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Assay Detail

CHEMBL648049

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

Binding
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-2A adrenergic receptor (CHEMBL4744)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.
Saari WS, Halczenko W, Randall WC, Lotti VJ.
J Med Chem (1983) 26 : 1769 -1772
PubMed 6139481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.12 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL597 PHENTOLAMINE 4.0 1 8.68
CHEMBL51131 1 8.25
CHEMBL51358 1 7.26
CHEMBL300628 1 6.82
CHEMBL300053 1 6.64
CHEMBL49953 1 6.52
CHEMBL51479 1 6.42
CHEMBL541208 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL597 PHENTOLAMINE Ki = 2.1 nM 8.68
CHEMBL51131 Ki = 5.6 nM 8.25
CHEMBL51358 Ki = 55.0 nM 7.26
CHEMBL300628 Ki = 150.0 nM 6.82
CHEMBL300053 Ki = 230.0 nM 6.64
CHEMBL49953 Ki = 300.0 nM 6.52
CHEMBL51479 Ki = 380.0 nM 6.42
CHEMBL541208 Ki = 424.0 nM 6.37