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Assay Detail

CHEMBL856312

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

Binding
Inhibition of human NHE2 expressed in Ap1 cell line
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Ap1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium/hydrogen exchanger 2 (CHEMBL3133)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of 5-aryl-4-(4-(5-methyl-1H-imidazol-4-yl)piperidin-1-yl)pyrimidine analogs as potent, highly selective, and orally bioavailable NHE-1 inhibitors.
Atwal KS, O'Neil SV, Ahmad S, Doweyko L, Kirby M, Dorso CR, Chandrasena G, Chen BC, Zhao R, Zahler R.
Bioorg Med Chem Lett (2006) 16 : 4796 -4799
PubMed 16870436 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.68 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217698 1 5.05
CHEMBL64360 ENIPORIDE 2.0 1 4.77
CHEMBL436559 CARIPORIDE 2.0 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217698 IC50 = 9000.0 nM 5.05
CHEMBL64360 ENIPORIDE IC50 = 17000.0 nM 4.77
CHEMBL436559 CARIPORIDE IC50 = 62000.0 nM 4.21