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Assay Detail

CHEMBL644783

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

Binding
Binding affinity against Alpha-1 adrenergic receptor, activity is expressed as IC50 values
15
Total Activities
11
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

Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.
Bøgesø KP, Arnt J, Frederiksen K, Hansen HO, Hyttel J, Pedersen H.
J Med Chem (1995) 38 : 4380 -4392
PubMed 7473566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.78 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL136630 2 8.41
CHEMBL136722 1 8.36
CHEMBL136235 2 8.33
CHEMBL42 CLOZAPINE 4.0 1 8.04
CHEMBL137960 2 8.00
CHEMBL136683 2 7.92
CHEMBL136226 1 7.85
CHEMBL137536 1 7.82
CHEMBL343282 1 7.60
CHEMBL136891 1 7.03
CHEMBL136190 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL136630 IC50 = 3.9 nM 8.41
CHEMBL136722 IC50 = 4.4 nM 8.36
CHEMBL136235 IC50 = 4.7 nM 8.33
CHEMBL136630 IC50 = 4.9 nM 8.31
CHEMBL42 CLOZAPINE IC50 = 9.2 nM 8.04
CHEMBL137960 IC50 = 10.0 nM 8.00
CHEMBL136235 IC50 = 12.0 nM 7.92
CHEMBL136683 IC50 = 12.0 nM 7.92
CHEMBL136226 IC50 = 14.0 nM 7.85
CHEMBL137536 IC50 = 15.0 nM 7.82
CHEMBL137960 IC50 = 23.0 nM 7.64
CHEMBL343282 IC50 = 25.0 nM 7.60
CHEMBL136683 IC50 = 39.0 nM 7.41
CHEMBL136891 IC50 = 94.0 nM 7.03
CHEMBL136190 IC50 = 970.0 nM 6.01