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Assay Detail

CHEMBL645244

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

Binding
Binding affinity towards alpha-1 adrenergic receptor from rat brain membranes using [3H]prazosin as radioligand
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
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 7.15 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL73589 1 8.44
CHEMBL70319 1 8.15
CHEMBL42 CLOZAPINE 4.0 1 8.04
CHEMBL72292 1 7.92
CHEMBL54 HALOPERIDOL 4.0 1 7.75
CHEMBL430798 1 7.57
CHEMBL415300 ISOCLOZAPINE 1 7.19
CHEMBL72794 1 6.92
CHEMBL307163 1 6.80
CHEMBL73074 1 6.62
CHEMBL308090 1 6.58
CHEMBL70377 1 5.92
CHEMBL70609 1 5.06
CHEMBL310712 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL73589 IC50 = 3.6 nM 8.44
CHEMBL70319 IC50 = 7.1 nM 8.15
CHEMBL42 CLOZAPINE IC50 = 9.2 nM 8.04
CHEMBL72292 IC50 = 12.0 nM 7.92
CHEMBL54 HALOPERIDOL IC50 = 18.0 nM 7.75
CHEMBL430798 IC50 = 27.0 nM 7.57
CHEMBL415300 ISOCLOZAPINE IC50 = 64.0 nM 7.19
CHEMBL72794 IC50 = 120.0 nM 6.92
CHEMBL307163 IC50 = 160.0 nM 6.80
CHEMBL73074 IC50 = 240.0 nM 6.62
CHEMBL308090 IC50 = 260.0 nM 6.58
CHEMBL70377 IC50 = 1200.0 nM 5.92
CHEMBL70609 IC50 = 8700.0 nM 5.06
CHEMBL310712 IC50 > 1000.0 nM -