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Assay Detail

CHEMBL642135

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

Functional
Alpha-2 adrenergic receptor antagonistic activity in rat vas deferens vs clonidin
15
Total Activities
15
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

Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
Hlasta DJ, Luttinger D, Perrone MH, Silbernagel MJ, Ward SJ, Haubrich DR.
J Med Chem (1987) 30 : 1555 -1562
PubMed 2887657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 15 7.90 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36616 1 8.91
CHEMBL38788 1 8.76
CHEMBL38829 1 8.65
CHEMBL39254 1 8.56
CHEMBL41720 1 8.45
CHEMBL38406 1 8.13
CHEMBL10316 IDAZOXAN 3.0 1 8.11
CHEMBL37352 1 8.03
CHEMBL41861 1 8.00
CHEMBL289153 1 7.93
CHEMBL289098 1 7.59
CHEMBL41803 1 6.96
CHEMBL288337 1 6.60
CHEMBL38790 1 5.88
CHEMBL41305 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36616 Kd = 1.23 nM 8.91
CHEMBL38788 Kd = 1.738 nM 8.76
CHEMBL38829 Kd = 2.239 nM 8.65
CHEMBL39254 Kd = 2.754 nM 8.56
CHEMBL41720 Kd = 3.548 nM 8.45
CHEMBL38406 Kd = 7.413 nM 8.13
CHEMBL10316 IDAZOXAN Kd = 7.762 nM 8.11
CHEMBL37352 Kd = 9.333 nM 8.03
CHEMBL41861 Kd = 10.0 nM 8.00
CHEMBL289153 Kd = 11.75 nM 7.93
CHEMBL289098 Kd = 25.7 nM 7.59
CHEMBL41803 Kd = 109.65 nM 6.96
CHEMBL288337 Kd = 251.19 nM 6.60
CHEMBL38790 Kd = 1318.26 nM 5.88
CHEMBL41305 Kd > 1000.0 nM -