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Assay Detail

CHEMBL793161

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

Functional
Compound was tested for alpha-adrenoceptor blocking activity by its ability to antagonize norepinephrine contraction in the rat thoracic aorta
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Thoracic aorta
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Pyrimidine derivatives. 4. Synthesis and antihypertensive activity of 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives.
Sekiya T, Hiranuma H, Hata S, Mizogami S, Hanazuka M, Yamada S.
J Med Chem (1983) 26 : 411 -416
PubMed 6131135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 9.20 10.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1558 PRAZOSIN HYDROCHLORIDE 4.0 1 10.29
CHEMBL538288 1 9.85
CHEMBL268768 1 9.14
CHEMBL135797 1 8.66
CHEMBL597 PHENTOLAMINE 4.0 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1558 PRAZOSIN HYDROCHLORIDE Kd = 0.05129 nM 10.29
CHEMBL538288 Kd = 0.1413 nM 9.85
CHEMBL268768 Kd = 0.7244 nM 9.14
CHEMBL135797 Kd = 2.188 nM 8.66
CHEMBL597 PHENTOLAMINE Kd = 8.511 nM 8.07