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Assay Detail

CHEMBL838690

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

Binding
Binding affinity against alpha 2 adrenergic receptor in rat cortex using [3H]clonidine as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.
Grunewald GL, Romero FA, Seim MR, Criscione KR, Deupree JD, Spackman CC, Bylund DB.
Bioorg Med Chem Lett (2005) 15 : 1143 -1147
PubMed 15686930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.08 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41487 1 6.00
CHEMBL361749 1 5.89
CHEMBL185233 1 5.32
CHEMBL59441 1 4.72
CHEMBL182970 1 4.34
CHEMBL182774 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41487 Ki = 1000.0 nM 6.00
CHEMBL361749 Ki = 1300.0 nM 5.89
CHEMBL185233 Ki = 4800.0 nM 5.32
CHEMBL59441 Ki = 19000.0 nM 4.72
CHEMBL182970 Ki = 46000.0 nM 4.34
CHEMBL182774 Ki = 59000.0 nM 4.23