Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3767682

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

Binding
Antagonist activity at 5HT2A receptor in Sprague-Dawley rat ileum assessed as inhibition of 5-HT-induced contraction
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.
Fiorino F, Ciano A, Magli E, Severino B, Corvino A, Perissutti E, Frecentese F, Di Vaio P, Izzo AA, Capasso R, Massarelli P, Nencini C, Rossi I, Kędzierska E, Orzelska-Gòrka J, Bielenica A, Santagada V, Caliendo G.
Eur J Med Chem (2016) 110 : 133 -150
PubMed 26820556 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.66 7.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763558 1 7.91
CHEMBL3765122 1 5.93
CHEMBL3764420 1 5.79
CHEMBL3763474 1 5.37
CHEMBL3765231 1 5.01
CHEMBL3765471 1 4.99
CHEMBL3764341 1 4.63
CHEMBL3763812 1 -
CHEMBL3764080 1 -
CHEMBL3764177 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763558 IC50 = 12.2 nM 7.91
CHEMBL3765122 IC50 = 1170.0 nM 5.93
CHEMBL3764420 IC50 = 1640.0 nM 5.79
CHEMBL3763474 IC50 = 4290.0 nM 5.37
CHEMBL3765231 IC50 = 9830.0 nM 5.01
CHEMBL3765471 IC50 = 10300.0 nM 4.99
CHEMBL3764341 IC50 = 23300.0 nM 4.63
CHEMBL3763812 IC50 - -
CHEMBL3764080 IC50 - -
CHEMBL3764177 IC50 - -