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Assay Detail

CHEMBL617618

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

Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Stomach
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2B (CHEMBL323)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist.
Forbes IT, Jones GE, Murphy OE, Holland V, Baxter GS.
J Med Chem (1995) 38 : 855 -857
PubMed 7699699 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.53 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL323356 1 7.95
CHEMBL172269 1 7.82
CHEMBL536255 1 7.41
CHEMBL354951 1 7.33
CHEMBL422923 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL323356 Kd = 11.22 nM 7.95
CHEMBL172269 Kd = 15.14 nM 7.82
CHEMBL536255 Kd = 38.9 nM 7.41
CHEMBL354951 Kd = 46.77 nM 7.33
CHEMBL422923 Kd = 69.18 nM 7.16