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Assay Detail

CHEMBL4041957

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

Binding
Inhibition of human recombinant CDK5/p25 after 30 mins by [gamma-33P]ATP based scintillation counting analysis
60
Total Activities
60
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

Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.
Bendjeddou LZ, Loaëc N, Villiers B, Prina E, Späth GF, Galons H, Meijer L, Oumata N.
Eur J Med Chem (2017) 125 : 696 -709
PubMed 27721154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 5.61 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061526 1 6.72
CHEMBL4102871 1 6.66
CHEMBL4074499 1 6.41
CHEMBL4093104 1 6.32
CHEMBL4070227 1 6.23
CHEMBL4097368 1 6.23
CHEMBL4105084 1 6.21
CHEMBL4069158 1 6.12
CHEMBL4076448 1 6.09
CHEMBL4089652 1 6.09
CHEMBL4070189 1 6.05
CHEMBL4065432 1 6.00
CHEMBL4092673 1 5.96
CHEMBL4071322 1 5.96
CHEMBL4062820 1 5.92
CHEMBL4074132 1 5.85
CHEMBL4100956 1 5.77
CHEMBL4072506 1 5.75
CHEMBL4092047 1 5.66
CHEMBL4090770 1 5.51
CHEMBL4088717 1 5.42
CHEMBL4090223 1 5.38
CHEMBL4076906 1 5.33
CHEMBL4070065 1 5.33
CHEMBL4079347 1 5.29
CHEMBL4084364 1 5.29
CHEMBL4071413 1 5.21
CHEMBL4091942 1 5.17
CHEMBL4061394 1 5.17
CHEMBL4104296 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061526 IC50 = 190.0 nM 6.72
CHEMBL4102871 IC50 = 220.0 nM 6.66
CHEMBL4074499 IC50 = 390.0 nM 6.41
CHEMBL4093104 IC50 = 480.0 nM 6.32
CHEMBL4070227 IC50 = 590.0 nM 6.23
CHEMBL4097368 IC50 = 590.0 nM 6.23
CHEMBL4105084 IC50 = 610.0 nM 6.21
CHEMBL4069158 IC50 = 750.0 nM 6.12
CHEMBL4076448 IC50 = 820.0 nM 6.09
CHEMBL4089652 IC50 = 820.0 nM 6.09
CHEMBL4070189 IC50 = 890.0 nM 6.05
CHEMBL4065432 IC50 = 1000.0 nM 6.00
CHEMBL4071322 IC50 = 1100.0 nM 5.96
CHEMBL4092673 IC50 = 1100.0 nM 5.96
CHEMBL4062820 IC50 = 1200.0 nM 5.92
CHEMBL4074132 IC50 = 1400.0 nM 5.85
CHEMBL4100956 IC50 = 1700.0 nM 5.77
CHEMBL4072506 IC50 = 1800.0 nM 5.75
CHEMBL4092047 IC50 = 2200.0 nM 5.66
CHEMBL4090770 IC50 = 3100.0 nM 5.51
CHEMBL4088717 IC50 = 3800.0 nM 5.42
CHEMBL4090223 IC50 = 4200.0 nM 5.38
CHEMBL4076906 IC50 = 4700.0 nM 5.33
CHEMBL4070065 IC50 = 4700.0 nM 5.33
CHEMBL4084364 IC50 = 5100.0 nM 5.29
CHEMBL4079347 IC50 = 5100.0 nM 5.29
CHEMBL4071413 IC50 = 6100.0 nM 5.21
CHEMBL4091942 IC50 = 6700.0 nM 5.17
CHEMBL4061394 IC50 = 6800.0 nM 5.17
CHEMBL4104296 IC50 = 7100.0 nM 5.15
CHEMBL4082981 IC50 = 8300.0 nM 5.08
CHEMBL4067477 IC50 = 17000.0 nM 4.77
CHEMBL4098107 IC50 = 18000.0 nM 4.75
CHEMBL4089542 IC50 = 29000.0 nM 4.54
CHEMBL4086402 IC50 = 50000.0 nM 4.30
CHEMBL4087260 IC50 = 71000.0 nM 4.15
CHEMBL4098237 IC50 > 10000.0 nM -
CHEMBL4083948 IC50 > 10000.0 nM -
CHEMBL4075509 IC50 > 10000.0 nM -
CHEMBL4071013 IC50 > 10000.0 nM -
CHEMBL4064988 IC50 > 10000.0 nM -
CHEMBL4091127 IC50 > 10000.0 nM -
CHEMBL4067420 IC50 > 10000.0 nM -
CHEMBL4062568 IC50 > 10000.0 nM -
CHEMBL4077125 IC50 > 10000.0 nM -
CHEMBL4063254 IC50 > 10000.0 nM -
CHEMBL4079343 IC50 > 10000.0 nM -
CHEMBL4062683 IC50 > 10000.0 nM -
CHEMBL4084919 IC50 > 10000.0 nM -
CHEMBL4076663 IC50 > 10000.0 nM -