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Assay Detail

CHEMBL650237

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

Binding
Displacement of [3H]idazoxan from alpha-2 adrenergic receptor from rat brain cerebral cortex.
9
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
Welbourn AP, Chapleo CB, Lane AC, Myers PL, Roach AG, Smith CF, Stillings MR, Tulloch IF.
J Med Chem (1986) 29 : 2000 -2003
PubMed 2876101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.71 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10332 3 9.44
CHEMBL61325 3 8.62
CHEMBL61234 3 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10332 Ki = 0.36 nM 9.44
CHEMBL10332 Ki = 0.8 nM 9.10
CHEMBL61325 Ki = 2.4 nM 8.62
CHEMBL61325 Ki = 4.4 nM 8.36
CHEMBL61234 Ki = 8.0 nM 8.10
CHEMBL61234 Ki = 16.3 nM 7.79
CHEMBL10332 Ki = 256.0 nM 6.59
CHEMBL61325 Ki = 487.0 nM 6.31
CHEMBL61234 Ki = 8734.0 nM 5.06