ChEMBL ligand: CHEMBL2139947
porcupine O-acyltransferase/Protein-serine O-palmitoleoyltransferase porcupine in Human [ChEMBL: CHEMBL1255163] [GtoPdb: 3145] [UniProtKB: Q9H237] There should be some charts here, you may need to enable JavaScript!
Protein Wnt-3a in Human [ChEMBL: CHEMBL1255137] [UniProtKB: P56704] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
porcupine O-acyltransferase/Protein-serine O-palmitoleoyltransferase porcupine in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255163] [GtoPdb: 3145] [UniProtKB: Q9H237]
ChEMBL	Inhibition of porcupine in HEK293T cells transfected with Wnt3A-expressing vector assessed as suppression of Wnt/beta-catenin signaling after 22 hrs by Super-top flash reporter gene assay	B	9	pIC50	<1	nM	IC50	J Med Chem (2018) 61: 4087-4102 [PMID:29630366]
GtoPdb	Measuring inhibition of PORCN activity expressed in human HT1080 cells in a Wnt3A-driven luciferase production assay	-	10.13	pIC50	0.07	nM	IC50	Bioorg Med Chem Lett (2015) 25: 5472-6 [PMID:26522946]
ChEMBL	Inhibition of porcupine activity (unknown origin) expressed in human HT1080 cells assessed as suppression of Wnt3A-mediated super top flash activity by STF luciferase assay	B	10.13	pIC50	0.07	nM	IC50	Bioorg Med Chem Lett (2015) 25: 5472-5476 [PMID:26522946]
Protein Wnt-3a in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255137] [UniProtKB: P56704]
ChEMBL	Wnt-Luc Reporter Assay: Human embryonic kidney 293 cells (obtained from American Type Culture Collection, ATCC, Manassas, Va.) are cultured in DMEM medium (Gibco/Invitrogen, Carlsbad, Calif.) supplemented with 10% FBS (Gibco/Invitrogen, Carlsbad, Calif.), 50 unit/mL penicillin and 50 μg/mL of streptomycin (Gibco/Invitrogen, Carlsbad, Calif.) at 37° C. with 5% CO2 in air atmosphere. 293 cells in a 10 cm dish are co-transfected with 8 μg of STF-reporter plasmid containing a luciferase gene driven by Wnt-responsive elements and 2 μg of pcDNA3.1-Neo (Gibco/Invitrogen, Carlsbad, Calif.) with 30 μL of FuGENE6 (Roche Diagnostics, Indianapolis, Ind.) following the manufacturer's protocol. Stable cell lines (293 Wnt-Luc) were selected with 400 μg/mL of G418 (Gibco/Invitrogen, Carlsbad, Calif.). The 293 Wnt-Luc cells and L-cell Wnt3a cells (obtained from American Type Culture Collection, ATCC, Manassas, Va.) are trypsinized and co-cultured into a 384-well plate with DMEM medium supplemented with 2% FBS, and treated with different concentrations of a compound of the invention. After 24 hours, the firefly luciferase activities are assayed with the Bright-Glo Luciferase Assay System (Promega, Madison, Wis.). The IC50 is measured when the effect of the compound reduces the luminescence signal by 50%.	B	9.96	pIC50	<0.11	nM	IC50	US-10251893-B2. N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators (2019)

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]