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Assay Detail

CHEMBL831381

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

Binding
Inhibitory concentration against human sodium/hydrogen exchanger (NHE-1) in PS120 variant cells
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium/hydrogen exchanger 1 (CHEMBL2781)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Substituted (benzo[b]thiophene-2-carbonyl)guanidines as novel Na+/H+ exchanger isoform-1 (NHE-1) inhibitors.
Lee S, Lee H, Yi KY, Lee BH, Yoo SE, Lee K, Cho NS.
Bioorg Med Chem Lett (2005) 15 : 2998 -3001
PubMed 15914000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.71 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196715 1 6.77
CHEMBL197401 1 6.70
CHEMBL195422 1 6.70
CHEMBL196790 1 6.57
CHEMBL425378 1 6.51
CHEMBL197519 1 6.40
CHEMBL196487 1 6.32
CHEMBL436559 CARIPORIDE 2.0 1 6.17
CHEMBL425565 1 6.17
CHEMBL193812 1 6.07
CHEMBL196714 1 5.77
CHEMBL371454 1 5.70
CHEMBL197156 1 5.64
CHEMBL193701 1 5.60
CHEMBL193499 1 5.60
CHEMBL197155 1 5.47
CHEMBL372839 1 5.47
CHEMBL197409 1 5.41
CHEMBL370216 1 5.38
CHEMBL195986 1 5.36
CHEMBL263960 1 5.29
CHEMBL436285 1 5.25
CHEMBL196655 1 5.11
CHEMBL197147 1 5.08
CHEMBL195507 1 5.07
CHEMBL196066 1 5.05
CHEMBL196943 1 4.96
CHEMBL193941 1 4.96
CHEMBL196645 1 4.92
CHEMBL372360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196715 IC50 = 170.0 nM 6.77
CHEMBL197401 IC50 = 200.0 nM 6.70
CHEMBL195422 IC50 = 200.0 nM 6.70
CHEMBL196790 IC50 = 270.0 nM 6.57
CHEMBL425378 IC50 = 310.0 nM 6.51
CHEMBL197519 IC50 = 400.0 nM 6.40
CHEMBL196487 IC50 = 480.0 nM 6.32
CHEMBL436559 CARIPORIDE IC50 = 680.0 nM 6.17
CHEMBL425565 IC50 = 680.0 nM 6.17
CHEMBL193812 IC50 = 850.0 nM 6.07
CHEMBL196714 IC50 = 1700.0 nM 5.77
CHEMBL371454 IC50 = 2000.0 nM 5.70
CHEMBL197156 IC50 = 2300.0 nM 5.64
CHEMBL193701 IC50 = 2500.0 nM 5.60
CHEMBL193499 IC50 = 2500.0 nM 5.60
CHEMBL372839 IC50 = 3400.0 nM 5.47
CHEMBL197155 IC50 = 3400.0 nM 5.47
CHEMBL197409 IC50 = 3900.0 nM 5.41
CHEMBL370216 IC50 = 4200.0 nM 5.38
CHEMBL195986 IC50 = 4400.0 nM 5.36
CHEMBL263960 IC50 = 5100.0 nM 5.29
CHEMBL436285 IC50 = 5600.0 nM 5.25
CHEMBL196655 IC50 = 7700.0 nM 5.11
CHEMBL197147 IC50 = 8400.0 nM 5.08
CHEMBL195507 IC50 = 8600.0 nM 5.07
CHEMBL196066 IC50 = 8900.0 nM 5.05
CHEMBL196943 IC50 = 11000.0 nM 4.96
CHEMBL193941 IC50 = 11000.0 nM 4.96
CHEMBL196645 IC50 = 12000.0 nM 4.92
CHEMBL372360 IC50 > 30000.0 nM -
CHEMBL194606 IC50 > 30000.0 nM -
CHEMBL427551 IC50 > 30000.0 nM -