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Assay Detail

CHEMBL3294121

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

Functional
Vasorelaxant activity in Wistar rat endothelium-denuded thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 1 — Organism
Curated By Autocuration

Target

Aorta (CHEMBL613606)
Type TISSUE
Organism Rattus norvegicus

Publication

Synthesis, biological evaluation and structure-activity relationships of new phthalazinedione derivatives with vasorelaxant activity.
Munín J, Quezada E, Cuiñas A, Campos-Toimil M, Uriarte E, Santana L, Viña D.
Eur J Med Chem (2014) 82 : 407 -417
PubMed 24929291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 4.84 5.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3290856 1 5.43
CHEMBL3290849 1 5.31
CHEMBL3290854 1 5.25
CHEMBL3290874 1 5.17
CHEMBL3290860 1 5.13
CHEMBL3290869 1 5.07
CHEMBL3290858 1 4.93
CHEMBL3290861 1 4.88
CHEMBL3290859 1 4.88
CHEMBL3290857 1 4.88
CHEMBL3290852 1 4.84
CHEMBL3290870 1 4.81
CHEMBL3290855 1 4.80
CHEMBL3290862 1 4.74
CHEMBL3290873 1 4.70
CHEMBL3290853 1 4.63
CHEMBL3290872 1 4.57
CHEMBL12856 INAMRINONE 4.0 1 4.55
CHEMBL3290866 1 4.52
CHEMBL3290871 1 4.49
CHEMBL12 DIAZEPAM 4.0 1 4.11
CHEMBL276832 HYDRALAZINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3290856 EC50 = 3710.0 nM 5.43
CHEMBL3290849 EC50 = 4850.0 nM 5.31
CHEMBL3290854 EC50 = 5570.0 nM 5.25
CHEMBL3290874 EC50 = 6710.0 nM 5.17
CHEMBL3290860 EC50 = 7440.0 nM 5.13
CHEMBL3290869 EC50 = 8460.0 nM 5.07
CHEMBL3290858 EC50 = 11710.0 nM 4.93
CHEMBL3290861 EC50 = 13300.0 nM 4.88
CHEMBL3290859 EC50 = 13190.0 nM 4.88
CHEMBL3290857 EC50 = 13100.0 nM 4.88
CHEMBL3290852 EC50 = 14560.0 nM 4.84
CHEMBL3290870 EC50 = 15450.0 nM 4.81
CHEMBL3290855 EC50 = 15940.0 nM 4.80
CHEMBL3290862 EC50 = 18230.0 nM 4.74
CHEMBL3290873 EC50 = 20160.0 nM 4.70
CHEMBL3290853 EC50 = 23610.0 nM 4.63
CHEMBL3290872 EC50 = 27160.0 nM 4.57
CHEMBL12856 INAMRINONE EC50 = 28000.0 nM 4.55
CHEMBL3290866 EC50 = 30180.0 nM 4.52
CHEMBL3290871 EC50 = 32550.0 nM 4.49
CHEMBL12 DIAZEPAM EC50 = 77200.0 nM 4.11
CHEMBL276832 HYDRALAZINE EC50 = 1320000.0 nM -