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Assay Detail

CHEMBL617056

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

Binding
Inhibition of human 5-hydroxytryptamine 2A receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From hit to lead. Analyzing structure-profile relationships.
Poulain R, Horvath D, Bonnet B, Eckhoff C, Chapelain B, Bodinier MC, Déprez B.
J Med Chem (2001) 44 : 3391 -3401
PubMed 11585444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.13 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113956 1 6.64
CHEMBL116463 1 6.17
CHEMBL326263 1 6.15
CHEMBL325258 1 6.07
CHEMBL117537 1 6.02
CHEMBL115249 1 6.01
CHEMBL116735 1 5.99
CHEMBL325516 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113956 IC50 = 231.0 nM 6.64
CHEMBL116463 IC50 = 683.0 nM 6.17
CHEMBL326263 IC50 = 715.0 nM 6.15
CHEMBL325258 IC50 = 854.0 nM 6.07
CHEMBL117537 IC50 = 950.0 nM 6.02
CHEMBL115249 IC50 = 980.0 nM 6.01
CHEMBL116735 IC50 = 1030.0 nM 5.99
CHEMBL325516 IC50 = 1060.0 nM 5.97