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Assay Detail

CHEMBL895927

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Binding
Inhibition of human NHE1 expressed in PS120 cells
40
Total Activities
40
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 Intermediate

Target

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

Publication

3-Substituted-(5-arylfuran-2-ylcarbonyl)guanidines as NHE-1 inhibitors.
Lee S, Kim T, Lee BH, Yoo SE, Lee K, Yi KY.
Bioorg Med Chem Lett (2007) 17 : 1291 -1295
PubMed 17189690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.52 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392093 1 9.32
CHEMBL394633 1 8.10
CHEMBL395897 1 8.05
CHEMBL232748 1 8.00
CHEMBL395898 1 7.92
CHEMBL232940 1 7.82
CHEMBL397141 1 7.80
CHEMBL232974 1 7.62
CHEMBL396615 1 7.62
CHEMBL232744 1 7.14
CHEMBL233778 1 7.02
CHEMBL395667 1 6.92
CHEMBL233154 1 6.92
CHEMBL232355 1 6.92
CHEMBL232558 1 6.89
CHEMBL232124 1 6.82
CHEMBL231927 1 6.82
CHEMBL232975 1 6.64
CHEMBL398144 1 6.62
CHEMBL391171 1 6.39
CHEMBL392311 1 6.32
CHEMBL441127 1 6.17
CHEMBL231929 1 6.11
CHEMBL396616 1 6.09
CHEMBL395900 1 6.09
CHEMBL231926 1 5.92
CHEMBL436559 CARIPORIDE 2.0 1 5.92
CHEMBL398143 1 5.64
CHEMBL231784 1 5.52
CHEMBL233354 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392093 IC50 = 0.48 nM 9.32
CHEMBL394633 IC50 = 8.0 nM 8.10
CHEMBL395897 IC50 = 9.0 nM 8.05
CHEMBL232748 IC50 = 10.0 nM 8.00
CHEMBL395898 IC50 = 12.0 nM 7.92
CHEMBL232940 IC50 = 15.0 nM 7.82
CHEMBL397141 IC50 = 16.0 nM 7.80
CHEMBL232974 IC50 = 24.0 nM 7.62
CHEMBL396615 IC50 = 24.0 nM 7.62
CHEMBL232744 IC50 = 72.0 nM 7.14
CHEMBL233778 IC50 = 96.0 nM 7.02
CHEMBL395667 IC50 = 120.0 nM 6.92
CHEMBL232355 IC50 = 120.0 nM 6.92
CHEMBL233154 IC50 = 120.0 nM 6.92
CHEMBL232558 IC50 = 130.0 nM 6.89
CHEMBL232124 IC50 = 150.0 nM 6.82
CHEMBL231927 IC50 = 150.0 nM 6.82
CHEMBL232975 IC50 = 230.0 nM 6.64
CHEMBL398144 IC50 = 240.0 nM 6.62
CHEMBL391171 IC50 = 410.0 nM 6.39
CHEMBL392311 IC50 = 480.0 nM 6.32
CHEMBL441127 IC50 = 680.0 nM 6.17
CHEMBL231929 IC50 = 770.0 nM 6.11
CHEMBL396616 IC50 = 820.0 nM 6.09
CHEMBL395900 IC50 = 820.0 nM 6.09
CHEMBL231926 IC50 = 1200.0 nM 5.92
CHEMBL436559 CARIPORIDE IC50 = 1200.0 nM 5.92
CHEMBL398143 IC50 = 2300.0 nM 5.64
CHEMBL231784 IC50 = 3000.0 nM 5.52
CHEMBL233354 IC50 = 4500.0 nM 5.35
CHEMBL233779 IC50 = 5100.0 nM 5.29
CHEMBL232976 IC50 = 5600.0 nM 5.25
CHEMBL233353 IC50 = 6200.0 nM 5.21
CHEMBL443584 IC50 = 14000.0 nM 4.85
CHEMBL233352 IC50 = 14000.0 nM 4.85
CHEMBL233780 IC50 = 16000.0 nM 4.80
CHEMBL232180 IC50 = 33000.0 nM 4.48
CHEMBL232179 IC50 > 30000.0 nM -
CHEMBL395395 IC50 > 30000.0 nM -
CHEMBL231982 IC50 > 30000.0 nM -