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Assay Detail

CHEMBL3377890

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

Binding
Inhibition of human Rock2 assessed as incorporation of P33 from ATP into biotinylated-cofilin substrate by scintillation counting analysis in presence of 2 uM ATP
1
Total Activities
1
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

Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.
Harrison BA, Almstead ZY, Burgoon H, Gardyan M, Goodwin NC, Healy J, Liu Y, Mabon R, Marinelli B, Samala L, Zhang Y, Stouch TR, Whitlock NA, Gopinathan S, McKnight B, Wang S, Patel N, Wilson AG, Hamman BD, Rice DS, Rawlins DB.
ACS Med Chem Lett (2015) 6 : 84 -88
PubMed 25589936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.50 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356433 LX-7101 1.0 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356433 LX-7101 IC50 = 32.0 nM 7.50