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Assay Detail

CHEMBL746895

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Functional
In vitro concentration required to inhibit NHE-1 mediated intracellular maximal pH recovery by 50%
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility.
Guzman-Perez A, Wester RT, Allen MC, Brown JA, Buchholz AR, Cook ER, Day WW, Hamanaka ES, Kennedy SP, Knight DR, Kowalczyk PJ, Marala RB, Mularski CJ, Novomisle WA, Ruggeri RB, Tracey WR, Hill RJ.
Bioorg Med Chem Lett (2001) 11 : 803 -807
PubMed 11277524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.53 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355862 ZONIPORIDE 2.0 1 7.23
CHEMBL64360 ENIPORIDE 2.0 1 6.85
CHEMBL354137 1 6.80
CHEMBL355071 1 6.46
CHEMBL436559 CARIPORIDE 2.0 1 6.25
CHEMBL352933 1 6.08
CHEMBL167495 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355862 ZONIPORIDE IC50 = 59.0 nM 7.23
CHEMBL64360 ENIPORIDE IC50 = 140.0 nM 6.85
CHEMBL354137 IC50 = 160.0 nM 6.80
CHEMBL355071 IC50 = 350.0 nM 6.46
CHEMBL436559 CARIPORIDE IC50 = 560.0 nM 6.25
CHEMBL352933 IC50 = 830.0 nM 6.08
CHEMBL167495 IC50 = 860.0 nM 6.07