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Assay Detail

CHEMBL641153

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

Binding
Binding affinity was determined against alpha-2 adrenergic receptor of rat cerebral cortex using [3H]idazoxan as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for alpha-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled alpha 2-adrenoceptor vs the [3H]yohimbine-labeled site.
Clark RD, Berger J, Garg P, Weinhardt KK, Spedding M, Kilpatrick AT, Brown CM, MacKinnon AC.
J Med Chem (1990) 33 : 596 -600
PubMed 2153820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.28 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2448029 1 8.23
CHEMBL1203563 1 8.07
CHEMBL1203566 1 7.02
CHEMBL2448028 1 6.83
CHEMBL1203565 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2448029 Ki = 5.888 nM 8.23
CHEMBL1203563 Ki = 8.511 nM 8.07
CHEMBL1203566 Ki = 95.5 nM 7.02
CHEMBL2448028 Ki = 147.91 nM 6.83
CHEMBL1203565 Ki = 575.44 nM 6.24