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Assay Detail

CHEMBL5257163

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

Binding
Inhibition of ROCK2 (unknown origin)
21
Total Activities
21
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 2 (CHEMBL2973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rho Kinase (ROCK) Inhibitors and Their Therapeutic Potential.
Feng Y, LoGrasso PV, Defert O, Li R.
J Med Chem (2016) 59 : 2269 -2300
PubMed 26486225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.15 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5270382 1 9.00
CHEMBL5274003 1 9.00
CHEMBL3951271 1 9.00
CHEMBL1971943 BAY-549 1 9.00
CHEMBL225166 1 8.52
CHEMBL571948 Y-39983 1.0 1 8.44
CHEMBL5279379 1 8.22
CHEMBL3218011 1 8.21
CHEMBL5281033 1 8.05
CHEMBL225224 1 7.70
CHEMBL5284291 1 7.58
CHEMBL5283427 1 7.48
CHEMBL2005186 BELUMOSUDIL 4.0 1 7.22
CHEMBL3040797 1 6.70
CHEMBL3913336 1 -
CHEMBL428462 1 -
CHEMBL5266434 1 -
CHEMBL5278094 1 -
CHEMBL5282451 1 -
CHEMBL5280099 1 -
CHEMBL3544960 AT-13148 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5270382 IC50 = 1.0 nM 9.00
CHEMBL5274003 IC50 = 1.0 nM 9.00
CHEMBL3951271 IC50 = 1.0 nM 9.00
CHEMBL1971943 BAY-549 IC50 = 1.0 nM 9.00
CHEMBL225166 IC50 = 3.0 nM 8.52
CHEMBL571948 Y-39983 IC50 = 3.6 nM 8.44
CHEMBL5279379 IC50 = 6.0 nM 8.22
CHEMBL3218011 IC50 = 6.2 nM 8.21
CHEMBL5281033 IC50 = 9.0 nM 8.05
CHEMBL225224 IC50 = 20.0 nM 7.70
CHEMBL5284291 IC50 = 26.0 nM 7.58
CHEMBL5283427 IC50 = 33.0 nM 7.48
CHEMBL2005186 BELUMOSUDIL IC50 = 60.0 nM 7.22
CHEMBL3040797 IC50 = 200.0 nM 6.70
CHEMBL3913336 IC50 < 1.0 nM -
CHEMBL428462 IC50 < 100.0 nM -
CHEMBL5266434 IC50 < 100.0 nM -
CHEMBL5278094 IC50 < 100.0 nM -
CHEMBL5282451 IC50 < 100.0 nM -
CHEMBL5280099 IC50 < 100.0 nM -
CHEMBL3544960 AT-13148 IC50 < 10.0 nM -