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Assay Detail

CHEMBL642052

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

Binding
In vitro ability to inhibit norepinephrine binding to alpha-2 adrenergic receptor of guinea pig vas deferens
8
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Vas deferens
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2095158)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
Marciniak G, Delgado A, Leclerc G, Velly J, Decker N, Schwartz J.
J Med Chem (1989) 32 : 1402 -1407
PubMed 2542561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 - -
Kd 1 6.70 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542812 1 6.70
CHEMBL553942 1 -
CHEMBL554235 1 -
CHEMBL554455 1 -
CHEMBL30911 1 -
CHEMBL3350238 2 -
CHEMBL284056 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542812 Kd = 199.53 nM 6.70
CHEMBL553942 IC50 >> 10000.0 nM -
CHEMBL554235 IC50 > 100000.0 nM -
CHEMBL554455 IC50 > 1000.0 nM -
CHEMBL30911 IC50 > 1000.0 nM -
CHEMBL3350238 IC50 >> 1000.0 nM -
CHEMBL3350238 IC50 > 100000.0 nM -
CHEMBL284056 IC50 >> 1000.0 nM -