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Assay Detail

CHEMBL1011047

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Binding
Binding affinity to ROCK2 by fluorescence polarization assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases.
Lavogina D, Lust M, Viil I, König N, Raidaru G, Rogozina J, Enkvist E, Uri A, Bossemeyer D.
J Med Chem (2009) 52 : 308 -321
PubMed 19143565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 7.07 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297394 1 8.85
CHEMBL1315166 1 7.51
CHEMBL501706 1 7.05
CHEMBL505949 1 6.92
CHEMBL498924 1 6.73
CHEMBL495766 1 5.35
CHEMBL525385 1 -
CHEMBL524516 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297394 Kd = 1.4 nM 8.85
CHEMBL1315166 Kd = 31.0 nM 7.51
CHEMBL501706 Kd = 89.7 nM 7.05
CHEMBL505949 Kd = 119.0 nM 6.92
CHEMBL498924 Kd = 187.0 nM 6.73
CHEMBL495766 Kd = 4480.0 nM 5.35
CHEMBL525385 Kd < 1.0 nM -
CHEMBL524516 Kd < 1.0 nM -