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Assay Detail

CHEMBL4434176

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

Binding
Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assay
100
Total Activities
100
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 14/Cyclin-Y (CHEMBL4296115)
Type PROTEIN COMPLEX
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 100 7.21 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4563703 1 9.40
CHEMBL4535078 1 9.10
CHEMBL4446451 1 8.80
CHEMBL4522598 1 8.74
CHEMBL4515515 1 8.59
CHEMBL4530961 1 8.52
CHEMBL4542127 1 8.52
CHEMBL4527767 1 8.47
CHEMBL4579572 1 8.19
CHEMBL4519165 1 8.00
CHEMBL4456492 1 7.96
CHEMBL4563705 1 7.85
CHEMBL4459422 1 7.85
CHEMBL4555069 1 7.77
CHEMBL445813 AT-7519 2.0 1 7.70
CHEMBL4589122 1 7.57
CHEMBL4473682 1 7.47
CHEMBL4584359 1 7.39
CHEMBL4554744 1 7.35
CHEMBL4576258 1 7.35
CHEMBL4544087 1 7.32
CHEMBL4474689 1 7.31
CHEMBL4464758 1 7.30
CHEMBL4586749 1 7.21
CHEMBL4583677 1 7.17
CHEMBL4466362 1 7.14
CHEMBL4459085 1 7.11
CHEMBL4447871 1 7.09
CHEMBL4466865 1 7.09
CHEMBL4556640 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4563703 IC50 = 0.4 nM 9.40
CHEMBL4535078 IC50 = 0.8 nM 9.10
CHEMBL4446451 IC50 = 1.6 nM 8.80
CHEMBL4522598 IC50 = 1.8 nM 8.74
CHEMBL4515515 IC50 = 2.6 nM 8.59
CHEMBL4530961 IC50 = 3.0 nM 8.52
CHEMBL4542127 IC50 = 3.0 nM 8.52
CHEMBL4527767 IC50 = 3.4 nM 8.47
CHEMBL4579572 IC50 = 6.4 nM 8.19
CHEMBL4519165 IC50 = 10.0 nM 8.00
CHEMBL4456492 IC50 = 11.0 nM 7.96
CHEMBL4563705 IC50 = 14.0 nM 7.85
CHEMBL4459422 IC50 = 14.0 nM 7.85
CHEMBL4555069 IC50 = 17.0 nM 7.77
CHEMBL445813 AT-7519 IC50 = 19.8 nM 7.70
CHEMBL4589122 IC50 = 27.0 nM 7.57
CHEMBL4473682 IC50 = 34.0 nM 7.47
CHEMBL4584359 IC50 = 41.0 nM 7.39
CHEMBL4554744 IC50 = 45.0 nM 7.35
CHEMBL4576258 IC50 = 45.0 nM 7.35
CHEMBL4544087 IC50 = 48.0 nM 7.32
CHEMBL4474689 IC50 = 49.0 nM 7.31
CHEMBL4464758 IC50 = 50.0 nM 7.30
CHEMBL4586749 IC50 = 62.0 nM 7.21
CHEMBL4583677 IC50 = 68.0 nM 7.17
CHEMBL4466362 IC50 = 72.0 nM 7.14
CHEMBL4459085 IC50 = 77.0 nM 7.11
CHEMBL4447871 IC50 = 82.0 nM 7.09
CHEMBL4466865 IC50 = 82.0 nM 7.09
CHEMBL4556640 IC50 = 83.0 nM 7.08
CHEMBL4435761 IC50 = 88.0 nM 7.06
CHEMBL4434727 IC50 = 88.0 nM 7.06
CHEMBL4536978 IC50 = 108.0 nM 6.97
CHEMBL4561411 IC50 = 117.0 nM 6.93
CHEMBL4444448 IC50 = 126.0 nM 6.90
CHEMBL4531892 IC50 = 148.0 nM 6.83
CHEMBL4439068 IC50 = 151.0 nM 6.82
CHEMBL4461471 IC50 = 154.0 nM 6.81
CHEMBL4461838 IC50 = 169.0 nM 6.77
CHEMBL4570828 IC50 = 183.0 nM 6.74
CHEMBL4468007 IC50 = 208.0 nM 6.68
CHEMBL4464414 IC50 = 221.0 nM 6.66
CHEMBL4527939 IC50 = 218.0 nM 6.66
CHEMBL4459908 IC50 = 257.0 nM 6.59
CHEMBL4453025 IC50 = 267.0 nM 6.57
CHEMBL4446588 IC50 = 282.0 nM 6.55
CHEMBL4453129 IC50 = 308.0 nM 6.51
CHEMBL4447917 IC50 = 308.0 nM 6.51
CHEMBL4451930 IC50 = 315.0 nM 6.50
CHEMBL4543386 IC50 = 332.0 nM 6.48