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Assay Detail

CHEMBL871941

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

Binding
In vitro inhibition of H+/K+ ATPase activity was determined in gastric vesicles of pig using ATPase assay with pH 7
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Stomach
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Potassium-transporting ATPase alpha chain 1 (CHEMBL3919)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogues of 4-(arylamino)quinolines.
Brown TH, Ife RJ, Keeling DJ, Laing SM, Leach CA, Parsons ME, Price CA, Reavill DR, Wiggall KJ.
J Med Chem (1990) 33 : 527 -533
PubMed 2153816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.82 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47529 1 7.00
CHEMBL358421 1 6.77
CHEMBL346188 1 6.39
CHEMBL357193 1 6.38
CHEMBL440726 1 6.28
CHEMBL298695 1 6.19
CHEMBL151251 1 6.18
CHEMBL357596 1 6.12
CHEMBL95108 1 6.07
CHEMBL357510 1 6.00
CHEMBL153811 1 5.96
CHEMBL356892 1 5.89
CHEMBL149052 1 5.82
CHEMBL147246 1 5.80
CHEMBL151252 1 5.62
CHEMBL449033 1 5.54
CHEMBL146903 1 5.51
CHEMBL357274 1 5.01
CHEMBL151290 1 4.96
CHEMBL356246 1 4.66
CHEMBL443295 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47529 IC50 = 101.0 nM 7.00
CHEMBL358421 IC50 = 170.0 nM 6.77
CHEMBL346188 IC50 = 410.0 nM 6.39
CHEMBL357193 IC50 = 420.0 nM 6.38
CHEMBL440726 IC50 = 530.0 nM 6.28
CHEMBL298695 IC50 = 640.0 nM 6.19
CHEMBL151251 IC50 = 660.0 nM 6.18
CHEMBL357596 IC50 = 750.0 nM 6.12
CHEMBL95108 IC50 = 850.0 nM 6.07
CHEMBL357510 IC50 = 1000.0 nM 6.00
CHEMBL153811 IC50 = 1100.0 nM 5.96
CHEMBL356892 IC50 = 1300.0 nM 5.89
CHEMBL149052 IC50 = 1500.0 nM 5.82
CHEMBL147246 IC50 = 1600.0 nM 5.80
CHEMBL151252 IC50 = 2400.0 nM 5.62
CHEMBL449033 IC50 = 2900.0 nM 5.54
CHEMBL146903 IC50 = 3100.0 nM 5.51
CHEMBL357274 IC50 = 9800.0 nM 5.01
CHEMBL151290 IC50 = 11000.0 nM 4.96
CHEMBL356246 IC50 = 22000.0 nM 4.66
CHEMBL443295 IC50 = 69000.0 nM 4.16