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Compound Detail

CHEMBL5591253

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CN[C@@H](C)C(=O)N[C@H](C(=O)N1C[C@H](NC(=O)c2cnc(N3CCN(CCCOc4cc5ncnc(Nc6n[nH]c(C)c6C)c5cc4S(=O)(=O)C(C)(C)C)CC3)cn2)C[C@@H]1C(=O)Nc1c(F)cccc1F)C(C)(C)C

Basic Information

ChEMBL ID CHEMBL5591253
Phase Preclinical
Structure Type MOL
InChI Key CHNBEZLJAQUZEX-BPYLYCJUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

1045.2
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C50H66F2N14O7S
MW 1045.23

Activity Summary

IC50 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 12
CHEMBL3559692
IC50 8.0 8.0 10.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 12 IC50 = 10.0 nM 8.0 Inhibition of CDK12 (unknown origin) 39149114

Literature References

PubMed DOI Target Context # Activities
39149114 10.1039/d4md00142g Cyclin-dependent kinase 12 1

Data from ChEMBL 36 via Core Engine