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Assay Detail

CHEMBL2025930

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

Binding
Inhibition of human His-puritin-tagged ROCK1 expressed in Sf9 cells after 1 hr by FRET-based enzyme-coupled assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.
Li R, Martin MP, Liu Y, Wang B, Patel RA, Zhu JY, Sun N, Pireddu R, Lawrence NJ, Li J, Haura EB, Sung SS, Guida WC, Schonbrunn E, Sebti SM.
J Med Chem (2012) 55 : 2474 -2478
PubMed 22272748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.95 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2023154 1 6.19
CHEMBL2023156 1 5.94
CHEMBL2023160 1 5.85
CHEMBL2023158 1 5.77
CHEMBL2023153 1 5.66
CHEMBL2023155 1 5.61
CHEMBL2023152 1 5.58
CHEMBL2023159 1 5.58
CHEMBL2023151 1 5.54
CHEMBL2023150 1 5.34
CHEMBL2023157 1 5.04
CHEMBL225282 1 4.86
CHEMBL2023149 1 4.67
CHEMBL2023161 1 4.51
CHEMBL2023147 1 4.23
CHEMBL503641 1 4.19
CHEMBL2022282 1 4.14
CHEMBL67352 1 4.12
CHEMBL2023148 1 3.80
CHEMBL17551 1 3.74
CHEMBL1566648 1 3.57
CHEMBL2023144 1 -
CHEMBL2023145 1 -
CHEMBL2023146 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2023154 IC50 = 650.0 nM 6.19
CHEMBL2023156 IC50 = 1150.0 nM 5.94
CHEMBL2023160 IC50 = 1410.0 nM 5.85
CHEMBL2023158 IC50 = 1690.0 nM 5.77
CHEMBL2023153 IC50 = 2200.0 nM 5.66
CHEMBL2023155 IC50 = 2460.0 nM 5.61
CHEMBL2023152 IC50 = 2600.0 nM 5.58
CHEMBL2023159 IC50 = 2610.0 nM 5.58
CHEMBL2023151 IC50 = 2900.0 nM 5.54
CHEMBL2023150 IC50 = 4600.0 nM 5.34
CHEMBL2023157 IC50 = 9070.0 nM 5.04
CHEMBL225282 IC50 = 13900.0 nM 4.86
CHEMBL2023149 IC50 = 21500.0 nM 4.67
CHEMBL2023161 IC50 = 31010.0 nM 4.51
CHEMBL2023147 IC50 = 59100.0 nM 4.23
CHEMBL503641 IC50 = 65000.0 nM 4.19
CHEMBL2022282 IC50 = 72500.0 nM 4.14
CHEMBL67352 IC50 = 75500.0 nM 4.12
CHEMBL2023148 IC50 = 157100.0 nM 3.80
CHEMBL17551 IC50 = 181300.0 nM 3.74
CHEMBL1566648 IC50 = 270000.0 nM 3.57
CHEMBL2023144 IC50 > 400000.0 nM -
CHEMBL2023145 IC50 > 400000.0 nM -
CHEMBL2023146 IC50 - -