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Assay Detail

CHEMBL617605

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

Binding
Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
Liao Y, Venhuis BJ, Rodenhuis N, Timmerman W, Wikström H, Meier E, Bartoszyk GD, Böttcher H, Seyfried CA, Sundell S.
J Med Chem (1999) 42 : 2235 -2244
PubMed 10377229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.10 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL831 LOXAPINE 4.0 1 8.22
CHEMBL72794 1 7.92
CHEMBL415300 ISOCLOZAPINE 1 7.92
CHEMBL42 CLOZAPINE 4.0 1 7.92
CHEMBL70319 1 7.64
CHEMBL308090 1 7.46
CHEMBL72292 1 7.37
CHEMBL430798 1 7.32
CHEMBL54 HALOPERIDOL 4.0 1 7.26
CHEMBL73589 1 6.96
CHEMBL73074 1 6.80
CHEMBL306474 1 6.64
CHEMBL70377 1 6.51
CHEMBL310712 1 6.26
CHEMBL307163 1 6.06
CHEMBL70609 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL831 LOXAPINE IC50 = 6.0 nM 8.22
CHEMBL72794 IC50 = 12.0 nM 7.92
CHEMBL415300 ISOCLOZAPINE IC50 = 12.0 nM 7.92
CHEMBL42 CLOZAPINE IC50 = 12.0 nM 7.92
CHEMBL70319 IC50 = 23.0 nM 7.64
CHEMBL308090 IC50 = 35.0 nM 7.46
CHEMBL72292 IC50 = 43.0 nM 7.37
CHEMBL430798 IC50 = 48.0 nM 7.32
CHEMBL54 HALOPERIDOL IC50 = 55.0 nM 7.26
CHEMBL73589 IC50 = 110.0 nM 6.96
CHEMBL73074 IC50 = 160.0 nM 6.80
CHEMBL306474 IC50 = 230.0 nM 6.64
CHEMBL70377 IC50 = 310.0 nM 6.51
CHEMBL310712 IC50 = 550.0 nM 6.26
CHEMBL307163 IC50 = 880.0 nM 6.06
CHEMBL70609 IC50 = 4900.0 nM 5.31