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Assay Detail

CHEMBL1023020

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Functional
Vasodilative activity against KCl-precontracted Sprague-Dawley rat thoracic aorta assessed as reduction in phenylepinephrine-induced contraction
ChEMBL ↗
48
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aorta (CHEMBL613606) ↗
Type TISSUE
Organism Rattus norvegicus

Publication

Synthesis and vasodilator effects of rutaecarpine analogues which might be involved transient receptor potential vanilloid subfamily, member 1 (TRPV1).
Chen Z, Hu G, Li D, Chen J, Li Y, Zhou H, Xie Y.
Bioorg Med Chem (2009) 17 : 2351 -2359
PubMed 19254847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 5.10 5.91
Emax 24 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517793 — — 2 5.91
CHEMBL85139 RUTAECARPINE — 2 5.88
CHEMBL453260 — — 2 5.68
CHEMBL464022 — — 2 5.64
CHEMBL463235 — — 2 5.61
CHEMBL465229 — — 2 5.52
CHEMBL516838 — — 2 5.49
CHEMBL473786 — — 2 5.11
CHEMBL473363 — — 2 5.03
CHEMBL464421 — — 2 4.78
CHEMBL516036 — — 2 4.71
CHEMBL455777 RUTAECARPANE — 2 4.70
CHEMBL86078 — — 2 4.68
CHEMBL518398 — — 2 4.65
CHEMBL472788 RUTAECARPENE — 2 4.60
CHEMBL85106 — — 2 4.49
CHEMBL85826 — — 2 4.26
CHEMBL473368 — — 2 -
CHEMBL473369 — — 2 -
CHEMBL472784 — — 2 -
CHEMBL472786 — — 2 -
CHEMBL514293 — — 2 -
CHEMBL472787 — — 2 -
CHEMBL473787 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517793 — EC50 = 1240.0 nM 5.91
CHEMBL85139 RUTAECARPINE EC50 = 1330.0 nM 5.88
CHEMBL453260 — EC50 = 2110.0 nM 5.68
CHEMBL464022 — EC50 = 2310.0 nM 5.64
CHEMBL463235 — EC50 = 2440.0 nM 5.61
CHEMBL465229 — EC50 = 2990.0 nM 5.52
CHEMBL516838 — EC50 = 3250.0 nM 5.49
CHEMBL473786 — EC50 = 7860.0 nM 5.11
CHEMBL473363 — EC50 = 9400.0 nM 5.03
CHEMBL464421 — EC50 = 16800.0 nM 4.78
CHEMBL516036 — EC50 = 19700.0 nM 4.71
CHEMBL455777 RUTAECARPANE EC50 = 20100.0 nM 4.70
CHEMBL86078 — EC50 = 21100.0 nM 4.68
CHEMBL518398 — EC50 = 22500.0 nM 4.65
CHEMBL472788 RUTAECARPENE EC50 = 25100.0 nM 4.60
CHEMBL85106 — EC50 = 32300.0 nM 4.49
CHEMBL85826 — EC50 = 55100.0 nM 4.26
CHEMBL473368 — EC50 = 220000.0 nM -
CHEMBL473369 — EC50 = 1590000.0 nM -
CHEMBL472784 — EC50 = 63600000.0 nM -
CHEMBL472786 — EC50 = 934000.0 nM -
CHEMBL514293 — EC50 = 15400000.0 nM -
CHEMBL472787 — EC50 = 5700000.0 nM -
CHEMBL473787 — EC50 = 5460000.0 nM -
CHEMBL85139 RUTAECARPINE Emax = 79.3 % -
CHEMBL517793 — Emax = 85.1 % -
CHEMBL465229 — Emax = 47.0 % -
CHEMBL516838 — Emax = 68.2 % -
CHEMBL85826 — Emax = 42.6 % -
CHEMBL463235 — Emax = 50.1 % -
CHEMBL464022 — Emax = 51.0 % -
CHEMBL86078 — Emax = 36.6 % -
CHEMBL85106 — Emax = 40.6 % -
CHEMBL473786 — Emax = 42.5 % -
CHEMBL455777 RUTAECARPANE Emax = 63.6 % -
CHEMBL472788 RUTAECARPENE Emax = 68.9 % -
CHEMBL472787 — Emax = 13.2 % -
CHEMBL514293 — Emax = 14.1 % -
CHEMBL472786 — Emax = 31.6 % -
CHEMBL472784 — Emax = 13.0 % -
CHEMBL473369 — Emax = 29.9 % -
CHEMBL473368 — Emax = 39.8 % -
CHEMBL473363 — Emax = 40.3 % -
CHEMBL516036 — Emax = 37.1 % -
CHEMBL453260 — Emax = 55.2 % -
CHEMBL518398 — Emax = 33.9 % -
CHEMBL473787 — Emax = 15.5 % -
CHEMBL464421 — Emax = 39.6 % -