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Compound Detail

CHEMBL3393782

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Cc1nc(C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@H](CC(=O)N(C)[C@@H](Cc2ccccc2)C(N)=O)CC(C)C)nn1-c1cc(Cl)cc(Cl)c1

Basic Information

ChEMBL ID CHEMBL3393782
Phase Preclinical
Structure Type MOL
InChI Key POIGRZXVXQDGIF-URORMMCBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

716.7
MW (Da)
2.91
ALogP
8
HBA
5
HBD
207.4
PSA (Ų)
0.13
QED
1
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H43Cl2N9O5
MW 716.67
Aromatic Rings 3
Heavy Atoms 49
NP-Likeness -0.86

Activity Summary

IC50 1 meas. best 4.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK2/Cyclin A2
CHEMBL3038469
IC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK2/Cyclin A2 IC50 = 100000.0 nM 4.0 Inhibition of human recombinant CDK2/Cyclin A using fluoresceinyl-Ahx-Pro-Val-Ly... 25454794

Literature References

PubMed DOI Target Context # Activities
25454794 10.1021/jm5015023 DU-145 1
25454794 10.1021/jm5015023 U2OS 1
25454794 10.1021/jm5015023 Cyclin-dependent kinase 4/cyclin D1 1
25454794 10.1021/jm5015023 CDK2/Cyclin A2 1

Data from ChEMBL 36 via Core Engine