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Assay Detail

CHEMBL648807

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

Functional
Antagonistic activity against postsynaptic alpha-1 adrenergic receptor in rabbit pulmonary artery using l-norepinephrine as agonist
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Pulmonary artery
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
Vizi ES, Toth I, Somogyi GT, Szabo L, Harsing LG, Szantay C.
J Med Chem (1987) 30 : 1355 -1359
PubMed 2886664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 6.45 8.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 8.76
CHEMBL597 PHENTOLAMINE 4.0 1 7.82
CHEMBL10316 IDAZOXAN 3.0 1 6.85
CHEMBL15245 YOHIMBINE 3.0 1 6.83
CHEMBL281708 1 6.19
CHEMBL28531 1 5.39
CHEMBL29379 1 4.98
CHEMBL282636 1 4.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Kd = 1.738 nM 8.76
CHEMBL597 PHENTOLAMINE Kd = 15.14 nM 7.82
CHEMBL10316 IDAZOXAN Kd = 141.25 nM 6.85
CHEMBL15245 YOHIMBINE Kd = 147.91 nM 6.83
CHEMBL281708 Kd = 645.65 nM 6.19
CHEMBL28531 Kd = 4073.8 nM 5.39
CHEMBL29379 Kd = 10471.29 nM 4.98
CHEMBL282636 Kd = 15488.17 nM 4.81