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Assay Detail

CHEMBL2383108

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Functional
Vasorelaxant activity in Wistar rat endothelium-denuded aortic rings assessed as reduction of KCl-induced contraction
12
Total Activities
12
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

1,4-Benzothiazine ATP-sensitive potassium channel openers: modifications at the C-2 and C-6 positions.
Martelli A, Manfroni G, Sabbatini P, Barreca ML, Testai L, Novelli M, Sabatini S, Massari S, Tabarrini O, Masiello P, Calderone V, Cecchetti V.
J Med Chem (2013) 56 : 4718 -4728
PubMed 23662847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.91 10.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121402 1 10.38
CHEMBL2381499 1 8.84
CHEMBL2381493 1 8.08
CHEMBL2381495 1 7.18
CHEMBL2381500 1 6.81
CHEMBL100 LEVCROMAKALIM 2.0 1 6.49
CHEMBL2381494 1 6.27
CHEMBL2381496 1 6.14
CHEMBL2381498 1 6.10
CHEMBL2381497 1 6.03
CHEMBL2381501 1 5.40
CHEMBL2381502 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121402 IC50 = 0.04169 nM 10.38
CHEMBL2381499 IC50 = 1.445 nM 8.84
CHEMBL2381493 IC50 = 8.318 nM 8.08
CHEMBL2381495 IC50 = 66.07 nM 7.18
CHEMBL2381500 IC50 = 154.88 nM 6.81
CHEMBL100 LEVCROMAKALIM IC50 = 323.59 nM 6.49
CHEMBL2381494 IC50 = 537.03 nM 6.27
CHEMBL2381496 IC50 = 724.44 nM 6.14
CHEMBL2381498 IC50 = 794.33 nM 6.10
CHEMBL2381497 IC50 = 933.25 nM 6.03
CHEMBL2381501 IC50 = 3981.07 nM 5.40
CHEMBL2381502 IC50 = 6606.93 nM 5.18