis inducer; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug; tocolytic agent
n-(n-(3,5-difluorophenacetyl)alanyl)phenylglycine tert-butyl ester DAPT : A dipeptide consisting of alanylphenylglycine derivatised as a 3,5-difluorophenylacetamide at the amino terminal and a tert-butyl ester at the carboxy terminal. A gamma-secretase inhibitor.	3.23	1	carboxylic ester; difluorobenzene; dipeptide; tert-butyl ester	EC 3.4.23.46 (memapsin 2) inhibitor
sulindac sulfide sulindac sulfide: sulfated analog of indomethacin & inhibitor of prostaglandin synthesis in vitro; RN given refers to cpd without isomeric designation; structure given in first source. sulindac sulfide : An aryl sulfide that is a metabolite of sulindac. A non-steroidal anti-inflammatory drug, which also has anticancer activity.	2.07	1	aryl sulfide; monocarboxylic acid; organofluorine compound	antineoplastic agent; apoptosis inducer; non-steroidal anti-inflammatory drug
l 685458 L 685458: a gamma-secretase inhibitor; structure in first source. L-685,458 : A peptide and carboxamide that is L-leucyl-L-phenylalaninamide, L-Leu-L-Phe-NH2, which has been acylated on the N-terminus by a Phe-Phe hydroxyethylene dipeptide isotere, 2R-benzyl-5S-tert-butoxycarbonylamino-4R-hydroxy-6-phenylhexanoic acid. Compounds based on the structure of L-685,458 are potent inhibitors of gamma-secretase, which mediates the final catalytic step that generates the amyloid beta-peptide (Abeta), which assembles into the neurotoxic aggregates in the brains of sufferers of Alzheimer's disease.	4.38	3	carbamate ester; monocarboxylic acid amide; peptide; secondary alcohol	EC 3.4.23.46 (memapsin 2) inhibitor; peptidomimetic
mk 0752 [no description available]	3.23	1
ly 450139 [no description available]	4.09	2	peptide
ly 411575 [no description available]	4.09	2	dibenzoazepine; difluorobenzene; lactam; secondary alcohol	EC 3.4.23.46 (memapsin 2) inhibitor
4-(2-((1r)-1-(((4-chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid [no description available]	4.09	2	sulfonamide
begacestat [no description available]	4.09	2
incb-018424 [no description available]	2.31	1	nitrile; pyrazoles; pyrrolopyrimidine	antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
piperidines Piperidines: A family of hexahydropyridines.	2.07	1
pf 3084014 nirogacestat: an antineoplastic agent. nirogacestat : A member of the class of imidazoles that is 1H-imidazole substituted by a 1-[(2,2-dimethylpropyl)amino]-2-methylpropan-2-yl group at position 1 and a {N-[(2S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-L-norvalyl}amino group at position 4. It is a gamma-secretase inhibitor whose hydrobromide salt is indicated for adult patients with progressing desmoid tumours who require systemic treatment.	3.23	1
bms 708163 BMS 708163: structure in first source	3.14	1	oxadiazole; ring assembly
ro 4929097 [no description available]	3.23	1	dibenzoazepine; dicarboxylic acid diamide; lactam; organofluorine compound	EC 3.4.23.46 (memapsin 2) inhibitor
amyloid beta-peptides amyloid beta-protein (1-40): although acutely neurotoxic in both rat & monkey cerebral cortex, neuronal degeneration in primates resembles more closely to that found in Alzheimer's disease; amino acid sequence has been determined	2.03	1

Condition	Relationship Strength	Studies	Trials
Acute Confusional Senile Dementia [description not available]	5.75	7	1
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	5.75	7	1
Carcinogenesis The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.	3.04	1	0
Cirrhosis [description not available]	3.04	1	0
Innate Inflammatory Response [description not available]	3.04	1	0
Benign Neoplasms [description not available]	3.04	1	0
Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.	3.04	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	3.04	1	0
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	3.04	1	0
Congenital Zika Syndrome [description not available]	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.55	2	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1	0
Leukemia, Lymphoblastic, Acute, T Cell [description not available]	2.31	1	0
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma A leukemia/lymphoma found predominately in children and young adults and characterized LYMPHADENOPATHY and THYMUS GLAND involvement. It most frequently presents as a lymphoma, but a leukemic progression in the bone marrow is common.	2.31	1	0
Amyloid Deposits [description not available]	2.05	1	0
Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.	2.05	1	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	3.46	1	1

mrk 560

Description

Cross-References

Synonyms (25)

Research Excerpts

Compound-Compound Interactions

Bioavailability

Dosage Studied

Protein Targets (19)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (277)

Molecular Functions (81)

Ceullar Components (88)

Bioassays (30)

Research

Studies (20)

Market Indicators

Research Demand Index: 19.43

Study Types

mrk 560

Description

Cross-References

Synonyms (25)

Research Excerpts

Compound-Compound Interactions

Bioavailability

Dosage Studied

Protein Targets (19)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (277)

Molecular Functions (81)

Ceullar Components (88)

Bioassays (30)

Research

Studies (20)

Market Indicators

Research Demand Index: 19.43

Study Types

Related Drugs (22)

Related Conditions (17)