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Assay Detail

CHEMBL829527

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

Binding
Inhibition of [32P]ATP binding to Cyclin dependent kinase 2-cyclin E
33
Total Activities
33
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 2/cyclin E (CHEMBL2094126)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.
VanderWel SN, Harvey PJ, McNamara DJ, Repine JT, Keller PR, Quin J, Booth RJ, Elliott WL, Dobrusin EM, Fry DW, Toogood PL.
J Med Chem (2005) 48 : 2371 -2387
PubMed 15801830 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.40 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358057 1 7.41
CHEMBL364317 1 7.10
CHEMBL191046 1 7.07
CHEMBL372207 1 6.61
CHEMBL190460 1 6.44
CHEMBL189937 1 6.02
CHEMBL370237 1 5.82
CHEMBL192945 1 5.78
CHEMBL344812 1 5.34
CHEMBL190303 1 -
CHEMBL440028 1 -
CHEMBL189980 1 -
CHEMBL191617 1 -
CHEMBL364473 1 -
CHEMBL190072 1 -
CHEMBL428630 1 -
CHEMBL192803 1 -
CHEMBL190455 1 -
CHEMBL360675 1 -
CHEMBL426997 1 -
CHEMBL191839 1 -
CHEMBL190685 1 -
CHEMBL190664 1 -
CHEMBL192059 1 -
CHEMBL370976 1 -
CHEMBL190200 1 -
CHEMBL190096 1 -
CHEMBL365847 1 -
CHEMBL192641 1 -
CHEMBL426818 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358057 IC50 = 39.0 nM 7.41
CHEMBL364317 IC50 = 80.0 nM 7.10
CHEMBL191046 IC50 = 85.0 nM 7.07
CHEMBL372207 IC50 = 246.0 nM 6.61
CHEMBL190460 IC50 = 365.0 nM 6.44
CHEMBL189937 IC50 = 950.0 nM 6.02
CHEMBL370237 IC50 = 1500.0 nM 5.82
CHEMBL192945 IC50 = 1650.0 nM 5.78
CHEMBL344812 IC50 = 4550.0 nM 5.34
CHEMBL440028 IC50 > 5000.0 nM -
CHEMBL190684 IC50 > 5000.0 nM -
CHEMBL189980 IC50 > 5000.0 nM -
CHEMBL191617 IC50 > 5000.0 nM -
CHEMBL364473 IC50 > 5000.0 nM -
CHEMBL190072 IC50 > 5000.0 nM -
CHEMBL428630 IC50 > 5000.0 nM -
CHEMBL192803 IC50 > 5000.0 nM -
CHEMBL190455 IC50 > 5000.0 nM -
CHEMBL360675 IC50 > 5000.0 nM -
CHEMBL189956 IC50 > 5000.0 nM -
CHEMBL189849 IC50 > 5000.0 nM -
CHEMBL190303 IC50 > 5000.0 nM -
CHEMBL426997 IC50 > 5000.0 nM -
CHEMBL191839 IC50 > 5000.0 nM -
CHEMBL190685 IC50 > 5000.0 nM -
CHEMBL190664 IC50 > 5000.0 nM -
CHEMBL192059 IC50 > 5000.0 nM -
CHEMBL370976 IC50 > 5000.0 nM -
CHEMBL190200 IC50 > 5000.0 nM -
CHEMBL190096 IC50 > 5000.0 nM -
CHEMBL365847 IC50 - nM -
CHEMBL192641 IC50 > 5000.0 nM -
CHEMBL426818 IC50 > 5000.0 nM -