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Assay Detail

CHEMBL4313181

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

Binding
Inhibition of human NPP3 expressed in COS-7 cell membranes assessed as reduction in p-nitrophenol production using pNP-TMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and measured after 35 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Synthesis, biological evaluation, and docking studies of new raloxifene sulfonate or sulfamate derivatives as inhibitors of nucleotide pyrophosphatase/phosphodiesterase.
El-Gamal MI, Ullah S, Zaraei SO, Jalil S, Zaib S, Zaher DM, Omar HA, Anbar HS, Pelletier J, Sévigny J, Iqbal J.
Eur J Med Chem (2019) 181 : 111560 -111560
PubMed 31382118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.05 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4540180 1 6.64
CHEMBL4561757 1 6.31
CHEMBL4473374 1 6.15
CHEMBL4589775 1 5.91
CHEMBL4556663 1 5.82
CHEMBL4474803 1 5.81
CHEMBL4443387 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4540180 IC50 = 230.0 nM 6.64
CHEMBL4561757 IC50 = 490.0 nM 6.31
CHEMBL4473374 IC50 = 710.0 nM 6.15
CHEMBL4589775 IC50 = 1240.0 nM 5.91
CHEMBL4556663 IC50 = 1510.0 nM 5.82
CHEMBL4474803 IC50 = 1550.0 nM 5.81
CHEMBL4443387 IC50 = 1810.0 nM 5.74