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Assay Detail

CHEMBL617249

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

Binding
Binding affinity towards 5-hydroxytryptamine 2 receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor.
Hibert MF, Gittos MW, Middlemiss DN, Mir AK, Fozard JR.
J Med Chem (1988) 31 : 1087 -1093
PubMed 3373482 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.34 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12311 1 6.80
CHEMBL12129 1 6.70
CHEMBL12152 1 6.20
CHEMBL12124 1 6.10
CHEMBL11787 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12311 IC50 = 158.49 nM 6.80
CHEMBL12129 IC50 = 199.53 nM 6.70
CHEMBL12152 IC50 = 630.96 nM 6.20
CHEMBL12124 IC50 = 794.33 nM 6.10
CHEMBL11787 IC50 = 1258.93 nM 5.90