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Assay Detail

CHEMBL1832155

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

Binding
Inhibition of NHE1 in Sprague-Dawley rat assessed as inhibition of acid-induced platelet swelling by spectrophotometric analysis
25
Total Activities
25
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

Synthesis and Na+/H+ exchanger inhibitory activity of benzoylguanidine derivatives.
Jin L, Jiang XM, Du P, Xu J, Gong GQ, Wang QJ, Xu YG.
Eur J Med Chem (2011) 46 : 4107 -4116
PubMed 21724305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 8.27 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1829127 1 10.17
CHEMBL1829122 1 10.14
CHEMBL1829125 1 10.08
CHEMBL1829126 1 10.04
CHEMBL1829123 1 9.96
CHEMBL1829132 1 9.51
CHEMBL1829128 1 9.28
CHEMBL1829133 1 9.25
CHEMBL1829139 1 9.17
CHEMBL1829138 1 9.04
CHEMBL1829117 1 8.97
CHEMBL1829134 1 8.96
CHEMBL1829137 1 8.82
CHEMBL1789669 1 8.74
CHEMBL436559 CARIPORIDE 2.0 1 7.51
CHEMBL1829130 1 7.31
CHEMBL1829136 1 7.25
CHEMBL1829119 1 7.03
CHEMBL1829124 1 6.90
CHEMBL1829129 1 6.86
CHEMBL1829121 1 6.85
CHEMBL1829118 1 6.81
CHEMBL1829131 1 6.65
CHEMBL1829135 1 5.82
CHEMBL1829120 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1829127 IC50 = 0.068 nM 10.17
CHEMBL1829122 IC50 = 0.073 nM 10.14
CHEMBL1829125 IC50 = 0.084 nM 10.08
CHEMBL1829126 IC50 = 0.091 nM 10.04
CHEMBL1829123 IC50 = 0.11 nM 9.96
CHEMBL1829132 IC50 = 0.31 nM 9.51
CHEMBL1829128 IC50 = 0.53 nM 9.28
CHEMBL1829133 IC50 = 0.56 nM 9.25
CHEMBL1829139 IC50 = 0.67 nM 9.17
CHEMBL1829138 IC50 = 0.92 nM 9.04
CHEMBL1829117 IC50 = 1.06 nM 8.97
CHEMBL1829134 IC50 = 1.1 nM 8.96
CHEMBL1829137 IC50 = 1.5 nM 8.82
CHEMBL1789669 IC50 = 1.82 nM 8.74
CHEMBL436559 CARIPORIDE IC50 = 30.7 nM 7.51
CHEMBL1829130 IC50 = 49.3 nM 7.31
CHEMBL1829136 IC50 = 55.7 nM 7.25
CHEMBL1829119 IC50 = 93.5 nM 7.03
CHEMBL1829124 IC50 = 125.0 nM 6.90
CHEMBL1829129 IC50 = 139.0 nM 6.86
CHEMBL1829121 IC50 = 142.0 nM 6.85
CHEMBL1829118 IC50 = 154.0 nM 6.81
CHEMBL1829131 IC50 = 225.0 nM 6.65
CHEMBL1829135 IC50 = 1530.0 nM 5.82
CHEMBL1829120 IC50 = 3020.0 nM 5.52