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Assay Detail

CHEMBL648046

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

Binding
In vitro binding affinity against alpha-1 adrenergic receptor of rat cerebral cortex using [3H]prazosin as radioligand.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of a new model of arylpiperazines. 2. Three-dimensional quantitative structure-activity relationships of hydantoin-phenylpiperazine derivatives with affinity for 5-HT1A and alpha 1 receptors. A comparison of CoMFA models.
López-Rodríguez ML, Rosado ML, Benhamú B, Morcillo MJ, Fernández E, Schaper KJ.
J Med Chem (1997) 40 : 1648 -1656
PubMed 9171874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.99 6.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297844 1 6.87
CHEMBL297887 1 6.54
CHEMBL46471 1 6.30
CHEMBL46672 1 6.06
CHEMBL42881 1 5.92
CHEMBL42654 1 5.68
CHEMBL46470 1 5.59
CHEMBL295244 1 5.48
CHEMBL430567 1 5.48
CHEMBL295527 1 -
CHEMBL46862 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297844 Ki = 135.0 nM 6.87
CHEMBL297887 Ki = 292.0 nM 6.54
CHEMBL46471 Ki = 500.0 nM 6.30
CHEMBL46672 Ki = 869.0 nM 6.06
CHEMBL42881 Ki = 1193.0 nM 5.92
CHEMBL42654 Ki = 2075.0 nM 5.68
CHEMBL46470 Ki = 2588.0 nM 5.59
CHEMBL295244 Ki = 3296.0 nM 5.48
CHEMBL430567 Ki = 3296.0 nM 5.48
CHEMBL295527 Ki = 260000.0 nM -
CHEMBL46862 Ki = 260000.0 nM -