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Assay Detail

CHEMBL5625417

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Binding
Inhibition of human NHE-1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pharmacological activity and mechanism of pyrazines.
Hou W, Dai W, Huang H, Liu SL, Liu J, Huang LJ, Huang XH, Zeng JL, Gan ZW, Zhang ZY, Lan JX.
Eur J Med Chem (2023) 258 : 115544 -115544
PubMed 37300915 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.65 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL465179 1 10.80
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE 1 9.72
CHEMBL517986 5-(N-ETHYL-N-ISOPROPYL)AMILORIDE 1 8.43
CHEMBL64360 ENIPORIDE 2.0 1 -
CHEMBL436559 CARIPORIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL465179 IC50 = 0.016 nM 10.80
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE IC50 = 0.19 nM 9.72
CHEMBL517986 5-(N-ETHYL-N-ISOPROPYL)AMILORIDE IC50 = 3.7 nM 8.43
CHEMBL64360 ENIPORIDE IC50 = 0.004 nM -
CHEMBL436559 CARIPORIDE IC50 = 0.03 nM -