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Assay Detail

CHEMBL3863940

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

Binding
Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by neutral red uptake assay
11
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Shigella dysenteriae
Cell Type Vero
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Shiga toxin subunit A (CHEMBL3879822)
Type SINGLE PROTEIN
Organism Shigella dysenteriae

Publication

In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
Chauhan V, Chaudhary D, Pathak U, Saxena N, Dhaked RK.
J Med Chem (2016) 59 : 10763 -10773
PubMed 27933947 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.07 5.58
Inhibition 1 - -
Imax 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3935227 1 5.58
CHEMBL250859 1 5.11
CHEMBL3963596 3 5.10
CHEMBL3924676 1 5.09
CHEMBL219568 GUANINE 3.0 1 4.94
CHEMBL1467 ALLOPURINOL 4.0 1 4.62
CHEMBL3933587 1 -
CHEMBL3952356 1 -
CHEMBL3939786 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3935227 IC50 = 2630.0 nM 5.58
CHEMBL250859 IC50 = 7700.0 nM 5.11
CHEMBL3963596 IC50 = 7960.0 nM 5.10
CHEMBL3924676 IC50 = 8200.0 nM 5.09
CHEMBL219568 GUANINE IC50 = 11500.0 nM 4.94
CHEMBL1467 ALLOPURINOL IC50 = 23900.0 nM 4.62
CHEMBL3933587 IC50 - -
CHEMBL3952356 IC50 - -
CHEMBL3939786 IC50 - -
CHEMBL3963596 Inhibition - % -
CHEMBL3963596 Imax = 12.0 uM -