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Assay Detail

CHEMBL696490

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

Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Histamine H2-receptor agonists. Synthesis, in vitro pharmacology, and qualitative structure-activity relationships of substituted 4- and 5-(2-aminoethyl)thiazoles.
Eriks JC, van der Goot H, Sterk GJ, Timmerman H.
J Med Chem (1992) 35 : 3239 -3246
PubMed 1507209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 4.72 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL554964 1 5.30
CHEMBL111215 1 4.82
CHEMBL12344 DIMAPRIT 1 4.58
CHEMBL90 HISTAMINE 4.0 1 4.16
CHEMBL324864 1 -
CHEMBL540311 1 -
CHEMBL553981 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL554964 Kd = 5011.87 nM 5.30
CHEMBL111215 Kd = 15135.61 nM 4.82
CHEMBL12344 DIMAPRIT Kd = 26302.68 nM 4.58
CHEMBL90 HISTAMINE Kd = 69183.1 nM 4.16
CHEMBL324864 Kd = 109647.82 nM -
CHEMBL540311 Kd = 354813.39 nM -
CHEMBL553981 Kd = 173780.08 nM -