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Assay Detail

CHEMBL5369546

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

Binding
Inhibition of ROCK2 (unknown origin)
29
Total Activities
29
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 of Novel Oxazepine Derivatives as Akt/ROCK Inhibitors for Growth Arrest and Differentiation Induction in Neuroblastoma Treatment.
Che J, Bing S, Lu J, Jin Z, Gao J, Sheng H, Li D, Yang B, He Q, Ying M, Dong X.
J Med Chem (2023) 66 : 13530 -13555
PubMed 37749892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 8.10 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5408482 1 8.92
CHEMBL5437264 1 8.89
CHEMBL5421280 1 8.85
CHEMBL5428749 1 8.85
CHEMBL5406146 1 8.82
CHEMBL5438374 1 8.77
CHEMBL5426560 1 8.72
CHEMBL5400934 1 8.38
CHEMBL5412156 1 8.16
CHEMBL5422811 1 8.12
CHEMBL5407182 1 8.11
CHEMBL5428430 1 7.83
CHEMBL5414576 1 7.79
CHEMBL5404104 1 7.76
CHEMBL5411877 1 7.46
CHEMBL5440366 1 7.26
CHEMBL5425811 1 6.61
CHEMBL4595425 1 6.47
CHEMBL5395510 1 -
CHEMBL5405389 1 -
CHEMBL5399312 1 -
CHEMBL5430096 1 -
CHEMBL5400666 1 -
CHEMBL5407425 1 -
CHEMBL5424919 1 -
CHEMBL5398425 1 -
CHEMBL5409113 1 -
CHEMBL5405650 1 -
CHEMBL5425278 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5408482 IC50 = 1.2 nM 8.92
CHEMBL5437264 IC50 = 1.3 nM 8.89
CHEMBL5421280 IC50 = 1.4 nM 8.85
CHEMBL5428749 IC50 = 1.4 nM 8.85
CHEMBL5406146 IC50 = 1.5 nM 8.82
CHEMBL5438374 IC50 = 1.7 nM 8.77
CHEMBL5426560 IC50 = 1.9 nM 8.72
CHEMBL5400934 IC50 = 4.2 nM 8.38
CHEMBL5412156 IC50 = 6.9 nM 8.16
CHEMBL5422811 IC50 = 7.6 nM 8.12
CHEMBL5407182 IC50 = 7.8 nM 8.11
CHEMBL5428430 IC50 = 14.7 nM 7.83
CHEMBL5414576 IC50 = 16.2 nM 7.79
CHEMBL5404104 IC50 = 17.4 nM 7.76
CHEMBL5411877 IC50 = 34.3 nM 7.46
CHEMBL5440366 IC50 = 54.7 nM 7.26
CHEMBL5425811 IC50 = 246.8 nM 6.61
CHEMBL4595425 IC50 = 337.0 nM 6.47
CHEMBL5395510 IC50 - -
CHEMBL5405389 IC50 - -
CHEMBL5399312 IC50 - -
CHEMBL5430096 IC50 - -
CHEMBL5400666 IC50 > 10000.0 nM -
CHEMBL5407425 IC50 - -
CHEMBL5424919 IC50 - -
CHEMBL5398425 IC50 - -
CHEMBL5409113 IC50 - -
CHEMBL5405650 IC50 - -
CHEMBL5425278 IC50 - -