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Assay Detail

CHEMBL816960

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

Functional
In vitro antagonistic activity against alpha-2 adrenergic receptor in isolated electrically stimulated rat vas deferens (clonidine-induced decrease in twitch height)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
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
Kd 12 7.44 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10316 IDAZOXAN 3.0 1 8.11
CHEMBL15245 YOHIMBINE 3.0 1 7.91
CHEMBL553031 NAPAMEZOLE HYDROCHLORIDE -1.0 1 7.76
CHEMBL545647 1 7.71
CHEMBL544001 1 7.67
CHEMBL553439 1 7.43
CHEMBL559829 1 7.35
CHEMBL544706 1 7.22
CHEMBL544701 1 7.19
CHEMBL545646 1 7.19
CHEMBL35345 1 6.92
CHEMBL6437 MIANSERIN 4.0 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10316 IDAZOXAN Kd = 7.762 nM 8.11
CHEMBL15245 YOHIMBINE Kd = 12.3 nM 7.91
CHEMBL553031 NAPAMEZOLE HYDROCHLORIDE Kd = 17.38 nM 7.76
CHEMBL545647 Kd = 19.5 nM 7.71
CHEMBL544001 Kd = 21.38 nM 7.67
CHEMBL553439 Kd = 37.15 nM 7.43
CHEMBL559829 Kd = 44.67 nM 7.35
CHEMBL544706 Kd = 60.26 nM 7.22
CHEMBL544701 Kd = 64.57 nM 7.19
CHEMBL545646 Kd = 64.57 nM 7.19
CHEMBL35345 Kd = 120.23 nM 6.92
CHEMBL6437 MIANSERIN Kd = 158.49 nM 6.80