Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4040374

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

Binding
Inhibition of recombinant human N-terminal GST-tagged ROCK2 catalytic domain (1 to 553 residues) expressed in baculovirus expression system using STK 2-biotin as substrate measured after 60 mins by HTRF/TR-FRET assay
ChEMBL ↗
92
Total Activities
92
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

Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
Okawa T, Aramaki Y, Yamamoto M, Kobayashi T, Fukumoto S, Toyoda Y, Henta T, Hata A, Ikeda S, Kaneko M, Hoffman ID, Sang BC, Zou H, Kawamoto T.
J Med Chem (2017) 60 : 6942 -6990
PubMed 28699740 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 92 6.49 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067877 — — 1 8.14
CHEMBL4089087 — — 1 7.75
CHEMBL4093075 — — 1 7.75
CHEMBL4060973 — — 1 7.70
CHEMBL4100175 — — 1 7.66
CHEMBL4065690 — — 1 7.64
CHEMBL4082775 — — 1 7.62
CHEMBL4082853 — — 1 7.57
CHEMBL4082805 — — 1 7.52
CHEMBL4076320 — — 1 7.51
CHEMBL4101739 — — 1 7.33
CHEMBL4072828 — — 1 7.31
CHEMBL4077447 — — 1 7.30
CHEMBL4104512 — — 1 7.28
CHEMBL4082713 — — 1 7.24
CHEMBL4087117 — — 1 7.22
CHEMBL3728772 — — 1 7.21
CHEMBL4085317 — — 1 7.16
CHEMBL4072308 — — 1 7.13
CHEMBL4083276 — — 1 7.12
CHEMBL4095659 — — 1 7.07
CHEMBL4062649 — — 1 7.03
CHEMBL4062560 — — 1 7.03
CHEMBL4091566 — — 1 7.01
CHEMBL4075063 — — 1 7.00
CHEMBL4070100 — — 1 6.96
CHEMBL4072362 — — 1 6.92
CHEMBL4105466 — — 1 6.89
CHEMBL4086046 — — 1 6.85
CHEMBL4072686 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067877 — IC50 = 7.3 nM 8.14
CHEMBL4089087 — IC50 = 18.0 nM 7.75
CHEMBL4093075 — IC50 = 18.0 nM 7.75
CHEMBL4060973 — IC50 = 20.0 nM 7.70
CHEMBL4100175 — IC50 = 22.0 nM 7.66
CHEMBL4065690 — IC50 = 23.0 nM 7.64
CHEMBL4082775 — IC50 = 24.0 nM 7.62
CHEMBL4082853 — IC50 = 27.0 nM 7.57
CHEMBL4082805 — IC50 = 30.0 nM 7.52
CHEMBL4076320 — IC50 = 31.0 nM 7.51
CHEMBL4101739 — IC50 = 47.0 nM 7.33
CHEMBL4072828 — IC50 = 49.0 nM 7.31
CHEMBL4077447 — IC50 = 50.0 nM 7.30
CHEMBL4104512 — IC50 = 52.0 nM 7.28
CHEMBL4082713 — IC50 = 58.0 nM 7.24
CHEMBL4087117 — IC50 = 60.0 nM 7.22
CHEMBL3728772 — IC50 = 62.0 nM 7.21
CHEMBL4085317 — IC50 = 70.0 nM 7.16
CHEMBL4072308 — IC50 = 74.0 nM 7.13
CHEMBL4083276 — IC50 = 76.0 nM 7.12
CHEMBL4095659 — IC50 = 85.0 nM 7.07
CHEMBL4062649 — IC50 = 94.0 nM 7.03
CHEMBL4062560 — IC50 = 94.0 nM 7.03
CHEMBL4091566 — IC50 = 98.0 nM 7.01
CHEMBL4075063 — IC50 = 100.0 nM 7.00
CHEMBL4070100 — IC50 = 110.0 nM 6.96
CHEMBL4072362 — IC50 = 120.0 nM 6.92
CHEMBL4105466 — IC50 = 130.0 nM 6.89
CHEMBL4086046 — IC50 = 140.0 nM 6.85
CHEMBL4072686 — IC50 = 160.0 nM 6.80
CHEMBL4081217 — IC50 = 160.0 nM 6.80
CHEMBL4099309 — IC50 = 170.0 nM 6.77
CHEMBL1738878 — IC50 = 190.0 nM 6.72
CHEMBL4073882 — IC50 = 190.0 nM 6.72
CHEMBL4095595 — IC50 = 220.0 nM 6.66
CHEMBL4091067 — IC50 = 260.0 nM 6.58
CHEMBL4071201 — IC50 = 270.0 nM 6.57
CHEMBL4082714 — IC50 = 280.0 nM 6.55
CHEMBL3728445 — IC50 = 300.0 nM 6.52
CHEMBL4096791 — IC50 = 320.0 nM 6.50
CHEMBL4064232 — IC50 = 320.0 nM 6.50
CHEMBL4071398 — IC50 = 320.0 nM 6.50
CHEMBL4078768 — IC50 = 340.0 nM 6.47
CHEMBL4082173 — IC50 = 350.0 nM 6.46
CHEMBL4100891 — IC50 = 360.0 nM 6.44
CHEMBL4093686 — IC50 = 380.0 nM 6.42
CHEMBL4082559 — IC50 = 390.0 nM 6.41
CHEMBL4100779 — IC50 = 480.0 nM 6.32
CHEMBL4091573 — IC50 = 530.0 nM 6.28
CHEMBL4098177 — IC50 = 540.0 nM 6.27