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Assay Detail

CHEMBL694994

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

Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Histamine H2 receptor (CHEMBL2882)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
Lumma WC, Anderson PS, Baldwin JJ, Bolhofer WA, Habecker CN, Hirshfield JM, Pietruszkiewicz AM, Randall WC, Torchiana ML, Britcher SF, Clineschmidt BV, Denny GH, Hirschmann R, Hoffman MJ, Phillips BT, Streeter KB.
J Med Chem (1982) 25 : 207 -210
PubMed 6121913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.48 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306465 1 8.40
CHEMBL8982 1 8.20
CHEMBL63299 1 8.20
CHEMBL1790041 RANITIDINE 4.0 1 6.30
CHEMBL30 CIMETIDINE 4.0 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306465 Ki = 3.981 nM 8.40
CHEMBL8982 Ki = 6.31 nM 8.20
CHEMBL63299 Ki = 6.31 nM 8.20
CHEMBL1790041 RANITIDINE Ki = 501.19 nM 6.30
CHEMBL30 CIMETIDINE Ki = 501.19 nM 6.30