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Assay Detail

CHEMBL3295183

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

Binding
Inhibition of beta-glucuronidase activity (unknown origin) assessed as p-nitrophenol formation after 30 mins using p-nitrophenyl-beta-D-glucuronide as substrate by spectrophotometry
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-glucuronidase (CHEMBL2728)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and β-glucuronidase inhibitory activity of 2-arylquinazolin-4(3H)-ones.
Khan KM, Saad SM, Shaikh NN, Hussain S, Fakhri MI, Perveen S, Taha M, Choudhary MI.
Bioorg Med Chem (2014) 22 : 3449 -3454
PubMed 24844756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.19 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL137922 1 6.22
CHEMBL3289121 1 6.16
CHEMBL336718 1 5.96
CHEMBL3289115 1 5.93
CHEMBL3289116 1 5.82
CHEMBL3289123 1 5.75
CHEMBL3289122 1 5.75
CHEMBL3289384 1 5.68
CHEMBL3289117 1 5.68
CHEMBL3289112 1 5.55
CHEMBL3289119 1 5.50
CHEMBL1333995 1 5.26
CHEMBL1526444 1 5.00
CHEMBL1164165 1 4.70
CHEMBL3289108 1 4.65
CHEMBL3289120 1 4.51
CHEMBL3289113 1 4.42
CHEMBL1163173 1 4.40
CHEMBL3289124 1 4.36
CHEMBL1808316 D-SACCHARIC ACID 1,4-LACTONE 1 4.34
CHEMBL3289111 1 4.30
CHEMBL3289118 1 4.21
CHEMBL127066 1 -
CHEMBL3289114 1 -
CHEMBL3289110 1 -
CHEMBL3289109 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL137922 IC50 = 600.0 nM 6.22
CHEMBL3289121 IC50 = 700.0 nM 6.16
CHEMBL336718 IC50 = 1100.0 nM 5.96
CHEMBL3289115 IC50 = 1170.0 nM 5.93
CHEMBL3289116 IC50 = 1500.0 nM 5.82
CHEMBL3289123 IC50 = 1800.0 nM 5.75
CHEMBL3289122 IC50 = 1800.0 nM 5.75
CHEMBL3289384 IC50 = 2100.0 nM 5.68
CHEMBL3289117 IC50 = 2100.0 nM 5.68
CHEMBL3289112 IC50 = 2800.0 nM 5.55
CHEMBL3289119 IC50 = 3200.0 nM 5.50
CHEMBL1333995 IC50 = 5500.0 nM 5.26
CHEMBL1526444 IC50 = 10000.0 nM 5.00
CHEMBL1164165 IC50 = 20100.0 nM 4.70
CHEMBL3289108 IC50 = 22200.0 nM 4.65
CHEMBL3289120 IC50 = 30900.0 nM 4.51
CHEMBL3289113 IC50 = 37700.0 nM 4.42
CHEMBL1163173 IC50 = 39800.0 nM 4.40
CHEMBL3289124 IC50 = 44000.0 nM 4.36
CHEMBL1808316 D-SACCHARIC ACID 1,4-LACTONE IC50 = 45750.0 nM 4.34
CHEMBL3289111 IC50 = 50400.0 nM 4.30
CHEMBL3289118 IC50 = 61030.0 nM 4.21
CHEMBL127066 IC50 = 177000.0 nM -
CHEMBL3289114 IC50 = 120500.0 nM -
CHEMBL3289110 IC50 = 198200.0 nM -
CHEMBL3289109 IC50 = 172700.0 nM -