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Assay Detail

CHEMBL877456

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

Binding
Binding affinity towards Alpha-1 adrenergic receptor using 7-methoxy-[3H]-prazosin as radioligand in rat frontal cortex tissue
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Frontal cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.
Egle I, Barriault N, Bordeleau M, Drage J, Dube L, Peragine J, Mazzocco L, Arora J, Jarvie K, Tehim A.
Bioorg Med Chem Lett (2004) 14 : 4847 -4850
PubMed 15341937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.54 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426062 1 6.85
CHEMBL361035 1 6.80
CHEMBL366304 1 6.77
CHEMBL187113 1 6.77
CHEMBL186558 1 6.48
CHEMBL364782 1 6.21
CHEMBL360424 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426062 Ki = 140.0 nM 6.85
CHEMBL361035 Ki = 160.0 nM 6.80
CHEMBL366304 Ki = 170.0 nM 6.77
CHEMBL187113 Ki = 170.0 nM 6.77
CHEMBL186558 Ki = 330.0 nM 6.48
CHEMBL364782 Ki = 610.0 nM 6.21
CHEMBL360424 Ki = 1200.0 nM 5.92