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Compound Detail

CHEMBL5193697

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CC(=O)Nc1ccc(NC(=O)c2cncc(-c3ccc(C(=O)N4CCNCC4)cc3)c2)cc1

Basic Information

ChEMBL ID CHEMBL5193697
Phase Preclinical
Structure Type MOL
InChI Key YWGNVCOZCXFVOR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

443.5
MW (Da)
3.00
ALogP
5
HBA
3
HBD
103.4
PSA (Ų)
0.56
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25N5O3
MW 443.51
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.36

Activity Summary

IC50 1 meas. best 5.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK8/Cyclin C
CHEMBL3038474
IC50 5.98 5.98 1050.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK8/Cyclin C IC50 = 1050.0 nM 5.98 Inhibition of recombinant full length His tagged human CDK8/Cyclin C expressed i... 35536548

Literature References

PubMed DOI Target Context # Activities
35536548 10.1021/acs.jmedchem.2c00356 CDK8/Cyclin C 2
35536548 10.1021/acs.jmedchem.2c00356 BMDC 1
35536548 10.1021/acs.jmedchem.2c00356 Unchecked 1

Data from ChEMBL 36 via Core Engine