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Assay Detail

CHEMBL816957

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

Binding
Ability to displace [3H]clonidine from alpha-2 adrenergic receptor in rat brain homogenates in vitro
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives.
Wentland MP, Bailey DM, Alexander EJ, Castaldi MJ, Ferrari RA, Haubrich DR, Luttinger DA, Perrone MH.
J Med Chem (1987) 30 : 1482 -1489
PubMed 3039138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.22 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559829 1 8.18
CHEMBL545647 1 8.16
CHEMBL10316 IDAZOXAN 3.0 1 8.00
CHEMBL545646 1 7.92
CHEMBL553031 NAPAMEZOLE HYDROCHLORIDE -1.0 1 7.64
CHEMBL553439 1 7.50
CHEMBL544001 1 7.32
CHEMBL544701 1 7.12
CHEMBL6437 MIANSERIN 4.0 1 7.12
CHEMBL15245 YOHIMBINE 3.0 1 7.11
CHEMBL35345 1 7.06
CHEMBL544706 1 6.87
CHEMBL544704 1 6.48
CHEMBL544705 1 6.40
CHEMBL553103 1 6.36
CHEMBL553368 1 6.26
CHEMBL543535 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559829 Ki = 6.6 nM 8.18
CHEMBL545647 Ki = 6.9 nM 8.16
CHEMBL10316 IDAZOXAN Ki = 10.0 nM 8.00
CHEMBL545646 Ki = 12.0 nM 7.92
CHEMBL553031 NAPAMEZOLE HYDROCHLORIDE Ki = 23.0 nM 7.64
CHEMBL553439 Ki = 32.0 nM 7.50
CHEMBL544001 Ki = 48.0 nM 7.32
CHEMBL544701 Ki = 76.0 nM 7.12
CHEMBL6437 MIANSERIN Ki = 76.0 nM 7.12
CHEMBL15245 YOHIMBINE Ki = 78.0 nM 7.11
CHEMBL35345 Ki = 88.0 nM 7.06
CHEMBL544706 Ki = 135.0 nM 6.87
CHEMBL544704 Ki = 334.0 nM 6.48
CHEMBL544705 Ki = 401.0 nM 6.40
CHEMBL553103 Ki = 436.0 nM 6.36
CHEMBL553368 Ki = 548.0 nM 6.26
CHEMBL543535 Ki > 800.0 nM -