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Assay Detail

CHEMBL4026922

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

Binding
Inhibition of N-terminal His-tagged Escherichia coli beta-glucuronidase expressed in Escherichia coli BL21 (DE3) using pNPG as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Specific Inhibition of Bacterial β-Glucuronidase by Pyrazolo[4,3-c]quinoline Derivatives via a pH-Dependent Manner To Suppress Chemotherapy-Induced Intestinal Toxicity.
Cheng KW, Tseng CH, Yang CN, Tzeng CC, Cheng TC, Leu YL, Chuang YC, Wang JY, Lu YC, Chen YL, Cheng TL.
J Med Chem (2017) 60 : 9222 -9238
PubMed 29120626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.82 7.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4102433 1 7.84
CHEMBL4084481 1 7.75
CHEMBL4078421 1 7.61
CHEMBL4092228 1 7.53
CHEMBL4063043 1 7.46
CHEMBL4103626 1 7.43
CHEMBL4086989 1 7.42
CHEMBL4064529 1 7.26
CHEMBL4061756 1 7.25
CHEMBL4065549 1 7.01
CHEMBL4083535 1 6.88
CHEMBL4062030 1 6.87
CHEMBL4068317 1 6.81
CHEMBL4065558 1 6.62
CHEMBL4086195 1 6.55
CHEMBL4077288 1 6.51
CHEMBL4086978 1 6.22
CHEMBL4068253 1 6.21
CHEMBL4084537 1 6.20
CHEMBL4065186 1 6.17
CHEMBL3903683 1 6.07
CHEMBL4099232 1 6.05
CHEMBL4073118 1 5.04
CHEMBL1808316 D-SACCHARIC ACID 1,4-LACTONE 1 -
CHEMBL4063721 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4102433 IC50 = 14.4 nM 7.84
CHEMBL4084481 IC50 = 18.0 nM 7.75
CHEMBL4078421 IC50 = 24.7 nM 7.61
CHEMBL4092228 IC50 = 29.6 nM 7.53
CHEMBL4063043 IC50 = 34.8 nM 7.46
CHEMBL4103626 IC50 = 37.3 nM 7.43
CHEMBL4086989 IC50 = 38.1 nM 7.42
CHEMBL4064529 IC50 = 55.3 nM 7.26
CHEMBL4061756 IC50 = 55.6 nM 7.25
CHEMBL4065549 IC50 = 98.2 nM 7.01
CHEMBL4083535 IC50 = 132.6 nM 6.88
CHEMBL4062030 IC50 = 136.5 nM 6.87
CHEMBL4068317 IC50 = 153.6 nM 6.81
CHEMBL4065558 IC50 = 238.2 nM 6.62
CHEMBL4086195 IC50 = 281.4 nM 6.55
CHEMBL4077288 IC50 = 307.8 nM 6.51
CHEMBL4086978 IC50 = 597.7 nM 6.22
CHEMBL4068253 IC50 = 613.1 nM 6.21
CHEMBL4084537 IC50 = 626.0 nM 6.20
CHEMBL4065186 IC50 = 673.3 nM 6.17
CHEMBL3903683 IC50 = 846.0 nM 6.07
CHEMBL4099232 IC50 = 884.2 nM 6.05
CHEMBL4073118 IC50 = 9200.0 nM 5.04
CHEMBL1808316 D-SACCHARIC ACID 1,4-LACTONE IC50 > 10000.0 nM -
CHEMBL4063721 IC50 > 10000.0 nM -