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Assay Detail

CHEMBL2330993

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

Binding
Inhibition of porcupine-mediated Wnt signalling in mouse L cells after 24 hrs by SpringerImages-Topflash reporter assay
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The development of highly potent inhibitors for porcupine.
Wang X, Moon J, Dodge ME, Pan X, Zhang L, Hanson JM, Tuladhar R, Ma Z, Shi H, Williams NS, Amatruda JF, Carroll TJ, Lum L, Chen C.
J Med Chem (2013) 56 : 2700 -2704
PubMed 23477365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 63 7.44 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2323230 1 9.52
CHEMBL2322627 1 9.52
CHEMBL2323228 1 9.35
CHEMBL2323231 1 9.30
CHEMBL2322632 1 9.12
CHEMBL2323233 1 9.00
CHEMBL2322628 1 8.82
CHEMBL2322624 1 8.82
CHEMBL2322626 1 8.70
CHEMBL2323229 1 8.52
CHEMBL2322625 1 8.46
CHEMBL2322629 1 8.46
CHEMBL2322635 1 8.40
CHEMBL2322623 1 8.26
CHEMBL1581616 1 7.82
CHEMBL2323232 1 7.82
CHEMBL2324275 1 7.82
CHEMBL2324274 1 7.60
CHEMBL2322622 1 7.60
CHEMBL1257090 1 7.60
CHEMBL2324273 1 7.52
CHEMBL1257064 1 7.52
CHEMBL2323243 1 7.52
CHEMBL2325505 1 7.52
CHEMBL2325512 1 7.46
CHEMBL2322620 1 7.46
CHEMBL1257089 1 7.40
CHEMBL2324266 1 7.40
CHEMBL2324277 1 7.40
CHEMBL2325509 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2323230 EC50 = 0.3 nM 9.52
CHEMBL2322627 EC50 = 0.3 nM 9.52
CHEMBL2323228 EC50 = 0.45 nM 9.35
CHEMBL2323231 EC50 = 0.5 nM 9.30
CHEMBL2322632 EC50 = 0.75 nM 9.12
CHEMBL2323233 EC50 = 1.0 nM 9.00
CHEMBL2322628 EC50 = 1.5 nM 8.82
CHEMBL2322624 EC50 = 1.5 nM 8.82
CHEMBL2322626 EC50 = 2.0 nM 8.70
CHEMBL2323229 EC50 = 3.0 nM 8.52
CHEMBL2322625 EC50 = 3.5 nM 8.46
CHEMBL2322629 EC50 = 3.5 nM 8.46
CHEMBL2322635 EC50 = 4.0 nM 8.40
CHEMBL2322623 EC50 = 5.5 nM 8.26
CHEMBL2324275 EC50 = 15.0 nM 7.82
CHEMBL1581616 EC50 = 15.0 nM 7.82
CHEMBL2323232 EC50 = 15.0 nM 7.82
CHEMBL2324274 EC50 = 25.0 nM 7.60
CHEMBL2322622 EC50 = 25.0 nM 7.60
CHEMBL1257090 EC50 = 25.0 nM 7.60
CHEMBL2324273 EC50 = 30.0 nM 7.52
CHEMBL1257064 EC50 = 30.0 nM 7.52
CHEMBL2323243 EC50 = 30.0 nM 7.52
CHEMBL2325505 EC50 = 30.0 nM 7.52
CHEMBL2322620 EC50 = 35.0 nM 7.46
CHEMBL2325512 EC50 = 35.0 nM 7.46
CHEMBL1257089 EC50 = 40.0 nM 7.40
CHEMBL2324266 EC50 = 40.0 nM 7.40
CHEMBL2324277 EC50 = 40.0 nM 7.40
CHEMBL2325509 EC50 = 40.0 nM 7.40
CHEMBL2324279 EC50 = 50.0 nM 7.30
CHEMBL2325511 EC50 = 50.0 nM 7.30
CHEMBL2323239 EC50 = 55.0 nM 7.26
CHEMBL1257063 EC50 = 60.0 nM 7.22
CHEMBL2322631 EC50 = 90.0 nM 7.05
CHEMBL2324276 EC50 = 90.0 nM 7.05
CHEMBL2324265 EC50 = 90.0 nM 7.05
CHEMBL2325506 EC50 = 100.0 nM 7.00
CHEMBL2322621 EC50 = 100.0 nM 7.00
CHEMBL2324267 EC50 = 100.0 nM 7.00
CHEMBL2325513 EC50 = 110.0 nM 6.96
CHEMBL2322619 EC50 = 120.0 nM 6.92
CHEMBL2325510 EC50 = 175.0 nM 6.76
CHEMBL2322630 EC50 = 210.0 nM 6.68
CHEMBL2325507 EC50 = 240.0 nM 6.62
CHEMBL2324278 EC50 = 250.0 nM 6.60
CHEMBL2323234 EC50 = 300.0 nM 6.52
CHEMBL2323238 EC50 = 350.0 nM 6.46
CHEMBL2324272 EC50 = 470.0 nM 6.33
CHEMBL2323237 EC50 = 580.0 nM 6.24