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Assay Detail

CHEMBL873183

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

Binding
Compound was evaluated for alpha adrenergic binding affinity towards Alpha-2 adrenergic receptor of rat brain
7
Total Activities
7
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

Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors.
Macchia B, Balsamo A, Breschi MC, Lapucci A, Lucacchini A, Macchia F, Manera C, Martinelli A, Martini C, Martinotti E.
J Med Chem (1992) 35 : 1009 -1018
PubMed 1313109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.22 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1437 NOREPINEPHRINE 4.0 1 8.32
CHEMBL7681 1 7.58
CHEMBL7278 1 6.30
CHEMBL6898 1 5.80
CHEMBL7160 1 5.54
CHEMBL268881 1 5.29
CHEMBL434 ISOPROTERENOL 4.0 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1437 NOREPINEPHRINE Ki = 4.8 nM 8.32
CHEMBL7681 Ki = 26.0 nM 7.58
CHEMBL7278 Ki = 500.0 nM 6.30
CHEMBL6898 Ki = 1570.0 nM 5.80
CHEMBL7160 Ki = 2900.0 nM 5.54
CHEMBL268881 Ki = 5100.0 nM 5.29
CHEMBL434 ISOPROTERENOL Ki = 21000.0 nM 4.68