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Assay Detail

CHEMBL617656

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

Binding
Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL324)
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 14 6.99 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415300 ISOCLOZAPINE 1 8.54
CHEMBL42 CLOZAPINE 4.0 1 7.96
CHEMBL70319 1 7.89
CHEMBL72794 1 7.68
CHEMBL72292 1 7.47
CHEMBL308090 1 7.09
CHEMBL73074 1 7.07
CHEMBL430798 1 7.00
CHEMBL73589 1 6.55
CHEMBL70377 1 6.36
CHEMBL310712 1 6.21
CHEMBL307163 1 5.92
CHEMBL70609 1 5.13
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415300 ISOCLOZAPINE IC50 = 2.9 nM 8.54
CHEMBL42 CLOZAPINE IC50 = 11.0 nM 7.96
CHEMBL70319 IC50 = 13.0 nM 7.89
CHEMBL72794 IC50 = 21.0 nM 7.68
CHEMBL72292 IC50 = 34.0 nM 7.47
CHEMBL308090 IC50 = 81.0 nM 7.09
CHEMBL73074 IC50 = 86.0 nM 7.07
CHEMBL430798 IC50 = 100.0 nM 7.00
CHEMBL73589 IC50 = 280.0 nM 6.55
CHEMBL70377 IC50 = 440.0 nM 6.36
CHEMBL310712 IC50 = 620.0 nM 6.21
CHEMBL307163 IC50 = 1200.0 nM 5.92
CHEMBL70609 IC50 = 7400.0 nM 5.13
CHEMBL54 HALOPERIDOL IC50 > 1000.0 nM -