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Assay Detail

CHEMBL765030

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

Functional
Inhibition of [14C]aminopyrine (AP) accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Potassium-transporting ATPase (CHEMBL2095173)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Nicotinamide derivatives as a new class of gastric H+/K(+)-ATPase inhibitors. 1. Synthesis and structure-activity relationships of N-substituted 2-(benzhydryl- and benzylsulfinyl)nicotinamides.
Terauchi H, Tanitame A, Tada K, Nakamura K, Seto Y, Nishikawa Y.
J Med Chem (1997) 40 : 313 -321
PubMed 9022797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.71 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1503 OMEPRAZOLE 4.0 1 6.43
CHEMBL110960 1 6.40
CHEMBL108610 1 6.35
CHEMBL108536 1 6.34
CHEMBL323189 1 6.23
CHEMBL108285 1 5.92
CHEMBL111351 1 5.82
CHEMBL325803 1 5.77
CHEMBL109629 1 5.72
CHEMBL322809 1 4.78
CHEMBL111282 1 4.58
CHEMBL320710 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1503 OMEPRAZOLE IC50 = 370.0 nM 6.43
CHEMBL110960 IC50 = 400.0 nM 6.40
CHEMBL108610 IC50 = 450.0 nM 6.35
CHEMBL108536 IC50 = 460.0 nM 6.34
CHEMBL323189 IC50 = 590.0 nM 6.23
CHEMBL108285 IC50 = 1200.0 nM 5.92
CHEMBL111351 IC50 = 1500.0 nM 5.82
CHEMBL325803 IC50 = 1700.0 nM 5.77
CHEMBL109629 IC50 = 1900.0 nM 5.72
CHEMBL322809 IC50 = 16600.0 nM 4.78
CHEMBL111282 IC50 = 26000.0 nM 4.58
CHEMBL320710 IC50 = 59000.0 nM 4.23