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Assay Detail

CHEMBL3875854

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

Binding
Inhibition of human recombinant CDK5/p25 using histone H1 as substrate after 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis
47
Total Activities
47
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

Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors.
Labrière C, Lozach O, Blairvacq M, Meijer L, Guillou C.
Eur J Med Chem (2016) 124 : 920 -934
PubMed 27676471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 5.65 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3753668 1 6.89
CHEMBL3883660 1 6.36
CHEMBL3885431 1 6.34
CHEMBL3884015 1 6.11
CHEMBL3883639 1 6.10
CHEMBL3883764 1 6.10
CHEMBL3884932 1 6.03
CHEMBL3884583 1 5.80
CHEMBL3884861 1 5.35
CHEMBL3884845 1 5.27
CHEMBL3885328 1 5.25
CHEMBL3885360 1 5.22
CHEMBL3883820 1 5.22
CHEMBL3885021 1 5.19
CHEMBL3884821 1 5.19
CHEMBL3883448 1 5.16
CHEMBL3885335 1 5.10
CHEMBL3884627 1 5.05
CHEMBL3885316 1 -
CHEMBL3883458 1 -
CHEMBL3883414 1 -
CHEMBL3883541 1 -
CHEMBL3885036 1 -
CHEMBL3883813 1 -
CHEMBL3884031 1 -
CHEMBL3885333 1 -
CHEMBL3884570 1 -
CHEMBL3884241 1 -
CHEMBL3885092 1 -
CHEMBL3884027 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3753668 IC50 = 130.0 nM 6.89
CHEMBL3883660 IC50 = 440.0 nM 6.36
CHEMBL3885431 IC50 = 460.0 nM 6.34
CHEMBL3884015 IC50 = 780.0 nM 6.11
CHEMBL3883639 IC50 = 800.0 nM 6.10
CHEMBL3883764 IC50 = 800.0 nM 6.10
CHEMBL3884932 IC50 = 930.0 nM 6.03
CHEMBL3884583 IC50 = 1600.0 nM 5.80
CHEMBL3884861 IC50 = 4500.0 nM 5.35
CHEMBL3884845 IC50 = 5400.0 nM 5.27
CHEMBL3885328 IC50 = 5600.0 nM 5.25
CHEMBL3885360 IC50 = 6000.0 nM 5.22
CHEMBL3883820 IC50 = 6000.0 nM 5.22
CHEMBL3885021 IC50 = 6400.0 nM 5.19
CHEMBL3884821 IC50 = 6400.0 nM 5.19
CHEMBL3883448 IC50 = 7000.0 nM 5.16
CHEMBL3885335 IC50 = 8000.0 nM 5.10
CHEMBL3884627 IC50 = 9000.0 nM 5.05
CHEMBL3753955 IC50 > 10000.0 nM -
CHEMBL3884113 IC50 > 10000.0 nM -
CHEMBL3885482 IC50 > 10000.0 nM -
CHEMBL3883580 IC50 > 10000.0 nM -
CHEMBL3885267 IC50 > 10000.0 nM -
CHEMBL269538 HARMINE IC50 > 10000.0 nM -
CHEMBL3883356 IC50 > 10000.0 nM -
CHEMBL3884764 IC50 > 10000.0 nM -
CHEMBL3885315 IC50 - -
CHEMBL3884250 IC50 > 10000.0 nM -
CHEMBL3883943 IC50 > 10000.0 nM -
CHEMBL3885043 IC50 > 10000.0 nM -
CHEMBL3884086 IC50 > 10000.0 nM -
CHEMBL3751934 IC50 > 10000.0 nM -
CHEMBL3753970 IC50 > 10000.0 nM -
CHEMBL3754608 IC50 > 10000.0 nM -
CHEMBL3753782 IC50 > 10000.0 nM -
CHEMBL3884027 IC50 > 10000.0 nM -
CHEMBL3885092 IC50 > 10000.0 nM -
CHEMBL3884241 IC50 > 10000.0 nM -
CHEMBL3884570 IC50 > 10000.0 nM -
CHEMBL3885333 IC50 > 10000.0 nM -
CHEMBL3884031 IC50 > 10000.0 nM -
CHEMBL3883813 IC50 > 10000.0 nM -
CHEMBL3885036 IC50 > 10000.0 nM -
CHEMBL3883541 IC50 > 10000.0 nM -
CHEMBL3883414 IC50 > 10000.0 nM -
CHEMBL3883458 IC50 > 10000.0 nM -
CHEMBL3885316 IC50 > 10000.0 nM -