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Assay Detail

CHEMBL5716553

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Functional
Vasorelaxant activity in isolated Chinchilla rabbit saphenous artery vessels assessed as inhibition of phenylephrine-mediated contraction
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Saphenous artery
Confidence 1 — Organism
Curated By Autocuration

Target

Saphenous artery (CHEMBL4845615)
Type TISSUE
Organism Oryctolagus cuniculus

Publication

Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors.
Schirok H, Kast R, Figueroa-Pérez S, Bennabi S, Gnoth MJ, Feurer A, Heckroth H, Thutewohl M, Paulsen H, Knorr A, Hütter J, Lobell M, Münter K, Geiss V, Ehmke H, Lang D, Radtke M, Mittendorf J, Stasch JP.
ChemMedChem (2008) 3 : 1893 -1904
PubMed 18973168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.48 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5270382 1 7.70
CHEMBL5722966 1 7.25
CHEMBL1971943 BAY-549 1 7.19
CHEMBL5722984 1 7.09
CHEMBL5723002 1 7.08
CHEMBL5723015 1 7.05
CHEMBL5428272 1 7.00
CHEMBL5722939 1 6.64
CHEMBL5274003 1 6.57
CHEMBL5722956 1 6.43
CHEMBL5722977 1 6.39
CHEMBL5722955 1 6.34
CHEMBL5722947 1 6.30
CHEMBL5723011 1 6.24
CHEMBL5722999 1 6.15
CHEMBL5723017 1 6.03
CHEMBL5722951 1 5.96
CHEMBL5722974 1 5.92
CHEMBL5722952 1 5.82
CHEMBL5722953 1 5.77
CHEMBL5723027 1 5.17
CHEMBL5722997 1 -
CHEMBL5722964 1 -
CHEMBL5722995 1 -
CHEMBL5723010 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5270382 IC50 = 20.0 nM 7.70
CHEMBL5722966 IC50 = 56.0 nM 7.25
CHEMBL1971943 BAY-549 IC50 = 65.0 nM 7.19
CHEMBL5722984 IC50 = 82.0 nM 7.09
CHEMBL5723002 IC50 = 84.0 nM 7.08
CHEMBL5723015 IC50 = 89.0 nM 7.05
CHEMBL5428272 IC50 = 100.0 nM 7.00
CHEMBL5722939 IC50 = 230.0 nM 6.64
CHEMBL5274003 IC50 = 270.0 nM 6.57
CHEMBL5722956 IC50 = 370.0 nM 6.43
CHEMBL5722977 IC50 = 410.0 nM 6.39
CHEMBL5722955 IC50 = 460.0 nM 6.34
CHEMBL5722947 IC50 = 500.0 nM 6.30
CHEMBL5723011 IC50 = 570.0 nM 6.24
CHEMBL5722999 IC50 = 710.0 nM 6.15
CHEMBL5723017 IC50 = 940.0 nM 6.03
CHEMBL5722951 IC50 = 1100.0 nM 5.96
CHEMBL5722974 IC50 = 1200.0 nM 5.92
CHEMBL5722952 IC50 = 1500.0 nM 5.82
CHEMBL5722953 IC50 = 1700.0 nM 5.77
CHEMBL5723027 IC50 = 6800.0 nM 5.17
CHEMBL5722997 IC50 - -
CHEMBL5722964 IC50 - -
CHEMBL5722995 IC50 - -
CHEMBL5723010 IC50 - -