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Assay Detail

CHEMBL1805103

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

Binding
Inhibition of human recombinant CDK5/p25
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Debdab M, Carreaux F, Renault S, Soundararajan M, Fedorov O, Filippakopoulos P, Lozach O, Babault L, Tahtouh T, Baratte B, Ogawa Y, Hagiwara M, Eisenreich A, Rauch U, Knapp S, Meijer L, Bazureau JP.
J Med Chem (2011) 54 : 4172 -4186
PubMed 21615147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.61 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1802358 1 6.39
CHEMBL1802849 1 6.22
CHEMBL1803071 1 6.16
CHEMBL1179821 1 6.04
CHEMBL1803073 1 5.92
CHEMBL1802851 1 5.89
CHEMBL1802848 1 5.80
CHEMBL1803070 1 5.80
CHEMBL1802850 1 5.77
CHEMBL1803085 1 5.77
CHEMBL1802844 1 5.75
CHEMBL1802847 1 5.70
CHEMBL1803082 1 5.62
CHEMBL1802843 1 5.52
CHEMBL1802356 1 5.52
CHEMBL1802846 1 5.51
CHEMBL1802845 1 5.48
CHEMBL1802855 1 5.40
CHEMBL1803069 1 5.37
CHEMBL1802853 1 5.35
CHEMBL1803083 1 5.33
CHEMBL1803072 1 5.24
CHEMBL1803079 1 5.14
CHEMBL1802842 1 4.80
CHEMBL1802841 1 4.75
CHEMBL1802852 1 -
CHEMBL1802355 1 -
CHEMBL485053 LEUCETTAMINE B 1 -
CHEMBL1802357 1 -
CHEMBL1803067 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1802358 IC50 = 410.0 nM 6.39
CHEMBL1802849 IC50 = 600.0 nM 6.22
CHEMBL1803071 IC50 = 700.0 nM 6.16
CHEMBL1179821 IC50 = 910.0 nM 6.04
CHEMBL1803073 IC50 = 1200.0 nM 5.92
CHEMBL1802851 IC50 = 1300.0 nM 5.89
CHEMBL1802848 IC50 = 1600.0 nM 5.80
CHEMBL1803070 IC50 = 1600.0 nM 5.80
CHEMBL1802850 IC50 = 1700.0 nM 5.77
CHEMBL1803085 IC50 = 1700.0 nM 5.77
CHEMBL1802844 IC50 = 1800.0 nM 5.75
CHEMBL1802847 IC50 = 2000.0 nM 5.70
CHEMBL1803082 IC50 = 2400.0 nM 5.62
CHEMBL1802843 IC50 = 3000.0 nM 5.52
CHEMBL1802356 IC50 = 3000.0 nM 5.52
CHEMBL1802846 IC50 = 3100.0 nM 5.51
CHEMBL1802845 IC50 = 3300.0 nM 5.48
CHEMBL1802855 IC50 = 4000.0 nM 5.40
CHEMBL1803069 IC50 = 4300.0 nM 5.37
CHEMBL1802853 IC50 = 4500.0 nM 5.35
CHEMBL1803083 IC50 = 4700.0 nM 5.33
CHEMBL1803072 IC50 = 5800.0 nM 5.24
CHEMBL1803079 IC50 = 7300.0 nM 5.14
CHEMBL1802842 IC50 = 16000.0 nM 4.80
CHEMBL1802841 IC50 = 18000.0 nM 4.75
CHEMBL1803068 IC50 > 10000.0 nM -
CHEMBL1802857 IC50 > 10000.0 nM -
CHEMBL1802856 IC50 > 10000.0 nM -
CHEMBL1803084 IC50 > 10000.0 nM -
CHEMBL1802854 IC50 > 10000.0 nM -
CHEMBL1803067 IC50 > 10000.0 nM -
CHEMBL1802357 IC50 > 10000.0 nM -
CHEMBL485053 LEUCETTAMINE B IC50 > 10000.0 nM -
CHEMBL1802355 IC50 > 10000.0 nM -
CHEMBL1802852 IC50 > 100000.0 nM -