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Found 255 hits Enz. Inhib. hit(s) with Target = 'Protein-serine O-palmitoleoyltransferase porcupine'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50133864
PNG
(CHEMBL2139947 | US10251893, Compound 59)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cc2)-c2cccnc2)cc1
Show InChI InChI=1S/C25H21N3O/c1-18-15-22(12-14-27-18)20-6-4-19(5-7-20)16-25(29)28-24-10-8-21(9-11-24)23-3-2-13-26-17-23/h2-15,17H,16H2,1H3,(H,28,29)
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n/an/a 0.0740n/an/an/an/an/an/a



Experimental Therapeutics Centre

Curated by ChEMBL


Assay Description
Inhibition of porcupine activity (unknown origin) expressed in human HT1080 cells assessed as suppression of Wnt3A-mediated super top flash activity ...


Bioorg Med Chem Lett 25: 5472-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.10.032
BindingDB Entry DOI: 10.7270/Q21838C2
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374968
PNG
(US10251893, Cpd 166)
Show SMILES COC(=O)N1CCN(CC1)c1ccc(NC(=O)Cc2cnc(c(C)c2)-c2ccnc(C)c2)nc1
Show InChI InChI=1S/C25H28N6O3/c1-17-12-19(15-28-24(17)20-6-7-26-18(2)13-20)14-23(32)29-22-5-4-21(16-27-22)30-8-10-31(11-9-30)25(33)34-3/h4-7,12-13,15-16H,8-11,14H2,1-3H3,(H,27,29,32)
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n/an/a 0.100n/an/an/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374968
PNG
(US10251893, Cpd 166)
Show SMILES COC(=O)N1CCN(CC1)c1ccc(NC(=O)Cc2cnc(c(C)c2)-c2ccnc(C)c2)nc1
Show InChI InChI=1S/C25H28N6O3/c1-17-12-19(15-28-24(17)20-6-7-26-18(2)13-20)14-23(32)29-22-5-4-21(16-27-22)30-8-10-31(11-9-30)25(33)34-3/h4-7,12-13,15-16H,8-11,14H2,1-3H3,(H,27,29,32)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50125819
PNG
(CHEMBL3623895)
Show SMILES CC(Oc1ccc(cc1)-c1ccnc(C)c1)C(=O)Nc1ccc(cn1)-c1cnccn1
Show InChI InChI=1S/C24H21N5O2/c1-16-13-19(9-10-26-16)18-3-6-21(7-4-18)31-17(2)24(30)29-23-8-5-20(14-28-23)22-15-25-11-12-27-22/h3-15,17H,1-2H3,(H,28,29,30)
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n/an/a 0.110n/an/an/an/an/an/a



Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in mouse L Wnt3A cells co-cultured with TM3 cells harboring luciferase reporter gene assessed as r...


Bioorg Med Chem 23: 6855-68 (2015)


Article DOI: 10.1016/j.bmc.2015.09.048
BindingDB Entry DOI: 10.7270/Q2J10500
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50125820
PNG
(CHEMBL3623894)
Show SMILES Cc1cc(ccn1)-c1ccc(CCC(=O)Nc2ccc(cn2)-c2cnccn2)cc1
Show InChI InChI=1S/C24H21N5O/c1-17-14-20(10-11-26-17)19-5-2-18(3-6-19)4-9-24(30)29-23-8-7-21(15-28-23)22-16-25-12-13-27-22/h2-3,5-8,10-16H,4,9H2,1H3,(H,28,29,30)
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Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in mouse L Wnt3A cells co-cultured with TM3 cells harboring luciferase reporter gene assessed as r...


Bioorg Med Chem 23: 6855-68 (2015)


Article DOI: 10.1016/j.bmc.2015.09.048
BindingDB Entry DOI: 10.7270/Q2J10500
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374846
PNG
(US10251893, Cpd 50)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cc2)-c2ccccc2)cc1
Show InChI InChI=1S/C26H22N2O/c1-19-17-24(15-16-27-19)23-9-7-20(8-10-23)18-26(29)28-25-13-11-22(12-14-25)21-5-3-2-4-6-21/h2-17H,18H2,1H3,(H,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374847
PNG
(US10251893, Cpd 51)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cn2)-c2ccccc2)cn1
Show InChI InChI=1S/C24H20N4O/c1-17-13-20(11-12-25-17)22-9-7-18(15-26-22)14-24(29)28-23-10-8-21(16-27-23)19-5-3-2-4-6-19/h2-13,15-16H,14H2,1H3,(H,27,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374847
PNG
(US10251893, Cpd 51)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cn2)-c2ccccc2)cn1
Show InChI InChI=1S/C24H20N4O/c1-17-13-20(11-12-25-17)22-9-7-18(15-26-22)14-24(29)28-23-10-8-21(16-27-23)19-5-3-2-4-6-19/h2-13,15-16H,14H2,1H3,(H,27,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM375004
PNG
(2-(2'-fluoro-3-methyl-2,4'-bipyridin-5-yl)-N-(5-(p...)
Show SMILES Cc1cc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cnc1-c1ccnc(F)c1
Show InChI InChI=1S/C22H17FN6O/c1-14-8-15(11-28-22(14)16-4-5-26-19(23)10-16)9-21(30)29-20-3-2-17(12-27-20)18-13-24-6-7-25-18/h2-8,10-13H,9H2,1H3,(H,27,29,30)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM375004
PNG
(2-(2'-fluoro-3-methyl-2,4'-bipyridin-5-yl)-N-(5-(p...)
Show SMILES Cc1cc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cnc1-c1ccnc(F)c1
Show InChI InChI=1S/C22H17FN6O/c1-14-8-15(11-28-22(14)16-4-5-26-19(23)10-16)9-21(30)29-20-3-2-17(12-27-20)18-13-24-6-7-25-18/h2-8,10-13H,9H2,1H3,(H,27,29,30)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374846
PNG
(US10251893, Cpd 50)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cc2)-c2ccccc2)cc1
Show InChI InChI=1S/C26H22N2O/c1-19-17-24(15-16-27-19)23-9-7-20(8-10-23)18-26(29)28-25-13-11-22(12-14-25)21-5-3-2-4-6-21/h2-17H,18H2,1H3,(H,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50125941
PNG
(CHEMBL3623875)
Show SMILES Cc1cc(ccn1)-c1ccc(OC(=O)Nc2ccc(cn2)-c2cnccn2)cc1
Show InChI InChI=1S/C22H17N5O2/c1-15-12-17(8-9-24-15)16-2-5-19(6-3-16)29-22(28)27-21-7-4-18(13-26-21)20-14-23-10-11-25-20/h2-14H,1H3,(H,26,27,28)
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n/an/a 0.230n/an/an/an/an/an/a



Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in mouse L Wnt3A cells co-cultured with TM3 cells harboring luciferase reporter gene assessed as r...


Bioorg Med Chem 23: 6855-68 (2015)


Article DOI: 10.1016/j.bmc.2015.09.048
BindingDB Entry DOI: 10.7270/Q2J10500
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50125818
PNG
(CHEMBL3623896)
Show SMILES Cc1ccc(cn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
Show InChI InChI=1S/C23H20N6O/c1-15-9-17(11-28-23(15)19-4-3-16(2)26-13-19)10-22(30)29-21-6-5-18(12-27-21)20-14-24-7-8-25-20/h3-9,11-14H,10H2,1-2H3,(H,27,29,30)
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Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin)


Bioorg Med Chem 23: 6855-68 (2015)


Article DOI: 10.1016/j.bmc.2015.09.048
BindingDB Entry DOI: 10.7270/Q2J10500
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374920
PNG
(US10251893, Cpd 128)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cn1
Show InChI InChI=1S/C22H18N6O/c1-15-10-17(6-7-24-15)19-4-2-16(12-26-19)11-22(29)28-21-5-3-18(13-27-21)20-14-23-8-9-25-20/h2-10,12-14H,11H2,1H3,(H,27,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM50133870
PNG
(CHEBI:78030 | CHEMBL3188386 | US10251893, Compound...)
Show SMILES Cc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
Show InChI InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374916
PNG
(N-(2,3'-bipyridin-6'-yl)-2-(2',3-dimethyl-2,4'-bip...)
Show SMILES Cc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2ccccn2)cc1C
Show InChI InChI=1S/C24H21N5O/c1-16-11-18(14-28-24(16)19-8-10-25-17(2)12-19)13-23(30)29-22-7-6-20(15-27-22)21-5-3-4-9-26-21/h3-12,14-15H,13H2,1-2H3,(H,27,29,30)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50133870
PNG
(CHEBI:78030 | CHEMBL3188386 | US10251893, Compound...)
Show SMILES Cc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
Show InChI InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
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Experimental Therapeutics Centre , 31 Biopolis Way, No. 03-01 Nanos, 138669, Singapore.

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin)


J Med Chem 60: 6678-6692 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00662
BindingDB Entry DOI: 10.7270/Q2571FF5
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50257135
PNG
(CHEMBL4080208)
Show SMILES Cn1c2ncn(CC(=O)Nc3ccc(cc3)-c3ccsc3)c2c(=O)n(C)c1=O
Show InChI InChI=1S/C19H17N5O3S/c1-22-17-16(18(26)23(2)19(22)27)24(11-20-17)9-15(25)21-14-5-3-12(4-6-14)13-7-8-28-10-13/h3-8,10-11H,9H2,1-2H3,(H,21,25)
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Experimental Therapeutics Centre , 31 Biopolis Way, No. 03-01 Nanos, 138669, Singapore.

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in HEK293 cells after day 1 post treatment by Super-top flash reporter gene assay


J Med Chem 60: 6678-6692 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00662
BindingDB Entry DOI: 10.7270/Q2571FF5
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374920
PNG
(US10251893, Cpd 128)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cn1
Show InChI InChI=1S/C22H18N6O/c1-15-10-17(6-7-24-15)19-4-2-16(12-26-19)11-22(29)28-21-5-3-18(13-27-21)20-14-23-8-9-25-20/h2-10,12-14H,11H2,1H3,(H,27,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50133870
PNG
(CHEBI:78030 | CHEMBL3188386 | US10251893, Compound...)
Show SMILES Cc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
Show InChI InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
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Experimental Therapeutics Centre

Curated by ChEMBL


Assay Description
Inhibition of porcupine activity (unknown origin) expressed in human HT1080 cells assessed as suppression of Wnt3A-mediated super top flash activity ...


Bioorg Med Chem Lett 25: 5472-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.10.032
BindingDB Entry DOI: 10.7270/Q21838C2
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM50133870
PNG
(CHEBI:78030 | CHEMBL3188386 | US10251893, Compound...)
Show SMILES Cc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
Show InChI InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374916
PNG
(N-(2,3'-bipyridin-6'-yl)-2-(2',3-dimethyl-2,4'-bip...)
Show SMILES Cc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2ccccn2)cc1C
Show InChI InChI=1S/C24H21N5O/c1-16-11-18(14-28-24(16)19-8-10-25-17(2)12-19)13-23(30)29-22-7-6-20(15-27-22)21-5-3-4-9-26-21/h3-12,14-15H,13H2,1-2H3,(H,27,29,30)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM50197277
PNG
(CHEMBL3972086)
Show SMILES Cc1cc(ccn1)-c1ncc(CNC(=O)c2ccc3c(c2)[nH]c2ccccc32)cc1F
Show InChI InChI=1S/C25H19FN4O/c1-15-10-17(8-9-27-15)24-21(26)11-16(13-28-24)14-29-25(31)18-6-7-20-19-4-2-3-5-22(19)30-23(20)12-18/h2-13,30H,14H2,1H3,(H,29,31)
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Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells after 48 hrs by Super-top flash reporter gene assay


Bioorg Med Chem 24: 5861-5872 (2016)


Article DOI: 10.1016/j.bmc.2016.09.041
BindingDB Entry DOI: 10.7270/Q2HQ41VN
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50133865
PNG
(CHEMBL3633801)
Show SMILES C[C@@H](C(=O)Nc1ccc(cc1)-c1ccsc1)n1cnc2n(C)c(=O)n(C)c(=O)c12 |r|
Show InChI InChI=1S/C20H19N5O3S/c1-12(25-11-21-17-16(25)19(27)24(3)20(28)23(17)2)18(26)22-15-6-4-13(5-7-15)14-8-9-29-10-14/h4-12H,1-3H3,(H,22,26)/t12-/m0/s1
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Experimental Therapeutics Centre

Curated by ChEMBL


Assay Description
Inhibition of porcupine in human HEK293 cells assessed as reduction in Wnt secretion by measuring suppression of beta-catenin reporter activity after...


Bioorg Med Chem Lett 25: 5472-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.10.032
BindingDB Entry DOI: 10.7270/Q21838C2
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374918
PNG
(US10251893, Cpd 126)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cn2)-c2ccccn2)cn1
Show InChI InChI=1S/C23H19N5O/c1-16-12-18(9-11-24-16)21-7-5-17(14-26-21)13-23(29)28-22-8-6-19(15-27-22)20-4-2-3-10-25-20/h2-12,14-15H,13H2,1H3,(H,27,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374918
PNG
(US10251893, Cpd 126)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cn2)-c2ccccn2)cn1
Show InChI InChI=1S/C23H19N5O/c1-16-12-18(9-11-24-16)21-7-5-17(14-26-21)13-23(29)28-22-8-6-19(15-27-22)20-4-2-3-10-25-20/h2-12,14-15H,13H2,1H3,(H,27,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374802
PNG
(US10251893, Cpd 6)
Show SMILES COc1ccc2nc(NC(=O)Cc3ccc(cc3)-c3ccnc(C)c3)sc2c1
Show InChI InChI=1S/C22H19N3O2S/c1-14-11-17(9-10-23-14)16-5-3-15(4-6-16)12-21(26)25-22-24-19-8-7-18(27-2)13-20(19)28-22/h3-11,13H,12H2,1-2H3,(H,24,25,26)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374802
PNG
(US10251893, Cpd 6)
Show SMILES COc1ccc2nc(NC(=O)Cc3ccc(cc3)-c3ccnc(C)c3)sc2c1
Show InChI InChI=1S/C22H19N3O2S/c1-14-11-17(9-10-23-14)16-5-3-15(4-6-16)12-21(26)25-22-24-19-8-7-18(27-2)13-20(19)28-22/h3-11,13H,12H2,1-2H3,(H,24,25,26)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50125824
PNG
(CHEMBL3623893)
Show SMILES Cc1cc(ccn1)-c1ccc(SCC(=O)Nc2ccc(cn2)-c2cnccn2)cc1
Show InChI InChI=1S/C23H19N5OS/c1-16-12-18(8-9-25-16)17-2-5-20(6-3-17)30-15-23(29)28-22-7-4-19(13-27-22)21-14-24-10-11-26-21/h2-14H,15H2,1H3,(H,27,28,29)
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Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in mouse L Wnt3A cells co-cultured with TM3 cells harboring luciferase reporter gene assessed as r...


Bioorg Med Chem 23: 6855-68 (2015)


Article DOI: 10.1016/j.bmc.2015.09.048
BindingDB Entry DOI: 10.7270/Q2J10500
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50125818
PNG
(CHEMBL3623896)
Show SMILES Cc1ccc(cn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
Show InChI InChI=1S/C23H20N6O/c1-15-9-17(11-28-23(15)19-4-3-16(2)26-13-19)10-22(30)29-21-6-5-18(12-27-21)20-14-24-7-8-25-20/h3-9,11-14H,10H2,1-2H3,(H,27,29,30)
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Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in mouse L Wnt3A cells co-cultured with TM3 cells harboring luciferase reporter gene assessed as r...


Bioorg Med Chem 23: 6855-68 (2015)


Article DOI: 10.1016/j.bmc.2015.09.048
BindingDB Entry DOI: 10.7270/Q2J10500
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50125825
PNG
(CHEMBL3623892)
Show SMILES CN(CC(=O)Nc1ccc(cn1)-c1cnccn1)c1ccc(cc1)-c1ccnc(C)c1
Show InChI InChI=1S/C24H22N6O/c1-17-13-19(9-10-26-17)18-3-6-21(7-4-18)30(2)16-24(31)29-23-8-5-20(14-28-23)22-15-25-11-12-27-22/h3-15H,16H2,1-2H3,(H,28,29,31)
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Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in mouse L Wnt3A cells co-cultured with TM3 cells harboring luciferase reporter gene assessed as r...


Bioorg Med Chem 23: 6855-68 (2015)


Article DOI: 10.1016/j.bmc.2015.09.048
BindingDB Entry DOI: 10.7270/Q2J10500
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374948
PNG
(N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2',3...)
Show SMILES CC(=O)N1CCN(CC1)c1ccc(NC(=O)Cc2cnc(c(C)c2)-c2ccnc(C)c2)nc1
Show InChI InChI=1S/C25H28N6O2/c1-17-12-20(15-28-25(17)21-6-7-26-18(2)13-21)14-24(33)29-23-5-4-22(16-27-23)31-10-8-30(9-11-31)19(3)32/h4-7,12-13,15-16H,8-11,14H2,1-3H3,(H,27,29,33)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374822
PNG
(2-(4-(2-methylpyridin-4-yl)phenyl)-N-(5-phenylpyri...)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cn2)-c2ccccc2)cc1
Show InChI InChI=1S/C25H21N3O/c1-18-15-22(13-14-26-18)21-9-7-19(8-10-21)16-25(29)28-24-12-11-23(17-27-24)20-5-3-2-4-6-20/h2-15,17H,16H2,1H3,(H,27,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374948
PNG
(N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2',3...)
Show SMILES CC(=O)N1CCN(CC1)c1ccc(NC(=O)Cc2cnc(c(C)c2)-c2ccnc(C)c2)nc1
Show InChI InChI=1S/C25H28N6O2/c1-17-12-20(15-28-25(17)21-6-7-26-18(2)13-21)14-24(33)29-23-5-4-22(16-27-23)31-10-8-30(9-11-31)19(3)32/h4-7,12-13,15-16H,8-11,14H2,1-3H3,(H,27,29,33)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374822
PNG
(2-(4-(2-methylpyridin-4-yl)phenyl)-N-(5-phenylpyri...)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cn2)-c2ccccc2)cc1
Show InChI InChI=1S/C25H21N3O/c1-18-15-22(13-14-26-18)21-9-7-19(8-10-21)16-25(29)28-24-12-11-23(17-27-24)20-5-3-2-4-6-20/h2-15,17H,16H2,1H3,(H,27,28,29)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM50458259
PNG
(CHEMBL4215992)
Show SMILES Cc1cc(ccn1)-c1ncc(CNC(=O)c2ccc3c(c2)[nH]c2ccccc32)cc1C#N
Show InChI InChI=1S/C26H19N5O/c1-16-10-18(8-9-28-16)25-20(13-27)11-17(14-29-25)15-30-26(32)19-6-7-22-21-4-2-3-5-23(21)31-24(22)12-19/h2-12,14,31H,15H2,1H3,(H,30,32)
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Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells assessed as suppression of Wnt signaling after 48 hrs by Super-top flash...


Eur J Med Chem 149: 110-121 (2018)


Article DOI: 10.1016/j.ejmech.2018.02.034
BindingDB Entry DOI: 10.7270/Q2PR7ZMQ
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374998
PNG
(N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2'-f...)
Show SMILES CC(=O)N1CCN(CC1)c1ccc(NC(=O)Cc2cnc(c(C)c2)-c2ccnc(F)c2)nc1
Show InChI InChI=1S/C24H25FN6O2/c1-16-11-18(14-28-24(16)19-5-6-26-21(25)13-19)12-23(33)29-22-4-3-20(15-27-22)31-9-7-30(8-10-31)17(2)32/h3-6,11,13-15H,7-10,12H2,1-2H3,(H,27,29,33)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374998
PNG
(N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2'-f...)
Show SMILES CC(=O)N1CCN(CC1)c1ccc(NC(=O)Cc2cnc(c(C)c2)-c2ccnc(F)c2)nc1
Show InChI InChI=1S/C24H25FN6O2/c1-16-11-18(14-28-24(16)19-5-6-26-21(25)13-19)12-23(33)29-22-4-3-20(15-27-22)31-9-7-30(8-10-31)17(2)32/h3-6,11,13-15H,7-10,12H2,1-2H3,(H,27,29,33)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM50133870
PNG
(CHEBI:78030 | CHEMBL3188386 | US10251893, Compound...)
Show SMILES Cc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
Show InChI InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
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n/an/a 0.900n/an/an/an/an/an/a



Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells assessed as suppression of Wnt signaling after 48 hrs by Super-top flash...


Eur J Med Chem 149: 110-121 (2018)


Article DOI: 10.1016/j.ejmech.2018.02.034
BindingDB Entry DOI: 10.7270/Q2PR7ZMQ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM50133870
PNG
(CHEBI:78030 | CHEMBL3188386 | US10251893, Compound...)
Show SMILES Cc1cc(ccn1)-c1ncc(CC(=O)Nc2ccc(cn2)-c2cnccn2)cc1C
Show InChI InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
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n/an/a 0.900n/an/an/an/an/an/a



Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells after 48 hrs by Super-top flash reporter gene assay


Bioorg Med Chem 24: 5861-5872 (2016)


Article DOI: 10.1016/j.bmc.2016.09.041
BindingDB Entry DOI: 10.7270/Q2HQ41VN
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50125826
PNG
(CHEMBL3623891)
Show SMILES Cc1cc(ccn1)-c1ccc(NCC(=O)Nc2ccc(cn2)-c2cnccn2)cc1
Show InChI InChI=1S/C23H20N6O/c1-16-12-18(8-9-25-16)17-2-5-20(6-3-17)27-15-23(30)29-22-7-4-19(13-28-22)21-14-24-10-11-26-21/h2-14,27H,15H2,1H3,(H,28,29,30)
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n/an/a 0.960n/an/an/an/an/an/a



Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in mouse L Wnt3A cells co-cultured with TM3 cells harboring luciferase reporter gene assessed as r...


Bioorg Med Chem 23: 6855-68 (2015)


Article DOI: 10.1016/j.bmc.2015.09.048
BindingDB Entry DOI: 10.7270/Q2J10500
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50133864
PNG
(CHEMBL2139947 | US10251893, Compound 59)
Show SMILES Cc1cc(ccn1)-c1ccc(CC(=O)Nc2ccc(cc2)-c2cccnc2)cc1
Show InChI InChI=1S/C25H21N3O/c1-18-15-22(12-14-27-18)20-6-4-19(5-7-20)16-25(29)28-24-10-8-21(9-11-24)23-3-2-13-26-17-23/h2-15,17H,16H2,1H3,(H,28,29)
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Ulm University Hospital

Curated by ChEMBL


Assay Description
Inhibition of porcupine in HEK293T cells transfected with Wnt3A-expressing vector assessed as suppression of Wnt/beta-catenin signaling after 22 hrs ...


J Med Chem 61: 4087-4102 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00095
BindingDB Entry DOI: 10.7270/Q2GX4F5D
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50257160
PNG
(CHEMBL4096728)
Show SMILES CN1C(=O)C2=C(N(CC(=O)Nc3ccc(cn3)-c3ccccc3)CCC2)C1=O |t:4|
Show InChI InChI=1S/C21H20N4O3/c1-24-20(27)16-8-5-11-25(19(16)21(24)28)13-18(26)23-17-10-9-15(12-22-17)14-6-3-2-4-7-14/h2-4,6-7,9-10,12H,5,8,11,13H2,1H3,(H,22,23,26)
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Experimental Therapeutics Centre , 31 Biopolis Way, No. 03-01 Nanos, 138669, Singapore.

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in HEK293 cells after day 1 post treatment by Super-top flash reporter gene assay


J Med Chem 60: 6678-6692 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00662
BindingDB Entry DOI: 10.7270/Q2571FF5
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50257143
PNG
(CHEMBL4080021)
Show SMILES CN1C(=O)C2=C(N(CC(=O)Nc3ccc(nn3)-c3ccccc3)CCC2)C1=O |t:4|
Show InChI InChI=1S/C20H19N5O3/c1-24-19(27)14-8-5-11-25(18(14)20(24)28)12-17(26)21-16-10-9-15(22-23-16)13-6-3-2-4-7-13/h2-4,6-7,9-10H,5,8,11-12H2,1H3,(H,21,23,26)
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Experimental Therapeutics Centre , 31 Biopolis Way, No. 03-01 Nanos, 138669, Singapore.

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in HEK293 cells after day 1 post treatment by Super-top flash reporter gene assay


J Med Chem 60: 6678-6692 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00662
BindingDB Entry DOI: 10.7270/Q2571FF5
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50233629
PNG
(CHEMBL4080842)
Show SMILES C[C@H](Nc1ccc(nc1)-c1ccnn1C)C(=O)Nc1ccc(cn1)-c1ccccc1 |r|
Show InChI InChI=1S/C23H22N6O/c1-16(27-19-9-10-20(24-15-19)21-12-13-26-29(21)2)23(30)28-22-11-8-18(14-25-22)17-6-4-3-5-7-17/h3-16,27H,1-2H3,(H,25,28,30)/t16-/m0/s1
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Experimental Therapeutics Centre

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in HEK293-STF3A cells assessed as inhibition of Wnt signaling by measuring decrease in beta-cateni...


J Med Chem 58: 5889-99 (2015)


Article DOI: 10.1021/acs.jmedchem.5b00507
BindingDB Entry DOI: 10.7270/Q29K4DG1
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50233628
PNG
(CHEMBL4088716)
Show SMILES C[C@H](Nc1ccc(nc1)-c1ccnn1C)C(=O)Nc1ccc(cn1)-c1cccnc1 |r|
Show InChI InChI=1S/C22H21N7O/c1-15(27-18-6-7-19(24-14-18)20-9-11-26-29(20)2)22(30)28-21-8-5-17(13-25-21)16-4-3-10-23-12-16/h3-15,27H,1-2H3,(H,25,28,30)/t15-/m0/s1
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Experimental Therapeutics Centre

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in HEK293-STF3A cells assessed as inhibition of Wnt signaling by measuring decrease in beta-cateni...


J Med Chem 58: 5889-99 (2015)


Article DOI: 10.1021/acs.jmedchem.5b00507
BindingDB Entry DOI: 10.7270/Q29K4DG1
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM50197194
PNG
(CHEMBL3907027)
Show SMILES Cc1cc(ccn1)-c1ccc(CNC(=O)c2ccc(cc2)-c2ccccc2)cc1
Show InChI InChI=1S/C26H22N2O/c1-19-17-25(15-16-27-19)23-9-7-20(8-10-23)18-28-26(29)24-13-11-22(12-14-24)21-5-3-2-4-6-21/h2-17H,18H2,1H3,(H,28,29)
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Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells after 48 hrs by Super-top flash reporter gene assay


Bioorg Med Chem 24: 5861-5872 (2016)


Article DOI: 10.1016/j.bmc.2016.09.041
BindingDB Entry DOI: 10.7270/Q2HQ41VN
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM50458258
PNG
(CHEMBL4215124)
Show SMILES COc1cc(CNC(=O)c2ccc3c(c2)[nH]c2ccccc32)cnc1-c1ccnc(C)c1
Show InChI InChI=1S/C26H22N4O2/c1-16-11-18(9-10-27-16)25-24(32-2)12-17(14-28-25)15-29-26(31)19-7-8-21-20-5-3-4-6-22(20)30-23(21)13-19/h3-14,30H,15H2,1-2H3,(H,29,31)
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n/an/a 1.90n/an/an/an/an/an/a



Soochow University

Curated by ChEMBL


Assay Description
Inhibition of porcupine in mouse L Wnt3A cells co-cultured with HEK293 cells assessed as suppression of Wnt signaling after 48 hrs by Super-top flash...


Eur J Med Chem 149: 110-121 (2018)


Article DOI: 10.1016/j.ejmech.2018.02.034
BindingDB Entry DOI: 10.7270/Q2PR7ZMQ
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Homo sapiens (Human))
BDBM50233636
PNG
(CHEMBL4070649)
Show SMILES Cc1nccn1-c1ccc(OCC(=O)Nc2ccc(cc2)-c2ccccc2)cc1
Show InChI InChI=1S/C24H21N3O2/c1-18-25-15-16-27(18)22-11-13-23(14-12-22)29-17-24(28)26-21-9-7-20(8-10-21)19-5-3-2-4-6-19/h2-16H,17H2,1H3,(H,26,28)
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n/an/a 2n/an/an/an/an/an/a



Experimental Therapeutics Centre

Curated by ChEMBL


Assay Description
Inhibition of porcupine (unknown origin) expressed in HEK293-STF3A cells assessed as inhibition of Wnt signaling by measuring decrease in beta-cateni...


J Med Chem 58: 5889-99 (2015)


Article DOI: 10.1021/acs.jmedchem.5b00507
BindingDB Entry DOI: 10.7270/Q29K4DG1
More data for this
Ligand-Target Pair
Protein-serine O-palmitoleoyltransferase porcupine


(Mus musculus)
BDBM374798
PNG
(N-(6-methoxybenzo [d]thiazol-2-yl)-2-(4-(pyridin-4...)
Show SMILES COc1ccc2nc(NC(=O)Cc3ccc(cc3)-c3ccncc3)sc2c1
Show InChI InChI=1S/C21H17N3O2S/c1-26-17-6-7-18-19(13-17)27-21(23-18)24-20(25)12-14-2-4-15(5-3-14)16-8-10-22-11-9-16/h2-11,13H,12H2,1H3,(H,23,24,25)
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Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Inhibition of PORCN in mouse Leydig cells overexpressing Wnt3A co-cultured with TM3 cells transfected with Wnt-luciferase gene after 24 hrs by lumine...


ACS Med Chem Lett 7: 676-80 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00038
BindingDB Entry DOI: 10.7270/Q2FB56F9
More data for this
Ligand-Target Pair
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