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Assay Detail

CHEMBL1228451

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

Functional
Antihypertensive activity in spontaneously hypertensive rat aortic ring assessed as relaxation of phenylepinephrine-stimulated contraction
23
Total Activities
23
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

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 2, optimization for blood pressure reduction in spontaneously hypertensive rats.
Ginn JD, Bosanac T, Chen R, Cywin C, Hickey E, Kashem M, Kerr S, Kugler S, Li X, Prokopowicz A, Schlyer S, Smith JD, Turner MR, Wu F, Young ER.
Bioorg Med Chem Lett (2010) 20 : 5153 -5156
PubMed 20678931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.42 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1084107 1 7.16
CHEMBL1222571 1 6.75
CHEMBL1222416 1 6.75
CHEMBL1222573 1 6.72
CHEMBL1222418 1 6.72
CHEMBL1085082 1 6.66
CHEMBL1083113 1 6.60
CHEMBL1223498 1 6.30
CHEMBL1222413 1 6.16
CHEMBL1222482 1 5.95
CHEMBL1085141 1 5.62
CHEMBL1083114 1 5.60
CHEMBL1222417 1 -
CHEMBL1222415 1 -
CHEMBL1222483 1 -
CHEMBL1222484 1 -
CHEMBL1085083 1 -
CHEMBL1222414 1 -
CHEMBL1223500 1 -
CHEMBL1222570 1 -
CHEMBL1223499 1 -
CHEMBL1222572 1 -
CHEMBL1222574 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1084107 EC50 = 69.0 nM 7.16
CHEMBL1222571 EC50 = 180.0 nM 6.75
CHEMBL1222416 EC50 = 180.0 nM 6.75
CHEMBL1222573 EC50 = 190.0 nM 6.72
CHEMBL1222418 EC50 = 190.0 nM 6.72
CHEMBL1085082 EC50 = 220.0 nM 6.66
CHEMBL1083113 EC50 = 250.0 nM 6.60
CHEMBL1223498 EC50 = 500.0 nM 6.30
CHEMBL1222413 EC50 = 700.0 nM 6.16
CHEMBL1222482 EC50 = 1120.0 nM 5.95
CHEMBL1085141 EC50 = 2400.0 nM 5.62
CHEMBL1083114 EC50 = 2500.0 nM 5.60
CHEMBL1222417 EC50 - -
CHEMBL1222415 EC50 - -
CHEMBL1222483 EC50 - -
CHEMBL1222484 EC50 - -
CHEMBL1085083 EC50 - -
CHEMBL1222414 EC50 - -
CHEMBL1223500 EC50 - -
CHEMBL1222570 EC50 - -
CHEMBL1223499 EC50 - -
CHEMBL1222572 EC50 - -
CHEMBL1222574 EC50 - -