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Assay Detail

CHEMBL1787961

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

Binding
Inhibition of NHE1-mediated rat platelet swelling
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium/hydrogen exchanger 1 (CHEMBL2577)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis and biological evaluation of novel substituted benzoylguanidine derivatives as potent Na+/H+ exchanger inhibitors.
Xu WT, Jin N, Xu J, Xu YG, Wang QJ, You QD.
Bioorg Med Chem Lett (2009) 19 : 3283 -3287
PubMed 19433354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.55 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1783852 1 8.44
CHEMBL1783857 1 8.35
CHEMBL1783849 1 7.96
CHEMBL1783830 1 7.94
CHEMBL1783853 1 7.85
CHEMBL1783856 1 7.82
CHEMBL1783854 1 7.73
CHEMBL1783847 1 7.44
CHEMBL1783848 1 7.44
CHEMBL1783850 1 7.39
CHEMBL436559 CARIPORIDE 2.0 1 7.19
CHEMBL1783851 1 6.61
CHEMBL1783855 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1783852 IC50 = 3.6 nM 8.44
CHEMBL1783857 IC50 = 4.48 nM 8.35
CHEMBL1783849 IC50 = 11.1 nM 7.96
CHEMBL1783830 IC50 = 11.5 nM 7.94
CHEMBL1783853 IC50 = 14.2 nM 7.85
CHEMBL1783856 IC50 = 15.0 nM 7.82
CHEMBL1783854 IC50 = 18.7 nM 7.73
CHEMBL1783847 IC50 = 36.4 nM 7.44
CHEMBL1783848 IC50 = 36.5 nM 7.44
CHEMBL1783850 IC50 = 40.5 nM 7.39
CHEMBL436559 CARIPORIDE IC50 = 65.0 nM 7.19
CHEMBL1783851 IC50 = 248.0 nM 6.61
CHEMBL1783855 IC50 = 1150.0 nM 5.94