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Assay Detail

CHEMBL822170

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

Functional
Tested for the alpha-2-adrenoceptor blocking activity by antagonism of clonidine-induced depression of the twitch responses of the field-stimulated prostatic portion of isolated rat vas deferens
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Vas deferens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Structure-activity relationships in 1,4-benzodioxan-related compounds. 4. Effect of aryl and alkyl substituents at position 3 on alpha-adrenoreceptor blocking activity.
Quaglia W, Pigini M, Tayebati SK, Piergentili A, Giannella M, Marucci G, Melchiorre C.
J Med Chem (1993) 36 : 1520 -1528
PubMed 8098772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 5.74 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10316 IDAZOXAN 3.0 1 8.01
CHEMBL39745 1 6.46
CHEMBL25554 1 6.39
CHEMBL286329 1 5.94
CHEMBL286673 1 5.76
CHEMBL289428 1 5.70
CHEMBL36738 1 4.87
CHEMBL286565 1 4.37
CHEMBL287935 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10316 IDAZOXAN Kd = 9.772 nM 8.01
CHEMBL39745 Kd = 346.74 nM 6.46
CHEMBL25554 Kd = 407.38 nM 6.39
CHEMBL286329 Kd = 1148.15 nM 5.94
CHEMBL286673 Kd = 1737.8 nM 5.76
CHEMBL289428 Kd = 1995.26 nM 5.70
CHEMBL36738 Kd = 13489.63 nM 4.87
CHEMBL286565 Kd = 42657.95 nM 4.37
CHEMBL287935 Kd = 66069.34 nM 4.18