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Assay Detail

CHEMBL3383292

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Binding
Inhibition of ROCK-1 (unknown origin)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Rho-associated protein kinase 1 (CHEMBL3231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.
Shaw D, Hollingworth G, Soldermann N, Sprague E, Schuler W, Vangrevelinghe E, Duggan N, Thomas M, Kosaka T, Waters N, van Eis MJ.
Bioorg Med Chem Lett (2014) 24 : 4812 -4817
PubMed 25248678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.45 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406821 1 8.30
CHEMBL3338837 1 7.92
CHEMBL1956071 1 7.85
CHEMBL2147538 1 7.68
CHEMBL1214929 1 7.52
CHEMBL3338838 1 7.50
CHEMBL3338839 1 7.44
CHEMBL3338840 1 7.41
CHEMBL3338842 1 7.28
CHEMBL559147 Y-27632 1 7.03
CHEMBL3338841 1 6.85
CHEMBL3338843 1 6.63
CHEMBL3338844 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406821 IC50 = 5.0 nM 8.30
CHEMBL3338837 IC50 = 12.0 nM 7.92
CHEMBL1956071 IC50 = 14.0 nM 7.85
CHEMBL2147538 IC50 = 21.0 nM 7.68
CHEMBL1214929 IC50 = 30.0 nM 7.52
CHEMBL3338838 IC50 = 32.0 nM 7.50
CHEMBL3338839 IC50 = 36.0 nM 7.44
CHEMBL3338840 IC50 = 39.0 nM 7.41
CHEMBL3338842 IC50 = 52.0 nM 7.28
CHEMBL559147 Y-27632 IC50 = 93.0 nM 7.03
CHEMBL3338841 IC50 = 141.0 nM 6.85
CHEMBL3338843 IC50 = 233.0 nM 6.63
CHEMBL3338844 IC50 > 1000.0 nM -