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Assay Detail

CHEMBL3411299

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

Binding
Inhibition of human ROCK2 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK peptide substrate, ATP and [gamma33P]ATP
42
Total Activities
42
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

Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.
Yin Y, Zheng K, Eid N, Howard S, Jeong JH, Yi F, Guo J, Park CM, Bibian M, Wu W, Hernandez P, Park H, Wu Y, Luo JL, LoGrasso PV, Feng Y.
J Med Chem (2015) 58 : 1846 -1861
PubMed 25621531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.79 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3410022 1 7.35
CHEMBL1951443 1 7.05
CHEMBL1951349 1 6.88
CHEMBL1951441 1 6.78
CHEMBL1951350 1 6.61
CHEMBL3410050 1 6.34
CHEMBL3407526 1 6.11
CHEMBL3410026 1 6.01
CHEMBL1951344 1 5.87
CHEMBL1951346 1 5.79
CHEMBL3410037 1 5.79
CHEMBL3410038 1 5.72
CHEMBL3410033 1 5.64
CHEMBL3410028 1 5.63
CHEMBL3410031 1 5.59
CHEMBL3410047 1 5.49
CHEMBL3410039 1 5.49
CHEMBL3410040 1 5.48
CHEMBL3410042 1 5.36
CHEMBL3410029 1 5.27
CHEMBL3410023 1 5.25
CHEMBL3410045 1 5.23
CHEMBL3410036 1 5.18
CHEMBL3410030 1 5.18
CHEMBL3410027 1 5.15
CHEMBL3410044 1 5.05
CHEMBL3410041 1 4.95
CHEMBL3410025 1 -
CHEMBL3410056 1 -
CHEMBL3410055 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3410022 IC50 = 45.0 nM 7.35
CHEMBL1951443 IC50 = 90.0 nM 7.05
CHEMBL1951349 IC50 = 132.0 nM 6.88
CHEMBL1951441 IC50 = 166.0 nM 6.78
CHEMBL1951350 IC50 = 247.0 nM 6.61
CHEMBL3410050 IC50 = 460.0 nM 6.34
CHEMBL3407526 IC50 = 781.0 nM 6.11
CHEMBL3410026 IC50 = 976.0 nM 6.01
CHEMBL1951344 IC50 = 1365.0 nM 5.87
CHEMBL1951346 IC50 = 1608.0 nM 5.79
CHEMBL3410037 IC50 = 1605.0 nM 5.79
CHEMBL3410038 IC50 = 1898.0 nM 5.72
CHEMBL3410033 IC50 = 2290.0 nM 5.64
CHEMBL3410028 IC50 = 2358.0 nM 5.63
CHEMBL3410031 IC50 = 2572.0 nM 5.59
CHEMBL3410047 IC50 = 3219.0 nM 5.49
CHEMBL3410039 IC50 = 3239.0 nM 5.49
CHEMBL3410040 IC50 = 3339.0 nM 5.48
CHEMBL3410042 IC50 = 4357.0 nM 5.36
CHEMBL3410029 IC50 = 5421.0 nM 5.27
CHEMBL3410023 IC50 = 5570.0 nM 5.25
CHEMBL3410045 IC50 = 5932.0 nM 5.23
CHEMBL3410030 IC50 = 6652.0 nM 5.18
CHEMBL3410036 IC50 = 6565.0 nM 5.18
CHEMBL3410027 IC50 = 7083.0 nM 5.15
CHEMBL3410044 IC50 = 8940.0 nM 5.05
CHEMBL3410041 IC50 = 11270.0 nM 4.95
CHEMBL3410034 IC50 > 10000.0 nM -
CHEMBL3410032 IC50 > 10000.0 nM -
CHEMBL3410043 IC50 > 10000.0 nM -
CHEMBL3410046 IC50 > 10000.0 nM -
CHEMBL3410035 IC50 - -
CHEMBL3410048 IC50 > 10000.0 nM -
CHEMBL3410049 IC50 - -
CHEMBL3410024 IC50 > 10000.0 nM -
CHEMBL3410051 IC50 > 10000.0 nM -
CHEMBL3410052 IC50 > 10000.0 nM -
CHEMBL3410053 IC50 - -
CHEMBL3410054 IC50 - -
CHEMBL3410055 IC50 > 20000.0 nM -
CHEMBL3410056 IC50 > 20000.0 nM -
CHEMBL3410025 IC50 > 10000.0 nM -