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Assay Detail

CHEMBL1120082

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

Functional
Vasorelaxant activity in rat aortic ring assessed as inhibition of phenylephrine-induced contraction
26
Total Activities
26
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

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
Bosanac T, Hickey ER, Ginn J, Kashem M, Kerr S, Kugler S, Li X, Olague A, Schlyer S, Young ER.
Bioorg Med Chem Lett (2010) 20 : 3746 -3749
PubMed 20471253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.97 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082821 1 7.64
CHEMBL1082820 1 7.40
CHEMBL1084324 1 7.26
CHEMBL1082819 1 7.22
CHEMBL1083747 1 7.20
CHEMBL1084105 1 7.18
CHEMBL1083748 1 7.06
CHEMBL1084597 1 7.05
CHEMBL1084653 1 6.85
CHEMBL1084104 1 6.82
CHEMBL1084110 1 6.80
CHEMBL1084892 1 6.77
CHEMBL1083800 1 6.68
CHEMBL1085082 1 6.66
CHEMBL1083113 1 6.60
CHEMBL1085341 1 6.26
CHEMBL1084800 1 -
CHEMBL1083276 1 -
CHEMBL1083799 1 -
CHEMBL1084554 1 -
CHEMBL1085773 1 -
CHEMBL1084051 1 -
CHEMBL1083749 1 -
CHEMBL1084323 1 -
CHEMBL1085342 1 -
CHEMBL1085083 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082821 IC50 = 23.0 nM 7.64
CHEMBL1082820 IC50 = 40.0 nM 7.40
CHEMBL1084324 IC50 = 55.0 nM 7.26
CHEMBL1082819 IC50 = 60.0 nM 7.22
CHEMBL1083747 IC50 = 63.0 nM 7.20
CHEMBL1084105 IC50 = 66.0 nM 7.18
CHEMBL1083748 IC50 = 88.0 nM 7.06
CHEMBL1084597 IC50 = 89.0 nM 7.05
CHEMBL1084653 IC50 = 140.0 nM 6.85
CHEMBL1084104 IC50 = 150.0 nM 6.82
CHEMBL1084110 IC50 = 160.0 nM 6.80
CHEMBL1084892 IC50 = 170.0 nM 6.77
CHEMBL1083800 IC50 = 210.0 nM 6.68
CHEMBL1085082 IC50 = 220.0 nM 6.66
CHEMBL1083113 IC50 = 250.0 nM 6.60
CHEMBL1085341 IC50 = 550.0 nM 6.26
CHEMBL1084800 IC50 - -
CHEMBL1083276 IC50 - -
CHEMBL1083799 IC50 - -
CHEMBL1084554 IC50 - -
CHEMBL1085773 IC50 - -
CHEMBL1084051 IC50 - -
CHEMBL1083749 IC50 - -
CHEMBL1084323 IC50 - -
CHEMBL1085342 IC50 - -
CHEMBL1085083 IC50 - -