3.4.21.112: site-1 protease

This is an abbreviated version!
For detailed information about site-1 protease, go to the full flat file.

Word Map on EC 3.4.21.112

3.4.21.112

srebps

proprotein

furin

site-2

atf6

subtilase

lassa

arenaviruses

medicine

cleavage-activating

mbtps1

nonbasic

crimean-congo

mucolipidosis

glcnac-1-phosphotransferase

n-acetylglucosamine-1-phosphotransferase

degradation

Reaction

processes precursors containing basic and hydrophobic/aliphatic residues at P4 and P2, respectively, with a relatively relaxed acceptance of amino acids at P1 and P3 =

Synonyms

convertase site 1 protease, dS1P, hSKI-1, kexin, membrane-bound transcription factor protease, site-1, MEROPS S08.8063, PCSK8, prohormone convertase subtilisin-kexin isoenzyme-1, protease responsible for activating sigmaW, PrsW, S08.063, S1P, site 1 protease, site-1 protease, SK-1, SKI-1, SKI-1/S1P, SREBP site 1 protease, subtilisin kexin isoenzyme-1, subtilisin kexin isozyme 1/site 1 protease, subtilisin kexin isozyme-1, subtilisin kexin isozyme-1(SK-1)/site 1 protease (S1P), subtilisin kexin isozyme-1/site-1 protease, subtilisin kexin-isozyme-1, subtilisin-kexin isoenzyme-1, subtilisin-kexin-isozyme, subtilisin/kexin isozyme 1, YPDC

ECTree

3 Hydrolases

3.4 Acting on peptide bonds (peptidases)

3.4.21 Serine endopeptidases

3.4.21.112 site-1 protease

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Results	in table
4	Activating Compound
37	AA Sequence
15	Application
1	CAS Registry Number
19	Cloned(Commentary)
126	Disease/ Diagnostics
17	General Information
26	IC50 Value
70	Inhibitors
11	Ki Value [mM]
37	KM Value [mM]
26	Localization
8	Metals/Ions
9	Molecular Weight [Da]
22	Natural Substrates/ Products (Substrates)
61	Organism
4	pH Optimum
11	Posttranslational Modification
39	Protein Variants
4	Purification (Commentary)
1	Reaction
18	Reaction Type
53	Reference
55	Source Tissue
3	Specific Activity [micromol/min/mg]
1	Storage Stability
82	Substrates and Products (Substrate)
1	Subunits
81	Synonyms
1	Temperature Optimum [°C]
3	Turnover Number [1/s]

IC50 Value

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IC50 Value on EC 3.4.21.112 - site-1 protease

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0.000175 - 0.0005

(R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide

2 entries

0.000393 - 0.000971

(S)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide

2 entries

0.00016

1-(4-[[2-(2-methoxyphenyl)ethyl](pyrrolidin-3-yl)carbamoyl]benzyl)piperidine-3-carboxamide

Homo sapiens

685579

0.000095

4-(2-azabicyclo[2.2.1]hept-2-ylmethyl)-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.000029

4-(6-azabicyclo[3.2.1]oct-6-ylmethyl)-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00059

4-(benzyloxy)-N-[2-(2-chlorophenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00031

4-(benzyloxy)-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00051

4-(benzyloxy)-N-[2-(3-chlorophenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.0001

4-([[(1S 2S)-2-hydroxycyclohexyl]amino]methyl)-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.016

4-[(diethylamino)methyl]-N-[2-(2-ethoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00054

4-[(diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00017

4-[(diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-[(3R)-pyrrolidin-3-yl]benzamide

Homo sapiens

685579

0.0016

4-[(diethylamino)methyl]-N-[2-(2-methylphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00014

4-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.005

N-(2-chlorobenzyl)-4-(1-methylethoxy)-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00043

N-[2-(2 6-dichlorophenyl)ethyl]-4-[(diethylamino)methyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.0014

N-[2-(2-chlorophenyl)ethyl]-4-(1-methylethoxy)-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00084

N-[2-(2-chlorophenyl)ethyl]-4-[(diethylamino)methyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.000008

N-[2-(2-chlorophenyl)ethyl]-4-[[3-(2-methylphenyl)piperidin-1-yl]methyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

most potent inhibitor

685579

0.009

N-[2-(2-fluorophenyl)ethyl]-4-(1-methylethoxy)-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.00025

N-[2-(2-methoxyphenyl)ethyl]-4-(piperidin-1-ylmethyl)-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.000037

N-[2-(2-methoxyphenyl)ethyl]-4-[[3-(2-methylphenyl)piperidin-1-yl]methyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.0096

N-[2-(3-chlorophenyl)ethyl]-4-(1-methylethoxy)-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579

0.0037

N-[2-(4-chlorophenyl)ethyl]-4-[(diethylamino)methyl]-N-pyrrolidin-3-ylbenzamide

Homo sapiens

685579