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Compound Detail

CHEMBL4645503

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C=CC(=O)Nc1ccc(C(=O)N2CCC[C@@H](Nc3ncc(Cl)c(SCc4ncc(C(C)(C)C)o4)n3)C2)cc1

Basic Information

ChEMBL ID CHEMBL4645503
Phase Preclinical
Structure Type MOL
InChI Key PUZGAVMGSWIMSU-LJQANCHMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

555.1
MW (Da)
5.55
ALogP
8
HBA
2
HBD
113.2
PSA (Ų)
0.21
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31ClN6O3S
MW 555.10
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.69

Activity Summary

IC50 1 meas. best 5.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK7/Cyclin H/MNAT1
CHEMBL3038473
IC50 5.29 5.29 5120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK7/Cyclin H/MNAT1 IC50 = 5120.0 nM 5.29 Inhibition of recombinant human full-length His-tagged CDK7/Cyclin H/MNAT1 expre... 32502343

Literature References

PubMed DOI Target Context # Activities
32502343 10.1021/acs.jmedchem.9b01929 CDK2/Cyclin A1 1
32502343 10.1021/acs.jmedchem.9b01929 CDK7/Cyclin H/MNAT1 1
32502343 10.1021/acs.jmedchem.9b01929 CDK9/cyclin T1 1
32502343 10.1021/acs.jmedchem.9b01929 Cyclin-dependent kinase 12/13 1

Data from ChEMBL 36 via Core Engine