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Assay Detail

CHEMBL3778288

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

Binding
Inhibition of human notum pectinacetylesterase expressed in 293F cells after 30 mins by TCF/LEF cell sensor assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Palmitoleoyl-protein carboxylesterase NOTUM (CHEMBL3714531)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase.
Tarver JE, Pabba PK, Barbosa J, Han Q, Gardyan MW, Brommage R, Thompson AY, Schmidt JM, Wilson AG, He W, Lombardo VK, Carson KG.
Bioorg Med Chem Lett (2016) 26 : 1525 -1528
PubMed 26897593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 6.45 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3774864 1 7.92
CHEMBL3774760 1 7.68
CHEMBL3775257 1 7.06
CHEMBL3774528 1 6.97
CHEMBL3775525 1 6.94
CHEMBL3774472 1 6.84
CHEMBL3775309 1 6.78
CHEMBL3775700 1 6.68
CHEMBL3775154 1 6.68
CHEMBL3775791 1 6.60
CHEMBL3775931 1 6.60
CHEMBL3775182 1 6.55
CHEMBL3775492 1 6.41
CHEMBL3774544 1 6.40
CHEMBL3775531 1 6.38
CHEMBL3775413 1 6.36
CHEMBL3775896 1 6.35
CHEMBL3775859 1 6.32
CHEMBL3775635 1 6.25
CHEMBL1689356 1 6.24
CHEMBL3774810 1 6.10
CHEMBL3775731 1 6.08
CHEMBL3775000 1 6.07
CHEMBL3774802 1 6.05
CHEMBL3774730 1 6.05
CHEMBL3775407 1 5.83
CHEMBL3774524 1 5.71
CHEMBL3774745 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3774864 EC50 = 12.0 nM 7.92
CHEMBL3774760 EC50 = 21.0 nM 7.68
CHEMBL3775257 EC50 = 88.0 nM 7.06
CHEMBL3774528 EC50 = 107.0 nM 6.97
CHEMBL3775525 EC50 = 115.0 nM 6.94
CHEMBL3774472 EC50 = 144.0 nM 6.84
CHEMBL3775309 EC50 = 168.0 nM 6.78
CHEMBL3775700 EC50 = 208.0 nM 6.68
CHEMBL3775154 EC50 = 211.0 nM 6.68
CHEMBL3775791 EC50 = 249.0 nM 6.60
CHEMBL3775931 EC50 = 250.0 nM 6.60
CHEMBL3775182 EC50 = 280.0 nM 6.55
CHEMBL3775492 EC50 = 393.0 nM 6.41
CHEMBL3774544 EC50 = 400.0 nM 6.40
CHEMBL3775531 EC50 = 417.0 nM 6.38
CHEMBL3775413 EC50 = 435.0 nM 6.36
CHEMBL3775896 EC50 = 445.0 nM 6.35
CHEMBL3775859 EC50 = 477.0 nM 6.32
CHEMBL3775635 EC50 = 556.0 nM 6.25
CHEMBL1689356 EC50 = 570.0 nM 6.24
CHEMBL3774810 EC50 = 789.0 nM 6.10
CHEMBL3775731 EC50 = 835.0 nM 6.08
CHEMBL3775000 EC50 = 857.0 nM 6.07
CHEMBL3774802 EC50 = 885.0 nM 6.05
CHEMBL3774730 EC50 = 881.0 nM 6.05
CHEMBL3775407 EC50 = 1462.0 nM 5.83
CHEMBL3774524 EC50 = 1965.0 nM 5.71
CHEMBL3774745 EC50 = 21928.0 nM 4.66