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Assay Detail

CHEMBL671265

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

Binding
Binding affinity towards human D4.2 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

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 7 6.96 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.19
CHEMBL42 CLOZAPINE 4.0 1 7.28
CHEMBL415300 ISOCLOZAPINE 1 6.96
CHEMBL72292 1 6.92
CHEMBL430798 1 6.82
CHEMBL70319 1 6.31
CHEMBL73589 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL IC50 = 6.5 nM 8.19
CHEMBL42 CLOZAPINE IC50 = 52.0 nM 7.28
CHEMBL415300 ISOCLOZAPINE IC50 = 110.0 nM 6.96
CHEMBL72292 IC50 = 120.0 nM 6.92
CHEMBL430798 IC50 = 150.0 nM 6.82
CHEMBL70319 IC50 = 490.0 nM 6.31
CHEMBL73589 IC50 = 570.0 nM 6.24