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Assay Detail

CHEMBL1647667

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Binding
Inhibition of ROCK-2 by Immobilized metal ion affinity-based fluorescence polarization assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Rho-associated protein kinase 2 (CHEMBL2973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Bennett J, Boucharens S, Black D, Cook A, Brown AR, Epemolu O, Fletcher D, Haunso A, Huggett M, Jones P, Laats S, Lyons A, Mestres J, de Man J, Morphy R, Rankovic Z, Sherborne B, Sherry L, van Straten N, Westwood P, Zaman GZ.
Bioorg Med Chem Lett (2011) 21 : 97 -101
PubMed 21145740 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.15 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559147 Y-27632 1 6.61
CHEMBL1233300 HYDROXYFASUDIL 1 6.24
CHEMBL1643361 1 5.89
CHEMBL38380 FASUDIL 3.0 1 5.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559147 Y-27632 IC50 = 245.47 nM 6.61
CHEMBL1233300 HYDROXYFASUDIL IC50 = 575.44 nM 6.24
CHEMBL1643361 IC50 = 1288.25 nM 5.89
CHEMBL38380 FASUDIL IC50 = 1348.96 nM 5.87