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Assay Detail

CHEMBL832458

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

Binding
Inhibitory activity against Na+/H+ exchanger 1 (NHE-1) expressed in PS120 cells
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PS120
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.
Lee S, Yi KY, Hwang SK, Lee BH, Yoo SE, Lee K.
J Med Chem (2005) 48 : 2882 -2891
PubMed 15828827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 5.80 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192227 1 7.09
CHEMBL195277 1 7.03
CHEMBL192825 1 6.92
CHEMBL371801 1 6.89
CHEMBL363344 1 6.85
CHEMBL193004 1 6.85
CHEMBL189789 1 6.64
CHEMBL192634 1 6.47
CHEMBL189792 1 6.32
CHEMBL366228 1 6.19
CHEMBL193311 1 6.14
CHEMBL192185 1 6.12
CHEMBL189970 1 5.96
CHEMBL189048 1 5.96
CHEMBL436559 CARIPORIDE 2.0 1 5.92
CHEMBL194157 1 5.89
CHEMBL366227 1 5.89
CHEMBL372051 1 5.85
CHEMBL192601 1 5.77
CHEMBL192109 1 5.77
CHEMBL424813 1 5.70
CHEMBL425186 1 5.64
CHEMBL370954 1 5.64
CHEMBL195160 1 5.62
CHEMBL192635 1 5.62
CHEMBL373324 1 5.58
CHEMBL365153 1 5.52
CHEMBL192690 1 5.51
CHEMBL364926 1 5.46
CHEMBL192664 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192227 IC50 = 81.0 nM 7.09
CHEMBL195277 IC50 = 93.0 nM 7.03
CHEMBL192825 IC50 = 120.0 nM 6.92
CHEMBL371801 IC50 = 130.0 nM 6.89
CHEMBL363344 IC50 = 140.0 nM 6.85
CHEMBL193004 IC50 = 140.0 nM 6.85
CHEMBL189789 IC50 = 230.0 nM 6.64
CHEMBL192634 IC50 = 340.0 nM 6.47
CHEMBL189792 IC50 = 480.0 nM 6.32
CHEMBL366228 IC50 = 650.0 nM 6.19
CHEMBL193311 IC50 = 730.0 nM 6.14
CHEMBL192185 IC50 = 750.0 nM 6.12
CHEMBL189970 IC50 = 1100.0 nM 5.96
CHEMBL189048 IC50 = 1100.0 nM 5.96
CHEMBL436559 CARIPORIDE IC50 = 1200.0 nM 5.92
CHEMBL194157 IC50 = 1300.0 nM 5.89
CHEMBL366227 IC50 = 1300.0 nM 5.89
CHEMBL372051 IC50 = 1400.0 nM 5.85
CHEMBL192601 IC50 = 1700.0 nM 5.77
CHEMBL192109 IC50 = 1700.0 nM 5.77
CHEMBL424813 IC50 = 2000.0 nM 5.70
CHEMBL425186 IC50 = 2300.0 nM 5.64
CHEMBL370954 IC50 = 2300.0 nM 5.64
CHEMBL195160 IC50 = 2400.0 nM 5.62
CHEMBL192635 IC50 = 2400.0 nM 5.62
CHEMBL373324 IC50 = 2600.0 nM 5.58
CHEMBL365153 IC50 = 3000.0 nM 5.52
CHEMBL192690 IC50 = 3100.0 nM 5.51
CHEMBL364926 IC50 = 3500.0 nM 5.46
CHEMBL192664 IC50 = 3700.0 nM 5.43
CHEMBL440029 IC50 = 4400.0 nM 5.36
CHEMBL190607 IC50 = 4400.0 nM 5.36
CHEMBL364735 IC50 = 6000.0 nM 5.22
CHEMBL195607 IC50 = 7400.0 nM 5.13
CHEMBL364681 IC50 = 7900.0 nM 5.10
CHEMBL439854 IC50 = 9400.0 nM 5.03
CHEMBL364923 IC50 = 15000.0 nM 4.82
CHEMBL192981 IC50 = 20000.0 nM 4.70
CHEMBL192250 IC50 = 27000.0 nM 4.57
CHEMBL192197 IC50 = 39000.0 nM 4.41
CHEMBL436322 IC50 > 30000.0 nM -
CHEMBL193121 IC50 > 30000.0 nM -
CHEMBL364731 IC50 > 30000.0 nM -
CHEMBL195608 IC50 > 30000.0 nM -
CHEMBL191456 IC50 > 30000.0 nM -
CHEMBL194156 IC50 > 30000.0 nM -
CHEMBL192283 IC50 > 30000.0 nM -
CHEMBL192284 IC50 > 30000.0 nM -
CHEMBL192151 IC50 > 30000.0 nM -
CHEMBL191671 IC50 > 30000.0 nM -