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Assay Detail

CHEMBL4223022

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

Binding
Inhibition of recombinant Neisseria meningitidis glycosyltransferase LgtC using UDP-Gal/lactose as substrate preincubated for 30 mins with UDP-Gal followed by lactose addition measured after 20 mins in presence of MnCl2 and calf intestinal phosphatase by malachite green dye based enzyme-coupled colorimetric assay relative to control
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Neisseria meningitidis
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

LgtC (CHEMBL4295919)
Type SINGLE PROTEIN
Organism Neisseria meningitidis

Publication

Structure-activity relationships in a new class of non-substrate-like covalent inhibitors of the bacterial glycosyltransferase LgtC.
Xu Y, Cuccui J, Denman C, Maharjan T, Wren BW, Wagner GK.
Bioorg Med Chem (2018) 26 : 2973 -2983
PubMed 29602676 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.10 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379966 1 5.54
CHEMBL4227320 1 5.52
CHEMBL4060241 1 5.51
CHEMBL4227590 1 5.37
CHEMBL4226574 1 4.92
CHEMBL4074318 1 4.75
CHEMBL4229261 1 4.60
CHEMBL4227242 1 4.55
CHEMBL4228599 1 -
CHEMBL4226164 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379966 IC50 = 2900.0 nM 5.54
CHEMBL4227320 IC50 = 3000.0 nM 5.52
CHEMBL4060241 IC50 = 3100.0 nM 5.51
CHEMBL4227590 IC50 = 4300.0 nM 5.37
CHEMBL4226574 IC50 = 12000.0 nM 4.92
CHEMBL4074318 IC50 = 18000.0 nM 4.75
CHEMBL4229261 IC50 = 25000.0 nM 4.60
CHEMBL4227242 IC50 = 28000.0 nM 4.55
CHEMBL4228599 IC50 > 50000.0 nM -
CHEMBL4226164 IC50 > 100000.0 nM -