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Assay Detail

CHEMBL3870974

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

Binding
Inhibition of porcupine-mediated Wnt signaling in mouse L-cells after 24 hrs by springerImage-Topflash reporter assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein-serine O-palmitoleoyltransferase porcupine (CHEMBL1255164)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Development of a triazole class of highly potent Porcn inhibitors.
You L, Zhang C, Yarravarapu N, Morlock L, Wang X, Zhang L, Williams NS, Lum L, Chen C.
Bioorg Med Chem Lett (2016) 26 : 5891 -5895
PubMed 27876319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 8.36 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3970245 1 10.10
CHEMBL3933984 1 9.89
CHEMBL3952126 1 9.85
CHEMBL3952665 1 9.74
CHEMBL3925918 1 9.70
CHEMBL3899701 1 9.70
CHEMBL3943764 1 9.59
CHEMBL3935037 1 9.52
CHEMBL3952501 1 9.40
CHEMBL3927718 1 9.40
CHEMBL3892208 1 9.37
CHEMBL3897216 1 9.32
CHEMBL3980962 1 9.22
CHEMBL3953544 1 9.22
CHEMBL3981277 1 9.19
CHEMBL3907204 1 9.15
CHEMBL3905849 1 8.74
CHEMBL3943114 1 8.74
CHEMBL3893457 1 8.52
CHEMBL3947115 1 8.30
CHEMBL3968025 1 8.19
CHEMBL3954145 1 8.15
CHEMBL3982830 1 8.10
CHEMBL3972297 1 8.10
CHEMBL3926685 1 8.05
CHEMBL3936691 1 8.05
CHEMBL3959152 1 7.92
CHEMBL3908085 1 7.75
CHEMBL3908747 1 7.40
CHEMBL3916470 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3970245 EC50 = 0.08 nM 10.10
CHEMBL3933984 EC50 = 0.13 nM 9.89
CHEMBL3952126 EC50 = 0.14 nM 9.85
CHEMBL3952665 EC50 = 0.18 nM 9.74
CHEMBL3925918 EC50 = 0.2 nM 9.70
CHEMBL3899701 EC50 = 0.2 nM 9.70
CHEMBL3943764 EC50 = 0.26 nM 9.59
CHEMBL3935037 EC50 = 0.3 nM 9.52
CHEMBL3952501 EC50 = 0.4 nM 9.40
CHEMBL3927718 EC50 = 0.4 nM 9.40
CHEMBL3892208 EC50 = 0.43 nM 9.37
CHEMBL3897216 EC50 = 0.48 nM 9.32
CHEMBL3980962 EC50 = 0.6 nM 9.22
CHEMBL3953544 EC50 = 0.6 nM 9.22
CHEMBL3981277 EC50 = 0.65 nM 9.19
CHEMBL3907204 EC50 = 0.7 nM 9.15
CHEMBL3905849 EC50 = 1.8 nM 8.74
CHEMBL3943114 EC50 = 1.8 nM 8.74
CHEMBL3893457 EC50 = 3.0 nM 8.52
CHEMBL3947115 EC50 = 5.0 nM 8.30
CHEMBL3968025 EC50 = 6.5 nM 8.19
CHEMBL3954145 EC50 = 7.0 nM 8.15
CHEMBL3982830 EC50 = 8.0 nM 8.10
CHEMBL3972297 EC50 = 8.0 nM 8.10
CHEMBL3926685 EC50 = 9.0 nM 8.05
CHEMBL3936691 EC50 = 9.0 nM 8.05
CHEMBL3959152 EC50 = 12.0 nM 7.92
CHEMBL3908085 EC50 = 18.0 nM 7.75
CHEMBL3908747 EC50 = 40.0 nM 7.40
CHEMBL3916470 EC50 = 100.0 nM 7.00
CHEMBL3893937 EC50 = 200.0 nM 6.70
CHEMBL3961192 EC50 = 270.0 nM 6.57
CHEMBL3917072 EC50 = 400.0 nM 6.40
CHEMBL3986815 EC50 = 500.0 nM 6.30
CHEMBL3978552 EC50 = 2500.0 nM 5.60
CHEMBL3901161 EC50 = 80000.0 nM 4.10
CHEMBL3889524 EC50 > 5000.0 nM -
CHEMBL3963609 EC50 > 1000.0 nM -
CHEMBL3917551 EC50 > 5000.0 nM -
CHEMBL3945422 EC50 > 1000.0 nM -