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Compound Detail

CHEMBL1241935

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CC1(C)CC2(C)Nc3cc(-c4ccc5c(c4)NC4(C)CC(C)(C)NC(=S)N54)ccc3N2C(=S)N1

Basic Information

ChEMBL ID CHEMBL1241935
Phase Preclinical
Structure Type MOL
InChI Key YRCQSKRHPCULTG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

492.7
MW (Da)
5.36
ALogP
4
HBA
4
HBD
54.6
PSA (Ų)
0.40
QED
1
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H32N6S2
MW 492.72
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.17

Activity Summary

IC50 2 meas. best 5.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 1
CHEMBL308
IC50 5.3 5.3 5000.0 1
Cyclin-dependent kinase 5
CHEMBL4036
IC50 4.6 4.6 25000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 1 IC50 = 5000.0 nM 5.3 Inhibition of CDK1 16584130
Cyclin-dependent kinase 5 IC50 = 25000.0 nM 4.6 Inhibition of CDK5 16584130

Literature References

PubMed DOI Target Context # Activities
16584130 10.1208/aapsj080125 Cyclin-dependent kinase 5 1
16584130 10.1208/aapsj080125 Cyclin-dependent kinase 1 1

Data from ChEMBL 36 via Core Engine