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Assay Detail

CHEMBL3762926

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

Binding
Inhibition of mouse notum pectinacetylesterase expressed in 293F cells by TCF/LEF CellSensor assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type 293F
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Palmitoleoyl-protein carboxylesterase NOTUM (CHEMBL3758064)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase.
Han Q, Pabba PK, Barbosa J, Mabon R, Healy JP, Gardyan MW, Terranova KM, Brommage R, Thompson AY, Schmidt JM, Wilson AG, Xu X, Tarver JE, Carson KG.
Bioorg Med Chem Lett (2016) 26 : 1184 -1187
PubMed 26821819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 7.46 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3759074 1 8.22
CHEMBL3760048 1 8.22
CHEMBL3758280 1 8.15
CHEMBL3758963 1 8.15
CHEMBL3759297 1 8.15
CHEMBL3758291 1 8.10
CHEMBL3758275 1 8.10
CHEMBL3759274 1 8.05
CHEMBL3758560 1 7.92
CHEMBL3759069 1 7.89
CHEMBL3760062 1 7.89
CHEMBL3759323 1 7.85
CHEMBL3758326 1 7.80
CHEMBL3758279 1 7.77
CHEMBL3759908 1 7.77
CHEMBL3759117 1 7.75
CHEMBL3759576 1 7.72
CHEMBL3760106 1 7.70
CHEMBL3759044 1 7.68
CHEMBL3758668 1 7.64
CHEMBL3759027 1 7.57
CHEMBL3758454 1 7.55
CHEMBL3759406 1 7.51
CHEMBL3759035 1 7.44
CHEMBL3759995 1 7.42
CHEMBL3758201 1 7.41
CHEMBL3758520 1 7.41
CHEMBL3758861 1 7.39
CHEMBL3759700 1 7.34
CHEMBL3760065 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3759074 EC50 = 6.0 nM 8.22
CHEMBL3760048 EC50 = 6.0 nM 8.22
CHEMBL3758963 EC50 = 7.0 nM 8.15
CHEMBL3759297 EC50 = 7.0 nM 8.15
CHEMBL3758280 EC50 = 7.0 nM 8.15
CHEMBL3758291 EC50 = 8.0 nM 8.10
CHEMBL3758275 EC50 = 8.0 nM 8.10
CHEMBL3759274 EC50 = 9.0 nM 8.05
CHEMBL3758560 EC50 = 12.0 nM 7.92
CHEMBL3759069 EC50 = 13.0 nM 7.89
CHEMBL3760062 EC50 = 13.0 nM 7.89
CHEMBL3759323 EC50 = 14.0 nM 7.85
CHEMBL3758326 EC50 = 16.0 nM 7.80
CHEMBL3758279 EC50 = 17.0 nM 7.77
CHEMBL3759908 EC50 = 17.0 nM 7.77
CHEMBL3759117 EC50 = 18.0 nM 7.75
CHEMBL3759576 EC50 = 19.0 nM 7.72
CHEMBL3760106 EC50 = 20.0 nM 7.70
CHEMBL3759044 EC50 = 21.0 nM 7.68
CHEMBL3758668 EC50 = 23.0 nM 7.64
CHEMBL3759027 EC50 = 27.0 nM 7.57
CHEMBL3758454 EC50 = 28.0 nM 7.55
CHEMBL3759406 EC50 = 31.0 nM 7.51
CHEMBL3759035 EC50 = 36.0 nM 7.44
CHEMBL3759995 EC50 = 38.0 nM 7.42
CHEMBL3758201 EC50 = 39.0 nM 7.41
CHEMBL3758520 EC50 = 39.0 nM 7.41
CHEMBL3758861 EC50 = 41.0 nM 7.39
CHEMBL3759700 EC50 = 46.0 nM 7.34
CHEMBL3760065 EC50 = 49.0 nM 7.31
CHEMBL3758239 EC50 = 53.0 nM 7.28
CHEMBL3758678 EC50 = 59.0 nM 7.23
CHEMBL3759635 EC50 = 67.0 nM 7.17
CHEMBL3760070 EC50 = 77.0 nM 7.11
CHEMBL3759129 EC50 = 84.0 nM 7.08
CHEMBL3758297 EC50 = 133.0 nM 6.88
CHEMBL3759300 EC50 = 175.0 nM 6.76
CHEMBL3759068 EC50 = 243.0 nM 6.61
CHEMBL1421818 EC50 = 361.0 nM 6.44
CHEMBL3758736 EC50 = 706.0 nM 6.15
CHEMBL3758532 EC50 = 1185.0 nM 5.93
CHEMBL1499110 EC50 = 1360.0 nM 5.87