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Assay Detail

CHEMBL643927

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

Binding
The compound was evaluated for the inhibition of [3H]rauwolscine binding to alpha-2-adrenergic receptor from rat cortex
5
Total Activities
5
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-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Conformationally defined adrenergic agents. 2. Catechol imidazoline derivatives: biological effects at alpha 1 and alpha 2 adrenergic receptors.
DeBernardis JF, Kyncl JJ, Basha FZ, Arendsen DL, Martin YC, Winn M, Kerkman DJ.
J Med Chem (1986) 29 : 463 -467
PubMed 2870187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.36 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL545092 1 8.48
CHEMBL543684 1 8.15
CHEMBL1437 NOREPINEPHRINE 4.0 1 7.48
CHEMBL544627 1 7.31
CHEMBL554004 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL545092 IC50 = 3.3 nM 8.48
CHEMBL543684 IC50 = 7.0 nM 8.15
CHEMBL1437 NOREPINEPHRINE IC50 = 33.0 nM 7.48
CHEMBL544627 IC50 = 49.0 nM 7.31
CHEMBL554004 IC50 = 4200.0 nM 5.38