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Assay Detail

CHEMBL4040030

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of porcupine (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein-serine O-palmitoleoyltransferase porcupine (CHEMBL1255163)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.
Ho SY, Alam J, Jeyaraj DA, Wang W, Lin GR, Ang SH, Tan ESW, Lee MA, Ke Z, Madan B, Virshup DM, Ding LJ, Manoharan V, Chew YS, Low CB, Pendharkar V, Sangthongpitag K, Hill J, Keller TH, Poulsen A.
J Med Chem (2017) 60 : 6678 -6692
PubMed 28671458 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.39 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3188386 WNT-974 2.0 1 9.40
CHEMBL3633802 ETC-159 1.0 1 8.54
CHEMBL4088085 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3188386 WNT-974 IC50 = 0.4 nM 9.40
CHEMBL3633802 ETC-159 IC50 = 2.9 nM 8.54
CHEMBL4088085 IC50 = 60.0 nM 7.22