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Assay Detail

CHEMBL4434178

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

Binding
Inhibition of FLAG-tagged CDK14 (unknown origin) expressed in human HEK293 cells assessed as blocking of CDK14 pulldown incubated for 4 hrs by biotinylated JNK-IN- based pull down assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 14 (CHEMBL6162)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.
Ferguson FM, Doctor ZM, Ficarro SB, Marto JA, Kim ND, Sim T, Gray NS.
Bioorg Med Chem Lett (2019) 29 : 1985 -1993
PubMed 31175010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.40 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4522598 1 7.30
CHEMBL4542127 1 7.30
CHEMBL4554744 1 6.30
CHEMBL4534124 1 6.30
CHEMBL4522564 1 6.00
CHEMBL4555069 1 6.00
CHEMBL4589122 1 6.00
CHEMBL4530961 1 6.00
CHEMBL4456492 1 -
CHEMBL4584359 1 -
CHEMBL4466865 1 -
CHEMBL4464758 1 -
CHEMBL4434727 1 -
CHEMBL4544087 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4522598 IC50 = 50.0 nM 7.30
CHEMBL4542127 IC50 = 50.0 nM 7.30
CHEMBL4554744 IC50 = 500.0 nM 6.30
CHEMBL4534124 IC50 = 500.0 nM 6.30
CHEMBL4522564 IC50 = 1000.0 nM 6.00
CHEMBL4555069 IC50 = 1000.0 nM 6.00
CHEMBL4589122 IC50 = 1000.0 nM 6.00
CHEMBL4530961 IC50 = 1000.0 nM 6.00
CHEMBL4456492 IC50 > 1000.0 nM -
CHEMBL4584359 IC50 > 1000.0 nM -
CHEMBL4466865 IC50 > 1000.0 nM -
CHEMBL4464758 IC50 > 1000.0 nM -
CHEMBL4434727 IC50 >= 500.0 nM -
CHEMBL4544087 IC50 > 1000.0 nM -