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Assay Detail

CHEMBL899067

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

Functional
Effect on acid secretion in rabbit intact gastric glands assessed as inhibition of [14C]dimethylaminopyridine accumulation
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Gastric gland
Confidence 1 — Organism
Curated By Autocuration

Target

Gastric gland (CHEMBL613448)
Type TISSUE
Organism Oryctolagus cuniculus

Publication

Preparation of tetrahydroimidazo[2,1-a]isoquinolines and their use as inhibitors of gastric acid secretion.
Palmer AM, Grobbel B, Brehm C, Zimmermann PJ, Buhr W, Feth MP, Holst HC, Simon WA.
Bioorg Med Chem (2007) 15 : 7647 -7660
PubMed 17881235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.71 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296482 1 7.20
CHEMBL392544 1 6.50
CHEMBL241801 1 6.40
CHEMBL442250 1 6.10
CHEMBL391485 1 6.00
CHEMBL238822 1 5.90
CHEMBL239034 1 5.70
CHEMBL391200 1 5.70
CHEMBL392749 1 5.20
CHEMBL240099 1 5.10
CHEMBL238839 1 5.10
CHEMBL240337 1 5.00
CHEMBL400204 1 5.00
CHEMBL392543 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296482 IC50 = 63.1 nM 7.20
CHEMBL392544 IC50 = 316.23 nM 6.50
CHEMBL241801 IC50 = 398.11 nM 6.40
CHEMBL442250 IC50 = 794.33 nM 6.10
CHEMBL391485 IC50 = 1000.0 nM 6.00
CHEMBL238822 IC50 = 1258.93 nM 5.90
CHEMBL239034 IC50 = 1995.26 nM 5.70
CHEMBL391200 IC50 = 1995.26 nM 5.70
CHEMBL392749 IC50 = 6309.57 nM 5.20
CHEMBL240099 IC50 = 7943.28 nM 5.10
CHEMBL238839 IC50 = 7943.28 nM 5.10
CHEMBL240337 IC50 = 10000.0 nM 5.00
CHEMBL400204 IC50 = 10000.0 nM 5.00
CHEMBL392543 IC50 = 10000.0 nM 5.00