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Assay Detail

CHEMBL4742549

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

Binding
Binding affinity to DNA-tagged CDK-12 expressed in HEK293 cells (unknown origin) by qPCR analysis
25
Total Activities
18
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 12 (CHEMBL3559692)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted Pyrazole Derivatives As Selective CDK12/13 Inhibitors
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 25 7.60 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4781207 3 7.60
CHEMBL4781668 3 7.60
CHEMBL4779066 2 7.60
CHEMBL4779633 1 7.60
CHEMBL4800324 1 7.60
CHEMBL4778361 3 7.60
CHEMBL4778214 1 7.60
CHEMBL4777358 1 7.60
CHEMBL4788447 1 -
CHEMBL4786663 1 -
CHEMBL4781396 1 -
CHEMBL4799698 1 -
CHEMBL4788085 1 -
CHEMBL4787409 1 -
CHEMBL4785443 1 -
CHEMBL4790705 1 -
CHEMBL4800122 1 -
CHEMBL4790458 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4778214 Kd = 25.0 nM 7.60
CHEMBL4781207 Kd = 25.0 nM 7.60
CHEMBL4778361 Kd = 25.0 nM 7.60
CHEMBL4800324 Kd = 25.0 nM 7.60
CHEMBL4779633 Kd = 25.0 nM 7.60
CHEMBL4779066 Kd = 25.0 nM 7.60
CHEMBL4781668 Kd = 25.0 nM 7.60
CHEMBL4777358 Kd = 25.0 nM 7.60
CHEMBL4799698 Kd > 100.0 nM -
CHEMBL4778361 Kd < 25.0 nM -
CHEMBL4778361 Kd < 25.0 nM -
CHEMBL4790458 Kd > 100.0 nM -
CHEMBL4779066 Kd < 25.0 nM -
CHEMBL4800122 Kd < 25.0 nM -
CHEMBL4790705 Kd < 25.0 nM -
CHEMBL4785443 Kd < 25.0 nM -
CHEMBL4787409 Kd < 25.0 nM -
CHEMBL4788085 Kd < 25.0 nM -
CHEMBL4781668 Kd > 100.0 nM -
CHEMBL4781668 Kd > 100.0 nM -
CHEMBL4781396 Kd < 25.0 nM -
CHEMBL4786663 Kd < 25.0 nM -
CHEMBL4788447 Kd < 25.0 nM -
CHEMBL4781207 Kd < 25.0 nM -
CHEMBL4781207 Kd < 25.0 nM -