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Assay Detail

CHEMBL648584

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

Binding
Alpha-1 adrenergic receptor binding affinity was evaluated by its ability to displace [3H]prazosin in rat brain synaptosomes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Preparation and in vitro biological evaluation of the enantiomers of the diydropyridine BMY 20014, a combination calcium and 1-adrenoreceptor antagonist
Lawson JE, Poindexter GS, Owens DA, Cavanagh RL, Goggins GD, Sarmiento J, Bleiberg BB, Weselcouch EO
Bioorg Med Chem Lett (1993) 3 : 561 -564
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.30 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 9.52
CHEMBL3301661 1 8.34
CHEMBL151910 1 7.89
CHEMBL2115538 1 7.44
CHEMBL2111260 1 -
CHEMBL2111202 1 -
CHEMBL193 NIFEDIPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Ki = 0.3 nM 9.52
CHEMBL3301661 Ki = 4.6 nM 8.34
CHEMBL151910 Ki = 13.0 nM 7.89
CHEMBL2115538 Ki = 36.0 nM 7.44
CHEMBL2111260 Ki > 1000.0 nM -
CHEMBL2111202 Ki > 1000.0 nM -
CHEMBL193 NIFEDIPINE Ki > 1000.0 nM -