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Assay Detail

CHEMBL2444040

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

Binding
Inhibition of ROCK2 (unknown origin) using long S6 kinase peptide as substrate by radiometric assay
28
Total Activities
28
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

3-[2-(Aminomethyl)-5-[(pyridin-4-yl)carbamoyl]phenyl] benzoates as soft ROCK inhibitors.
Boland S, Defert O, Alen J, Bourin A, Castermans K, Kindt N, Boumans N, Panitti L, Van de Velde S, Stalmans I, Leysen D.
Bioorg Med Chem Lett (2013) 23 : 6442 -6446
PubMed 24119557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.04 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2440742 1 8.92
CHEMBL2440735 1 8.85
CHEMBL2440745 1 8.85
CHEMBL2440733 1 8.82
CHEMBL2440737 1 8.60
CHEMBL2440730 1 8.57
CHEMBL2440743 1 8.54
CHEMBL2440732 1 8.44
CHEMBL2440756 1 8.37
CHEMBL2440747 1 8.31
CHEMBL2440753 1 8.30
CHEMBL2440750 1 8.29
CHEMBL2440746 1 8.26
CHEMBL2440752 1 8.21
CHEMBL2440749 1 8.11
CHEMBL2440736 1 8.06
CHEMBL2440738 1 7.92
CHEMBL2440755 1 7.89
CHEMBL2440751 1 7.70
CHEMBL2440748 1 7.66
CHEMBL2440734 1 7.43
CHEMBL2440731 1 7.35
CHEMBL2440754 1 7.32
CHEMBL559147 Y-27632 1 7.27
CHEMBL2440740 1 7.26
CHEMBL2440741 1 6.99
CHEMBL2440739 1 6.78
CHEMBL2440744 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2440742 IC50 = 1.2 nM 8.92
CHEMBL2440735 IC50 = 1.4 nM 8.85
CHEMBL2440745 IC50 = 1.4 nM 8.85
CHEMBL2440733 IC50 = 1.5 nM 8.82
CHEMBL2440737 IC50 = 2.5 nM 8.60
CHEMBL2440730 IC50 = 2.7 nM 8.57
CHEMBL2440743 IC50 = 2.9 nM 8.54
CHEMBL2440732 IC50 = 3.6 nM 8.44
CHEMBL2440756 IC50 = 4.3 nM 8.37
CHEMBL2440747 IC50 = 4.9 nM 8.31
CHEMBL2440753 IC50 = 5.0 nM 8.30
CHEMBL2440750 IC50 = 5.1 nM 8.29
CHEMBL2440746 IC50 = 5.5 nM 8.26
CHEMBL2440752 IC50 = 6.2 nM 8.21
CHEMBL2440749 IC50 = 7.8 nM 8.11
CHEMBL2440736 IC50 = 8.7 nM 8.06
CHEMBL2440738 IC50 = 12.0 nM 7.92
CHEMBL2440755 IC50 = 13.0 nM 7.89
CHEMBL2440751 IC50 = 20.0 nM 7.70
CHEMBL2440748 IC50 = 22.0 nM 7.66
CHEMBL2440734 IC50 = 37.0 nM 7.43
CHEMBL2440731 IC50 = 45.0 nM 7.35
CHEMBL2440754 IC50 = 48.0 nM 7.32
CHEMBL559147 Y-27632 IC50 = 54.0 nM 7.27
CHEMBL2440740 IC50 = 55.0 nM 7.26
CHEMBL2440741 IC50 = 102.0 nM 6.99
CHEMBL2440739 IC50 = 167.0 nM 6.78
CHEMBL2440744 IC50 < 1.0 nM -