General Information of the Protein
Protein ID
PT04895
Protein Name
Protein-serine O-palmitoleoyltransferase porcupine
Secondarily
Protein Name
Protein MG61
Gene Name
PORCN
Secondarily
Gene Name
MG61
PORC
PPN
Sequence
MATFSRQEFFQQLLQGCLLPTAQQGLDQIWLLLAICLACRLLWRLGLPSYLKHASTVAGGFFSLYHFFQLHMVWVVLLSLLCYLVLFLCRHSSHRGVFLSVTILIYLLMGEMHMVDTVTWHKMRGAQMIVAMKAVSLGFDLDRGEVGTVPSPVEFMGYLYFVGTIVFGPWISFHSYLQAVQGRPLSCRWLQKVARSLALALLCLVLSTCVGPYLFPYFIPLNGDRLLRNKKRKARGTMVRWLRAYESAVSFHFSNYFVGFLSEATATLAGAGFTEEKDHLEWDLTVSKPLNVELPRSMVEVVTSWNLPMSYWLNNYVFKNALRLGTFSAVLVTYAASALLHGFSFHLAAVLLSLAFITYVEHVLRKRLARILSACVLSKRCPPDCSHQHRLGLGVRALNLLFGALAIFHLAYLGSLFDVDVDDTTEEQGYGMAYTVHKWSELSWASHWVTFGCWIFYRLIG
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Protein-serine O-palmitoleoyltransferase that acts as a key regulator of the Wnt signaling pathway by mediating the attachment of palmitoleate, a 16-carbon monounsaturated fatty acid (C16:1(9Z)), to Wnt proteins. Serine palmitoleoylation of WNT proteins is required for efficient binding to frizzled receptors.
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Uniprot ID
Primary ID:
Q9H237

Secondarily ID:
B2RBN8
B7ZAR3
Q14829
Q9H234
Q9H235
Q9H236
Q9UJU7
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Ensembl ID
ENSG00000102312
HGNC ID
HGNC:17652
Subcellular Location
Endoplasmic reticulum membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0548637
 Compound Info 
2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(4-thiophen-3-ylphenyl)acetamide
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C19H17N5O3S
  1
1
IC50 = 0.4 nM
 Bioactivity Info 
   TI
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CP0535260
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(5-phenylpyridin-2-yl)acetamide
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C21H20N4O3
  1
1
IC50 = 1 nM
 Bioactivity Info 
   TI
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CP0548638
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(6-phenylpyridazin-3-yl)acetamide
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C20H19N5O3
  1
1
IC50 = 1 nM
 Bioactivity Info 
   TI
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CP0566160
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(6-phenylpyridin-3-yl)acetamide
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C21H20N4O3
  1
1
IC50 = 6 nM
 Bioactivity Info 
   TI
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CP0558811
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(4-pyridin-3-ylphenyl)acetamide
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C21H20N4O3
  1
1
IC50 = 8 nM
 Bioactivity Info 
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CP0236560
 Compound Info 
N-[6-(5-fluoropyridin-3-yl)pyridazin-3-yl]-2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)acetamide
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C19H17FN6O3
  1
1
IC50 = 9 nM
 Bioactivity Info 
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CP0413127
 Compound Info 
2-(6-cyclopropyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-[6-(5-fluoropyridin-3-yl)pyridazin-3-yl]acetamide
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C21H19FN6O3
  1
1
IC50 = 11 nM
 Bioactivity Info 
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CP0564767
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(6-pyridin-3-ylpyridin-3-yl)acetamide
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C20H19N5O3
  1
1
IC50 = 11 nM
 Bioactivity Info 
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CP0119167
 Compound Info 
2-(6-cyclopropyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(6-pyridin-3-ylpyridazin-3-yl)acetamide
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C21H20N6O3
  1
1
IC50 = 12 nM
 Bioactivity Info 
   TI
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CP0161514
 Compound Info 
2-(6-cyclopropyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-[6-(6-methylpyridin-3-yl)pyridazin-3-yl]acetamide
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C22H22N6O3
  1
1
IC50 = 12 nM
 Bioactivity Info 
   TI
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CP0489081
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(4-phenylphenyl)acetamide
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C22H21N3O3
  1
1
IC50 = 12 nM
 Bioactivity Info 
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CP0358158
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-[4-(1,3-thiazol-2-yl)phenyl]acetamide
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C19H18N4O3S
  1
1
IC50 = 15 nM
 Bioactivity Info 
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CP0564766
 Compound Info 
2-(2-methyl-1,3-dioxoisoindol-4-yl)-N-[4-(1,3-thiazol-2-yl)phenyl]acetamide
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C20H15N3O3S
  1
1
IC50 = 15 nM
 Bioactivity Info 
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CP0566158
 Compound Info 
2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-[4-(1,3-thiazol-2-yl)phenyl]acetamide
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C18H16N6O3S
  1
1
IC50 = 24 nM
 Bioactivity Info 
   TI
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CP0099227
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(6-pyridin-3-ylpyridazin-3-yl)acetamide
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C19H18N6O3
  1
1
IC50 = 29 nM
 Bioactivity Info 
   TI
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CP0236561
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-[6-(6-methylpyridin-3-yl)pyridazin-3-yl]acetamide
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C20H20N6O3
  1
1
IC50 = 29 nM
 Bioactivity Info 
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CP0429544
 Compound Info 
2,4-dimethyl-1,3-dioxo-N-[4-(1,3-thiazol-2-yl)phenyl]-7,8-dihydro-6H-purino[7,8-a]pyrrole-8-carboxamide
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C20H18N6O3S
  1
1
IC50 = 42 nM
 Bioactivity Info 
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CP0566159
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(4-pyridin-2-ylphenyl)acetamide
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C21H20N4O3
  1
1
IC50 = 67 nM
 Bioactivity Info 
   TI
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CP0539079
 Compound Info 
2-(6-methyl-5,7-dioxo-3,4-dihydro-2H-pyrrolo[3,4-b]pyridin-1-yl)-N-(4-pyridin-4-ylphenyl)acetamide
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C21H20N4O3
  1
1
IC50 = 72 nM
 Bioactivity Info 
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Cell Line ID: CL000575 , L Wnt-3A
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0153409
 Compound Info 
2-[5-methyl-6-(6-methylpyridin-3-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide
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C23H20N6O
  1
1 IC50 = 0.38 nM
CP0414749
 Compound Info 
CHEBI:78030
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C23H20N6O
  1
1 IC50 = 0.4 nM
CP0420216
 Compound Info 
2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide
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C19H17N7O3
  1
1 IC50 = 2.9 nM
Clinical Information about the Protein
Target 1 ( Protein-serine O-palmitoleoyltransferase porcupine (PORCN) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 ETC-1922159
 Drug Info 
Phase 1
Solid tumour/cancer
2 LGK974
 Drug Info 
Phase 1
Solid tumour/cancer
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT04787 Protein-serine O-palmitoleoyltransferase porcupine Mus musculus, Mouse
 Protein Info