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Assay Detail

CHEMBL640537

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

Functional
Antagonistic affinity against native rat cortex Alpha-2 adrenergic receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
Minarini A, Budriesi R, Chiarini A, Leonardi A, Melchiorre C.
Bioorg Med Chem Lett (1998) 8 : 1353 -1358
PubMed 9871765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.43 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27013 1 7.00
CHEMBL2 PRAZOSIN 4.0 1 6.80
CHEMBL29591 1 6.23
CHEMBL423294 CYCLAZOSIN 1 6.13
CHEMBL543741 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27013 Ki = 100.0 nM 7.00
CHEMBL2 PRAZOSIN Ki = 158.49 nM 6.80
CHEMBL29591 Ki = 588.84 nM 6.23
CHEMBL423294 CYCLAZOSIN Ki = 741.31 nM 6.13
CHEMBL543741 Ki = 1047.13 nM 5.98