Information on EC 5.4.99.7 - Lanosterol synthase

Word Map on EC 5.4.99.7
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Specify your search results
Select one or more organisms in this record:
Show additional data
Do not include text mining results
Include (text mining) results (more...)
Include results (AMENDA + additional results, but less precise; more...)


The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY hide
5.4.99.7
-
RECOMMENDED NAME
GeneOntology No.
Lanosterol synthase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
(3S)-2,3-epoxy-2,3-dihydrosqualene = lanosterol
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
cyclization
-
-
-
-
group transfer
-
-
intramolecular
-
isomerization
-
-
-
-
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
lanosterol biosynthesis
-
-
cholesterol biosynthesis
-
-
Steroid biosynthesis
-
-
Metabolic pathways
-
-
Biosynthesis of secondary metabolites
-
-
Biosynthesis of antibiotics
-
-
SYSTEMATIC NAME
IUBMB Comments
(S)-2,3-Epoxysqualene mutase (cyclizing, lanosterol-forming)
-
CAS REGISTRY NUMBER
COMMENTARY hide
9032-71-7
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
UniProt
Manually annotated by BRENDA team
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
Cynomolgus
-
-
Manually annotated by BRENDA team
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
protozoa
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
strain SCY876
-
-
Manually annotated by BRENDA team
Saccharomyces cerevisiae SCY876 and BTY6-5-3
-
-
-
Manually annotated by BRENDA team
strain SMY8
SwissProt
Manually annotated by BRENDA team
strain STY2
-
-
Manually annotated by BRENDA team
strain TKW14
-
-
Manually annotated by BRENDA team
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
yeasts
-
-
-
Automatic Mining of ENzyme DAta
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
physiological function
-
functional role of the Cys703 residue in stabilizing the bicyclic C-8 cation and the rearranged intermediate or interacting with Phe699
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(3R)-Squalene epoxide
Epilanosterol
show the reaction diagram
-
-
-
-
(3S)-2,3-epoxy-2,3-dihydrosqualene
achilleol A
show the reaction diagram
(3S)-2,3-epoxy-2,3-dihydrosqualene
lanosterol
show the reaction diagram
(3S)-2,3-epoxy-2,3-dihydrosqualene
lanosterol + (13alphaH)-isomalabarica-14(26),17E,21-trien-3beta-ol
show the reaction diagram
-
reaction of mutant V454I
-
-
?
(3S)-2,3-epoxy-2,3-dihydrosqualene
lanosterol + (13alphaH)-isomalabarica-14(26),17E,21-trien-3beta-ol + protosta-16,24-dien-3beta-ol
show the reaction diagram
-
reaction of mutant Q450H/V454I
-
-
?
(3S)-2,3-epoxy-2,3-dihydrosqualene
lanosterol + achilleol A
show the reaction diagram
-
reaction of C457G/T509G
achilleol A is the main product
-
?
(3S)-2,3-epoxy-2,3-dihydrosqualene
lanosterol + achilleol A + 13alphaH-isomalabarica-14(26),17E,21-trien-3beta-ol
show the reaction diagram
-
reaction of mutant H234W/Y510V
lanosterol is the main product
-
?
(3S)-2,3-epoxy-2,3-dihydrosqualene
lanosterol + parkeol + 9beta-lanosta-7,24-dien-3beta-ol
show the reaction diagram
-
reaction of mutants T384Y, T384Y/Q450H, and T384Y/V454I
-
-
?
(3S)-2,3-epoxy-2,3-dihydrosqualene
parkeol
show the reaction diagram
(3S)-2,3-epoxy-2,3-dihydrosqualene
protosta-12,24-dien-3-beta-ol
show the reaction diagram
-
reaction of mutant H232T
-
-
?
(3S)-2,3-oxidosqualene
?
show the reaction diagram
-
two essential histidine residues per active site are necessary for complete activity
-
?
(3S)-2,3-oxidosqualene
lanosterol
show the reaction diagram
(3S)-Squalene epoxide
?
show the reaction diagram
(3S)-squalene-2,3-epoxide
lanosterol
show the reaction diagram
-
-
-
-
?
(S)-2,3-epoxysqualene
lanosterol
show the reaction diagram
(S)-2,3-oxidosqualene
lanosterol
show the reaction diagram
(S)-squalene-2,3-epoxide
Lanosterol
show the reaction diagram
2,3-monoepoxysqualene
lanosterol
show the reaction diagram
2,3-oxidosqualene
lanosterol
show the reaction diagram
2,3:22,23-diepoxysqualene
24(S),25-epoxylanosterol
show the reaction diagram
27-norsqualene
30-norlanosterol + 26-normalabaricatriene
show the reaction diagram
-
-
-
-
?
29-norsqualene
(2S,4aS,6aR,7R,10aR,12aR)-1,1,4a,6a,10a-pentamethyl-7-(4-methylpent-3-en-1-yl)-1,2,3,4,4a,5,6,6a,7,8,9,10,10a,11,12,12a-hexadecahydrochrysen-2-ol + (2S,4aS,6aS,7R,10aS,12aR)-1,1,4a,6a,10a-pentamethyl-7-(4-methylpent-3-en-1-yl)-1,2,3,4,4a,5,6,6a,7,8,9,10,10a,11,12,12a-hexadecahydrochrysen-2-ol
show the reaction diagram
-
-
-
-
?
3-[(3E,7E,15E)-16-ethyl-3,7,12,20-tetramethylhenicosa-3,7,11,15,19-pentaen-1-yl]-2,2-dimethyloxirane
?
show the reaction diagram
-
ethylation at C10 or C15
-
-
?
dioxidosqualene
24(S),25-epoxylanosterol
show the reaction diagram
oxidosqualene
lanosterol
show the reaction diagram
-
-
-
-
?
squalene
?
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
(3S)-2,3-epoxy-2,3-dihydrosqualene
lanosterol
show the reaction diagram
(3S)-2,3-oxidosqualene
lanosterol
show the reaction diagram
(S)-2,3-epoxysqualene
lanosterol
show the reaction diagram
(S)-2,3-oxidosqualene
lanosterol
show the reaction diagram
-
-
-
-
?
(S)-squalene-2,3-epoxide
Lanosterol
show the reaction diagram
2,3-monoepoxysqualene
lanosterol
show the reaction diagram
2,3-oxidosqualene
lanosterol
show the reaction diagram
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
potassium phosphate
-
high concentrations stimulate
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(14-trans)-28-methylidene-2,3:14,15-dioxidoundecanorsqualene
(18E)-29-Methylidene-2,3-oxidohexanorsqualene
(18E)-29-methylidene-2,3-oxidosqualene
(18E)-29-methylidene-20,21,22,23,24,30-hexanor-2,3-oxidosqualene
(18Z)-29-Methylidene-2,3-oxidohexanorsqualene
(18Z)-29-methylidene-2,3-oxidosqualene
(18Z)-29-methylidene-20,21,22,23,24,30-hexanor-2,3-oxidosqualene
(2-trans)-1-methylidene-2,3-oxido-1'-norsqualene
(22E)-24-methylidene-30-nor-2,3-oxidosqualene
(22Z)-24-methylidene-30-nor-2,3-oxidosqualene
(2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-yl 3-biphenyl-4-ylpropyl ether
(2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-yl 3-phenylpropyl ether
(2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-yl hexyl ether
(3-trans-7E,11E,15E)-3,4:19,20-diepoxy-7,12,16,20-tetramethyl-1,7,11,15-henicosatetraene
(3R,4S,7E)-15,16-epoxy-3-ethylthio-8,12,16-trimethyl-1,7,11-heptadecatrien-4-ol
(3R,4S,7E,11E)-15,16-epoxy-8,12,16-trimethyl-3-phenylthio-1,7,11-heptadecatrien-4-ol
(3R,4S,7E,11E,15E)-19,20-epoxy-3-ethylthio-7,12,16,20-tetramethyl-1,7,11,15-henicosatetraen-4-ol
(4-Benzenesulfonyl-piperazin-1-yl)-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone
(4-bromophenyl)[4-[6-(cyclopropylmethylmethylamino)hexyloxy]phenyl]methanone
-
IC50: 31.8 nM
(4-bromophenyl)[4-[6-[(3-hydroxypropyl)methylamino]-hexyloxy]phenyl]methanone
-
IC50: 15.7 nM
(4aalpha,5alpha,6alpha,8abeta)-Decahydro-5,8a-dimethyl-2-(1,5,9-trimethyldecyl)-6-isoquinolinol
-
and simplified analogues
(5E,9E)-13,14-epoxy-6,10,14-trimethyl-1-methylthio-1,5,9-pentadecatriene
(5E,9E,13E)-17,18-epoxy-5,10,14,18-tetramethyl-1-methylthio-1,5,9,13-nonadecatetraene
(5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-(trimethylsilylethynyl)tricosa-2,5,9,13,17-pentaene
-
+ (5Z,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-(trimethylsilylethynyl)tricosa-2,5,9,13,17-pentaene, IC50: 0.06 mM
(5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-vinyl-2,5,9,13,17-tricosapentaene
(5E,9E,13E,17E)-21,22-epoxy-5-ethynyl-2,9,14,18,22-pentamethyltricosa-2,5,9,13,17-pentaene
(5Z,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-(trimethylsilylethynyl)tricosa-2,5,9,13,17-pentaene
-
+ (5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-(trimethylsilylethynyl)tricosa-2,5,9,13,17-pentaene, IC50: 0.06 mM
(5Z,9E,13E,17E)-21,22-epoxy-5-ethynyl-2,9,14,18,22-pentamethyltricosa-2,5,9,13,17-pentaene
(6E)-10-Aza-10,11-dihydrosqualene-2,3-epoxide
(6E,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene
(6E,10E,14E,18E)-22,23-epoxy-6-ethynyl-2,10,15,19,23-pentamethyltetracosa-2,6,10,14,18-pentaene
(6Z)-10-Aza-10,11-dihydrosqualene-2,3-epoxide
(6Z,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-(2-methylthiovinyl)-2,6,10,14,18-tetracosapentaene
(6Z,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene
(6Z,10E,14E,18E)-22,23-epoxy-6-ethynyl-2,10,15,19,23-pentamethyltetracosa-2,6,10,14,18-pentaene
(Z)-3-[4-(4-bromobenzoyl)phenacylidene]quinuclidine
1,2-dilinoleoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
26% inhibition at 0.5 microM, no inhibition at 0.25 microM
1,2-dimyristoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
72% inhibition at 0.5 microM, 51% at 0.25 microM
1,2-dioleoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
57% inhibition at 0.5 microM, 42% at 0.25 microM
1,2-dipalmitoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
24% inhibition at 0.5 microM, 4% at 0.25 microM
1-(2-methyl-4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
1-(2-oxazolinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
-
87% inhibition at 0.001 mM
1-(2-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
-
8% inhibition at 0.001 mM
1-(2-thiazolinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
-
complete inhibition at 0.001 mM
1-(4-iodophenylsulfonyl)-4-(1-(4-pyridyl)piperidon-4-ylcarbonyl)piperazine
-
IC50: 82 nM
1-(4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
1-linolenoyl-2-palmitoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
26% inhibition at 0.5 microM, 5% inhibition at 0.25 microM
1-linoleoyl-2-linolenoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
45% inhibition at 0.5 microM, 18% at 0.25 microM
1-linoleoyl-2-myristoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
38% inhibition at 0.5 microM, 22% at 0.25 microM
1-linoleoyl-2-oleoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
31% inhibition at 0.5 microM, 8% at 0.25 microM
1-linoleoyl-2-palmitoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
27% inhibition at 0.5 microM, 3% at 0.25 microM
1-myristoyl-2-palmitoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
45% inhibition at 0.5 microM, 35% at 0.25 microM
1-oleoyl-2-linolenoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
29% inhibition at 0.5 microM, 7% at 0.25 microM
1-oleoyl-2-linoleoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
40% inhibition at 0.5 microM, 9% at 0.25 microM
1-oleoyl-2-palmitoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
46% inhibition at 0.5 microM, 24% at 0.25 microM
1-palmitoyl-2-linoleoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
20% inhibition at 0.5 microM, no inhibition at 0.25 microM
1-palmitoyl-2-oleoyl-3-(alpha-D-galactopyranosyl-1,6-beta-D-galactopyranosyl)-sn-glycerol
-
21% inhibition at 0.5 microM, 4% at 0.25 microM
1-[4-(trifluoromethoxy)phenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmeth yl]-piperazine
-
-
1-[4-chlorobenzyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
-
1-[4-chlorophenylcarbonyl]-4-[4-(1-methyl-pyrazol-4-yl)phenylmethyl]-piperazine
-
inactive at 200 nM
1-[4-chlorophenylcarbonyl]-4-[4-(5-methyl-1,2,4-oxadiazol-3-yl)phenylmethyl]-piperazine
-
inactive at 200 nM
1-[4-chlorophenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
-
-
1-[4-chlorophenylcarbonyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
-
-
1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-1-yl)phenylmethyl]-piperazine
-
inactive at 200 nM
1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-3-yl)phenylmethyl]-piperazine
-
inactive at 200 nM
1-[4-chlorophenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
-
1-[4-chlorophenylsulfonyl]-4-[3-(pyridin-4-yl)phenylmethyl]-piperazine
-
-
1-[4-chlorophenylsulfonyl]-4-[4-(4-methylpiperazin-1-yl)phenylmethyl]-piperazine
-
-
1-[4-chlorophenylsulfonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
-
-
1-[4-chlorophenylsulfonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
-
1-[4-methoxyphenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
-
1-[4-trifluoroacetyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
-
inactive at 200 nM
10,15-desdimethyl-2,3-oxidosqualene
-
-
10-desmethyl-2,3-oxidosqualene
-
-
18,19-dihydro-29-methylidene-2,3-oxidosqualene
-
IC50: 0.1 mM
18-heptanor-2,3-oxidosqualene
19-aza-18,19,22,23-tetrahydrosqualene-2,3-epoxide
19-Aza-18,19,22,3-tetrahydrosqualene-2,3-epoxide
19-Aza-18,19,22,3-tetrahydrosqualene-2,3-epoxide N-oxide
19-Azasqualene
19-Azasqualene-2,3-epoxide
2,3,18,19-Dioxidosqualene stereoisomers
-
-
2,3-Epoxy-10-aza-10,11-dehydrosqualene
2,3-Iminosqualenene
-
-
-
2-Aza-2,3-dihydrosqualene
2-Aza-2,3-dihydrosqualene alcohol
-
-
-
2-Aza-2,3-dihydrosqualene N-oxide
2-[(4E,8E)-12,13-epoxy-5,9,13-trimethyl-4,8-tetradecadienylidene]-1,3-dithiane
2-[(4E,8E,12E)-16,17-epoxy-4,9,13,17-tetramethyl-4,8,12-octadecatrienylidene]-1,3-benzodithiole
2-[(4E,8E,12E)-16,17-epoxy-4,9,13,17-tetramethyl-4,8,12-octadecatrienylidene]-1,3-dithiane
2-[(4E,8E,12E,16E)-20,21-epoxy-4,8,13,17,21-pentamethyl-4,8,12,16-docosatetraenylidene]-1,3-dithiane
22,23-Epoxy-2-aza-2,3-dihydrosqualene
-
slight
22,23-epoxy-2-aza-2,3-dihydrosqualene-N-oxide
-
0.01 mM, 14% inhibition
27,28-bisnoroxidosqualene
-
irreversible inhibition
27-norsqualene
-
-
28-noroxidosqualene
-
-
29-Methylidene-2,3-oxidohexanorsqualene
-
-
-
29-norsqualene
-
-
3-(3,7-Dimethyl-octadeca-3,7,11,15-tetraenyl)-2,2-dimethyl-oxirane
3-(biphenyl-4-yloxy)-N,N-dimethylpropan-1-amine
3-beta-(beta-dimethylaminoethoxy)-androst-5en-17one
3-carboxy-4-nitrophenyldithio-1,1',2-tris-nor-squalene
-
-
3-[(4-chlorobenzoyl)-4-phenoxy]quinuclidin-3-ol
3-[(4-chlorobenzoyl)-4-phenoxy]quinuclidine
3-[2-(4-bromobenzophenone)ethynyl]quinuclidin-3-ol
3-[Methyl-(4,8,13,17,21-pentamethyl-docosa-4,8,12,16,20-pentaenyl)-amino]-propan-1-ol
-
0.01 mM, 2% inhibition
3beta-(2-diethylaminoethoxy)androst-5-en-17-one hydrochloride
-
U18666A
4,4,10beta-trimethyl-trans-decal-3beta-ol
-
specific inhibitor
4-(4-bromobenzoyl)-1-(1-(4-pyridyl)piperidin-4-ylcarbonyl)piperazine
-
96% inhibition at 0.001 mM
4-(4-bromophenylmethyl)-1-(1-(4-pyridyl)piperidin-4-ylcarbonyl)piperazine
-
complete inhibition at 0.001 mM
4-chloro-N-(4-{4-[(dimethylamino)methyl]phenyl}cyclohexyl)-N-methylbenzamide
-
BIBX 79
6-desmethyl-2,3-oxidosqualene
-
-
7-(4'-allylmethylamino-but-2-ynyloxy)chromen-2-one
-
7-(morpholinyl-N-hexyloxy)chromen-2-one
-
7-(morpholinyl-N-octanyloxy)chromen-2-one
-
7-(piperidinyl-N-hexyloxy)chromen-2-one
-
7-[10-(allylmethylamino)-decyloxy]chromen-2-one
-
7-[4'-(N-diethylamino)-but-2-ynyloxy]chromen-2-one
-
7-[4'-(N-pyrrolidyn)-but-2-ynyloxy]chromen-2-one
-
7-[6-(allylmethylamino)-hexyloxy]-chromen-2-one
-
7-[8'(dimethylamino-N-octyloxy)]chromen-2-one
-
allyl-6-[4-(4-bromophenyl)-1H-benzo[d][1,2]oxazin-7-yloxy]hexylmethylamine
-
IC50: 4.1 nM
allyl[6-[1-(4-bromophenyl)-3,4-dihydroisoquinolin-6-yloxy]hexyl]methylamine
-
IC50: 7.9 nM
allyl[6-[1-(4-bromophenyl)isoquinolin-6-yloxy]hexyl]methylamine
-
IC50: 3.5 nM
allyl[6-[3-(4-bromophenyl)-1-methyl-1H-indazol-6-yloxy]hexyl]methylamine
-
IC50: 19.6 nM
allyl[6-[3-(4-bromophenyl)benzo[b]thiophen-6-yloxy]hexyl]methylamine
-
IC50: 5.6 nM
allyl[6-[3-(4-bromophenyl)benzo[d]isothiazol-6-yloxy]hexyl]methylamine
-
IC50: 2.9 nM
allyl[6-[4-(4-bromophenyl)-2H-chromen-7-yloxy]hexyl]methylamine
-
IC50: 11.4 nM
allyl[6-[4-(4-bromophenyl)quinazolin-7-yloxy]hexyl]methylamine
-
IC50: 12.3 nM
allyl[6-[4-(6-bromo-1,1-dioxobenzo[d]isothiazol-3-yl)phenoxy]hexyl]methylamine
-
IC50: 7.8 nM
azasqualene alcohol
-
0.01 mM, 13% inhibition
azasqualene alcohol N-oxide
BIBB 515
-
Chloroquine
-
-
cholesterol
dehydrocostus lactone
-
isolated from Laurus nobilis extract, 22% inhibition at 0.25 mM, 63% inhibition at 0.5 mM
diethyl dicarbonate
-
maximal inactivation at neutral pH, reactivation by hydroxylamine
diethyl-(4,8,13,17,21-pentamethyl-docosa-4,8,12,16,20-pentaenyl)-aminoxide
Diethyl-(4,8,13,17,21-pentamethyl-docosa-4,8,12,16,20-pentaenyl)-ammonium
dodecyl-maleimide
mutant C457D shows 41.6% inhibition at 1 mM, 10.0% at 0.2 mM, and 7.2% at 0.025 mM, mutant C457D/E526A shows 9.0% inhibition at 0.2 mM and 0.0% at 0.025 mM, mutant C457D/A525C shows 86.0% inhibition at 1 mM, 30.5% at 0.2 mM, and 1.0% at 0.025 mM, mutant C457D/E526C shows 89.6% inhibition at 0.2 mM, 74.7% at 0.025 mM, and 45.1% at 0.01 mM
-
eremanthine
-
isolated from Laurus nobilis extract, 12% inhibition at 0.25 mM, 70% inhibition at 0.5 mM
ethanol extract from Angelica keiskei leaves
-
11% inhibition at 0.3 mg/ml
-
ethanol extract from Basella rubra leaves
-
5% inhibition at 0.3 mg/ml
-
ethanol extract from Chrysanthemum morifolium flowers
-
13% inhibition at 0.3 mg/ml
-
ethanol extract from Chrysanthemum morifolium leaves
-
7% inhibition at 0.3 mg/ml
-
ethanol extract from Colocasia esculenta rhizomes
-
55% inhibition at 0.3 mg/ml
-
ethanol extract from Cryptotaenia japonica leaves
-
10% inhibition at 0.3 mg/ml
-
ethanol extract from Glycine max immature seeds
-
14% inhibition at 0.3 mg/ml
-
ethanol extract from Oenanthe stolonifera leaves
-
13% inhibition at 0.3 mg/ml
-
ethanol extract from Perilla frutescens leaves
-
5% inhibition at 0.3 mg/ml
-
ethanol extract from Petasites japonicus buds
-
6% inhibition at 0.3 mg/ml
-
ethanol extract from Zingiber officinale buds
-
14% inhibition at 0.3 mg/ml
-
ethanol extract from Zingiber officinale rhizomes
-
6% inhibition at 0.3 mg/ml
-
Iminosqualene
N,N-Diethylazasqualene
-
non-competitive
N,N-Diethylazasqualene N-oxide
-
competitive
N,N-dimethyl-N-(4-methylenebenzophenonyl)amine
-
IC50: 0.005 mM
N,N-Dimethylformamide
-
N-(1-Oxododecyl)-4alpha,10-dimethyl-8-aza-trans-decal-3beta-ol
-
potent, competitive
N-(2-methylenebenzophenonyl)pyridinium
-
IC50: 0.059 mM
N-(3-methylenebenzophenonyl)pyridinium bromide
-
IC50: 0.016 mM
N-(4-methylenebenzophenonyl)pyridinium bromide
-
IC50: 0.00079 mM
N-(Ethoxycarbonyl)-2-ethoxy-1,2-dihydroquinoline
-
slight
N-[(1,5,9)-Trimethyl-decyl]-4alpha,10-dimethyl-8-aza-decal-3beta-ol
-
strong
N-[2-(4-(3-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
-
inactive at 200 nM
N-[2-(4-(4-((pyrrolidin-1-yl)methyl)phenyl)phenyl)ethyl]-4-chlorobenzenesulfonamide
-
-
N-[2-(4-(4-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
-
-
N-[3-(1,1'-biphenyl-4-yloxy)propyl]-N,N-dimethylamine
-
IC50: 2500 nM
NaCl
-
at high concentrations
Ro 48-8071
RO0717625
-
-
-
Ro48-8071
S23515
-
Squalene maleimide
-
Sulfur-substituted squalene oxide analogues
-
trans-N-(4-(5-[ethyl-(2-hydroxy-ethyl)-amino]-pentyl)-cyclohexyl)-N-methyl-4-trifluoromethyl-benzenesulfonamide fumarate
-
RO0714565
-
Trimethyl-(4,8,13,17,21-pentamethyl-docosa-4,8,12,16,20-pentaenyl)-ammonium
U18666A
ZD-9720
-
-
[19-(3,3-Dimethyl-oxiranyl)-4,8,13,17-tetramethyl-nonadeca-4,8,12,16-tetraenyl]-dimethyl-amine
-
0.01 mM, 8% inhibition
[4'-(6-allyl-methyl-amino-hexyloxy)-2'-fluoro-phenyl]-(4-bromo-phenyl)-methanone fumarate
[4'-(6-allyl-methyl-amino-hexyloxy)-2'-fluoro-phenyl]-(4-bromophenyl)-methanone fumarate
-
Ro 48-8071
[4-(1-azabicyclo[2.2.2]oct-3-yloxy)phenyl](4-chlorophenyl)methanone
[4-(4-Bromo-benzenesulfonyl)-piperazin-1-yl]-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone
[4-[6-(allylmethylamino)hexyloxy]-2-hydroxyphenyl](4-bromophenyl)methanone
-
IC50: 6.3 nM
[4-[6-(allylmethylamino)hexyloxy]-2-methoxyphenyl](4-bromophenyl)methanone
-
IC50: 4.6 nM
[4-[6-(allylmethylamino)hexyloxy]-2-methylaminophenyl](4-bromophenyl)methanone
-
IC50: 4.1 nM
[4-[6-(allylmethylamino)hexyloxy]-2-methylsulfanylphenyl](4-bromophenyl)methanone
-
IC50: 6.2 nM
[4-[6-(allylmethylamino)hexyloxy]phenyl](4-bromophenol)methanone
-
IC50: 5.4 nM
[4-[6-(allylmethylamino)hexyloxy]phenyl](4-nitrophenyl)methanone
-
IC50: 1.9 nM
[4-[6-(allylmethylamino)hexyloxy]phenyl]-(4-fluorophenyl)methanone
-
IC50: 6.7 nM
[4-[6-(allylmethylamino)hexyloxy]phenyl]phenylmethanone
-
IC50: 22.5 nM
[5-(4-(4-chloro-benzoyl)-3-fluoro-phenoxy)-pentyl]-methyl-propyl-ammonium fumarate
-
IC50: 49 nM
[6-[6-(allylmethylamino)hexyloxy]pyridin-3-yl](4-bromophenyl)methanone
-
IC50: 8.7 nM
[6-[6-(cyclopropylmethylamino)hexyloxy]phenyl](4-bromophenyl)methanone
-
IC50: 35.3 nM
{4-[4-(4,5-Dihydro-oxazol-2-yl)-benzylidene]-piperidin-1-yl}-(4-trifluoromethyl-phenyl)-methanone
-
IC50: 90 nM, complete inhibition at 0.001 nM
{4-[6-(allyl-methyl-amino)-hexyloxy]-2-fluoro-phenyl}-(4-chloro-phenyl)-methanone
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
deoxycholate
-
the effective concentration range for enzyme activation is extremely narrow, around 0.1%. The enzyme activity may depend not only on the final concentration of sodium deoxycholate but also on its ratio to protein
Erg27p
-
required for activity of Erg7p
-
jasmonate
-
LAS1 gene expression is induced by the application of jasmonate
Rat liver cytosol carrier protein
-
enhances lanosterol synthase activity in placental microsomes
S105 protein from rat liver
-
required for optimal activity. The S105 protein acts internally within the microsomal membrane system facilitating the access of substrate to specific enzyme sites
-
steroid-3-ketoreductase
-
-
-
Triton X-100
additional information
-
no protective action of steroid-3-ketoreductase towards OSC is necessary
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.075
(3S)-2,3-epoxy-2,3-dihydrosqualene
-
pH 7.4, 37C, liver microsomes
0.011
(3S)-2,3-oxidosqualene
-
-
0.055
(3S)-squalene epoxide
-
-
0.015 - 0.035
2,3-epoxysqualene
0.231
3-[(3E,7E,15E)-16-ethyl-3,7,12,20-tetramethylhenicosa-3,7,11,15,19-pentaen-1-yl]-2,2-dimethyloxirane
-
pH 7.4, 37C, liver microsomes
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000013
27-norsqualene
-
pH 7.4, 37C, liver microsomes
0.00002
28-noroxidosqualene
-
pH 7.4, 37C, liver microsomes
0.000015
29-norsqualene
-
pH 7.4, 37C, liver microsomes
0.00112 - 0.00342
7-(4'-allylmethylamino-but-2-ynyloxy)chromen-2-one
-
0.07876 - 0.1028
7-(morpholinyl-N-hexyloxy)chromen-2-one
-
0.00535 - 0.1024
7-(morpholinyl-N-octanyloxy)chromen-2-one
-
0.00248 - 0.03154
7-(piperidinyl-N-hexyloxy)chromen-2-one
-
0.00018 - 0.00414
7-[10-(allylmethylamino)-decyloxy]chromen-2-one
-
0.00185 - 0.07266
7-[4'-(N-diethylamino)-but-2-ynyloxy]chromen-2-one
-
0.00052 - 0.1063
7-[4'-(N-pyrrolidyn)-but-2-ynyloxy]chromen-2-one
-
0.00015 - 0.00406
7-[6-(allylmethylamino)-hexyloxy]-chromen-2-one
-
0.00104 - 0.02543
7-[8'(dimethylamino-N-octyloxy)]chromen-2-one
-
0.008
S23515
-
-
-
additional information
7-(4'-allylmethylamino-but-2-ynyloxy)chromen-2-one
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0004 - 0.0015
(14-trans)-28-methylidene-2,3:14,15-dioxidoundecanorsqualene
0.0015 - 0.0035
(18E)-29-Methylidene-2,3-oxidohexanorsqualene
0.0035
(18E)-29-methylidene-2,3-oxidosqualene
Sus scrofa
-
IC50: 0.0035 mM
0.03 - 0.05
(18E)-29-methylidene-20,21,22,23,24,30-hexanor-2,3-oxidosqualene
0.015 - 0.02
(18Z)-29-Methylidene-2,3-oxidohexanorsqualene
0.0004 - 0.001
(18Z)-29-methylidene-2,3-oxidosqualene
0.05 - 0.06
(18Z)-29-methylidene-20,21,22,23,24,30-hexanor-2,3-oxidosqualene
0.1
(2-trans)-1-methylidene-2,3-oxido-1'-norsqualene
0.0017 - 0.0074
(2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-yl 3-biphenyl-4-ylpropyl ether
0.00033 - 0.0011
(2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-yl 3-phenylpropyl ether
0.00036 - 0.0027
(2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-yl hexyl ether
0.0015 - 0.0025
(3-trans-7E,11E,15E)-3,4:19,20-diepoxy-7,12,16,20-tetramethyl-1,7,11,15-henicosatetraene
0.012 - 0.025
(3R,4S,7E)-15,16-epoxy-3-ethylthio-8,12,16-trimethyl-1,7,11-heptadecatrien-4-ol
0.0075 - 0.04
(3R,4S,7E,11E)-15,16-epoxy-8,12,16-trimethyl-3-phenylthio-1,7,11-heptadecatrien-4-ol
0.001 - 0.0025
(3R,4S,7E,11E,15E)-19,20-epoxy-3-ethylthio-7,12,16,20-tetramethyl-1,7,11,15-henicosatetraen-4-ol
0.000143 - 0.000326
(4-Benzenesulfonyl-piperazin-1-yl)-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone
0.0000318
(4-bromophenyl)[4-[6-(cyclopropylmethylmethylamino)hexyloxy]phenyl]methanone
Homo sapiens
-
IC50: 31.8 nM
0.0000157
(4-bromophenyl)[4-[6-[(3-hydroxypropyl)methylamino]-hexyloxy]phenyl]methanone
Homo sapiens
-
IC50: 15.7 nM
0.0015 - 0.005
(5E,9E)-13,14-epoxy-6,10,14-trimethyl-1-methylthio-1,5,9-pentadecatriene
0.00005 - 0.001
(5E,9E,13E)-17,18-epoxy-5,10,14,18-tetramethyl-1-methylthio-1,5,9,13-nonadecatetraene
0.06
(5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-(trimethylsilylethynyl)tricosa-2,5,9,13,17-pentaene
Sus scrofa
-
+ (5Z,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-(trimethylsilylethynyl)tricosa-2,5,9,13,17-pentaene, IC50: 0.06 mM
0.018 - 0.032
(5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-vinyl-2,5,9,13,17-tricosapentaene
0.02 - 0.05
(5E,9E,13E,17E)-21,22-epoxy-5-ethynyl-2,9,14,18,22-pentamethyltricosa-2,5,9,13,17-pentaene
0.06
(5Z,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-(trimethylsilylethynyl)tricosa-2,5,9,13,17-pentaene
Sus scrofa
-
+ (5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-(trimethylsilylethynyl)tricosa-2,5,9,13,17-pentaene, IC50: 0.06 mM
0.02 - 0.05
(5Z,9E,13E,17E)-21,22-epoxy-5-ethynyl-2,9,14,18,22-pentamethyltricosa-2,5,9,13,17-pentaene
0.003 - 0.005
(6E)-10-Aza-10,11-dihydrosqualene-2,3-epoxide
0.004 - 0.005
(6E,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene
0.03
(6E,10E,14E,18E)-22,23-epoxy-6-ethynyl-2,10,15,19,23-pentamethyltetracosa-2,6,10,14,18-pentaene
0.02 - 0.1
(6Z)-10-Aza-10,11-dihydrosqualene-2,3-epoxide
0.0022 - 0.012
(6Z,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-(2-methylthiovinyl)-2,6,10,14,18-tetracosapentaene
0.0004 - 0.001
(6Z,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene
0.03
(6Z,10E,14E,18E)-22,23-epoxy-6-ethynyl-2,10,15,19,23-pentamethyltetracosa-2,6,10,14,18-pentaene
0.000083 - 0.000124
(Z)-3-[4-(4-bromobenzoyl)phenacylidene]quinuclidine
0.000112 - 0.000398
1-(2-methyl-4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
0.000082
1-(4-iodophenylsulfonyl)-4-(1-(4-pyridyl)piperidon-4-ylcarbonyl)piperazine
Rattus norvegicus
-
IC50: 82 nM
0.000037 - 0.000116
1-(4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
0.00002
1-[4-(trifluoromethoxy)phenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmeth yl]-piperazine
Homo sapiens
-
-
0.000316
1-[4-chlorobenzyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.0002
1-[4-chlorophenylcarbonyl]-4-[4-(1-methyl-pyrazol-4-yl)phenylmethyl]-piperazine
0.00004
1-[4-chlorophenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.000032
1-[4-chlorophenylcarbonyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.0002
1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-1-yl)phenylmethyl]-piperazine
0.000003
1-[4-chlorophenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.0005
1-[4-chlorophenylsulfonyl]-4-[3-(pyridin-4-yl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.000006
1-[4-chlorophenylsulfonyl]-4-[4-(4-methylpiperazin-1-yl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.000032
1-[4-chlorophenylsulfonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.000013
1-[4-chlorophenylsulfonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.002511
1-[4-methoxyphenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.0002
1-[4-trifluoroacetyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
Homo sapiens
-
-
0.1
18,19-dihydro-29-methylidene-2,3-oxidosqualene
Sus scrofa
-
IC50: 0.1 mM
0.015 - 0.07
18-heptanor-2,3-oxidosqualene
0.0015 - 0.035
19-aza-18,19,22,23-tetrahydrosqualene-2,3-epoxide
0.15 - 10
2-Aza-2,3-dihydrosqualene
3.3 - 16
2-Aza-2,3-dihydrosqualene N-oxide
0.0025 - 0.006
2-[(4E,8E)-12,13-epoxy-5,9,13-trimethyl-4,8-tetradecadienylidene]-1,3-dithiane
0.0035 - 0.012
2-[(4E,8E,12E)-16,17-epoxy-4,9,13,17-tetramethyl-4,8,12-octadecatrienylidene]-1,3-benzodithiole
0.00017 - 0.00035
2-[(4E,8E,12E)-16,17-epoxy-4,9,13,17-tetramethyl-4,8,12-octadecatrienylidene]-1,3-dithiane
0.035 - 0.1
2-[(4E,8E,12E,16E)-20,21-epoxy-4,8,13,17,21-pentamethyl-4,8,12,16-docosatetraenylidene]-1,3-dithiane
0.18
27-norsqualene
Sus scrofa
-
pH 7.4, 37C, liver microsomes
0.076
29-norsqualene
Sus scrofa
-
pH 7.4, 37C, liver microsomes
0.0015 - 0.0035
3-(3,7-Dimethyl-octadeca-3,7,11,15-tetraenyl)-2,2-dimethyl-oxirane
0.00028 - 0.016
3-(biphenyl-4-yloxy)-N,N-dimethylpropan-1-amine
0.00016
3-[(4-chlorobenzoyl)-4-phenoxy]quinuclidine
Rattus norvegicus
-
IC50: 160 nM
0.0000041
allyl-6-[4-(4-bromophenyl)-1H-benzo[d][1,2]oxazin-7-yloxy]hexylmethylamine
Homo sapiens
-
IC50: 4.1 nM
0.0000079
allyl[6-[1-(4-bromophenyl)-3,4-dihydroisoquinolin-6-yloxy]hexyl]methylamine
Homo sapiens
-
IC50: 7.9 nM
0.0000035
allyl[6-[1-(4-bromophenyl)isoquinolin-6-yloxy]hexyl]methylamine
Homo sapiens
-
IC50: 3.5 nM
0.0000196
allyl[6-[3-(4-bromophenyl)-1-methyl-1H-indazol-6-yloxy]hexyl]methylamine
Homo sapiens
-
IC50: 19.6 nM
0.0000056
allyl[6-[3-(4-bromophenyl)benzo[b]thiophen-6-yloxy]hexyl]methylamine
Homo sapiens
-
IC50: 5.6 nM
0.0000029
allyl[6-[3-(4-bromophenyl)benzo[d]isothiazol-6-yloxy]hexyl]methylamine
Homo sapiens
-
IC50: 2.9 nM
0.0000114
allyl[6-[4-(4-bromophenyl)-2H-chromen-7-yloxy]hexyl]methylamine
Homo sapiens
-
IC50: 11.4 nM
0.0000123
allyl[6-[4-(4-bromophenyl)quinazolin-7-yloxy]hexyl]methylamine
Homo sapiens
-
IC50: 12.3 nM
0.0000078
allyl[6-[4-(6-bromo-1,1-dioxobenzo[d]isothiazol-3-yl)phenoxy]hexyl]methylamine
Homo sapiens
-
IC50: 7.8 nM
0.055
azasqualene alcohol N-oxide
0.00000585
BIBB 515
Homo sapiens
-
-
-
1.5 - 14
diethyl-(4,8,13,17,21-pentamethyl-docosa-4,8,12,16,20-pentaenyl)-aminoxide
3.2 - 12.5
Diethyl-(4,8,13,17,21-pentamethyl-docosa-4,8,12,16,20-pentaenyl)-ammonium
0.005
N,N-dimethyl-N-(4-methylenebenzophenonyl)amine
Bos taurus
-
IC50: 0.005 mM
0.059
N-(2-methylenebenzophenonyl)pyridinium
Bos taurus
-
IC50: 0.059 mM
0.016
N-(3-methylenebenzophenonyl)pyridinium bromide
Bos taurus
-
IC50: 0.016 mM
0.00079
N-(4-methylenebenzophenonyl)pyridinium bromide
Bos taurus
-
IC50: 0.00079 mM
0.0002
N-[2-(4-(3-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
Homo sapiens
-
-
0.000063
N-[2-(4-(4-((pyrrolidin-1-yl)methyl)phenyl)phenyl)ethyl]-4-chlorobenzenesulfonamide
Homo sapiens
-
-
0.000028
N-[2-(4-(4-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
Homo sapiens
-
-
0.0025
N-[3-(1,1'-biphenyl-4-yloxy)propyl]-N,N-dimethylamine
Rattus norvegicus
-
IC50: 2500 nM
0.0000065 - 0.000008
Ro 48-8071
0.000022
Ro48-8071
Bos taurus
-
IC50: 22 nM
5.1 - 13.3
Trimethyl-(4,8,13,17,21-pentamethyl-docosa-4,8,12,16,20-pentaenyl)-ammonium
0.000022 - 0.0004
[4-(1-azabicyclo[2.2.2]oct-3-yloxy)phenyl](4-chlorophenyl)methanone
0.000161 - 0.000228
[4-(4-Bromo-benzenesulfonyl)-piperazin-1-yl]-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone
0.0000063
[4-[6-(allylmethylamino)hexyloxy]-2-hydroxyphenyl](4-bromophenyl)methanone
Homo sapiens
-
IC50: 6.3 nM
0.0000046
[4-[6-(allylmethylamino)hexyloxy]-2-methoxyphenyl](4-bromophenyl)methanone
Homo sapiens
-
IC50: 4.6 nM
0.0000041
[4-[6-(allylmethylamino)hexyloxy]-2-methylaminophenyl](4-bromophenyl)methanone
Homo sapiens
-
IC50: 4.1 nM
0.0000062
[4-[6-(allylmethylamino)hexyloxy]-2-methylsulfanylphenyl](4-bromophenyl)methanone
Homo sapiens
-
IC50: 6.2 nM
0.0000054
[4-[6-(allylmethylamino)hexyloxy]phenyl](4-bromophenol)methanone
Homo sapiens
-
IC50: 5.4 nM
0.0000019
[4-[6-(allylmethylamino)hexyloxy]phenyl](4-nitrophenyl)methanone
Homo sapiens
-
IC50: 1.9 nM
0.0000067
[4-[6-(allylmethylamino)hexyloxy]phenyl]-(4-fluorophenyl)methanone
Homo sapiens
-
IC50: 6.7 nM
0.0000225
[4-[6-(allylmethylamino)hexyloxy]phenyl]phenylmethanone
Homo sapiens
-
IC50: 22.5 nM
0.000049
[5-(4-(4-chloro-benzoyl)-3-fluoro-phenoxy)-pentyl]-methyl-propyl-ammonium fumarate
Rattus norvegicus
-
IC50: 49 nM
0.0000087
[6-[6-(allylmethylamino)hexyloxy]pyridin-3-yl](4-bromophenyl)methanone
Homo sapiens
-
IC50: 8.7 nM
0.0000353
[6-[6-(cyclopropylmethylamino)hexyloxy]phenyl](4-bromophenyl)methanone
Homo sapiens
-
IC50: 35.3 nM
0.00009
{4-[4-(4,5-Dihydro-oxazol-2-yl)-benzylidene]-piperidin-1-yl}-(4-trifluoromethyl-phenyl)-methanone
Rattus norvegicus
-
IC50: 90 nM, complete inhibition at 0.001 nM
0.0000043 - 0.000071
{4-[6-(allyl-methyl-amino)-hexyloxy]-2-fluoro-phenyl}-(4-chloro-phenyl)-methanone
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.0000015
mutant C457/E526A at 25C; mutant C457/E526C at 25C
0.0000025
mutant C457/E526C at 35C
0.0000048
mutant C457/E526A at 35C
0.0000063
mutant C457 at 25C
0.0000087
mutant C457/E526D at 25C
0.0000097
mutant C457/E526Q at 25C
0.0000113
mutant C457/E525C at 25C
0.0000128
mutant C457/E526D at 35C
0.0000172
wild-type, at 25C
0.0000192
mutant C457/E526Q at 35C
0.000021
mutant C457/E525C at 35C
0.0000213
mutant C457 at 35C
0.0000292
wild-type, at 35C
0.0000429
cataractous Shumiya cataract rat
0.000046
normal Shumiya cataract rat
0.0043
-
-
1.747
-
-
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 9
-
pH 6.0: about 20% of maximal activity, pH 7.0: about 90% of maximal activity, pH 9.0: about 50% of maximal activity
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25 - 50
-
optimal activity between 25C and 50C with a maximum at 37C