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Compound Detail

CHEMBL1241134

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CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(N)=O

Basic Information

ChEMBL ID CHEMBL1241134
Phase Preclinical
Structure Type BOTH
InChI Key AAWZQALNAHGICT-VUBDRERZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

721.8
MW (Da)
-3.43
ALogP
9
HBA
13
HBD
352.4
PSA (Ų)
0.03
QED
2
Ro5 Violations
23
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H52FN13O6
MW 721.84
Aromatic Rings 1
Heavy Atoms 51
NP-Likeness 0.02

Activity Summary

IC50 2 meas. best 6.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-A2
CHEMBL2582
IC50 6.28 6.28 530.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 5.14 5.14 7200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-A2 IC50 = 530.0 nM 6.28 Binding affinity to Cyclin A by competitive binding assay 16584130
Cyclin-dependent kinase 2/cyclin A IC50 = 7200.0 nM 5.14 Inhibition of CDK2/cyclin A 16584130

Literature References

PubMed DOI Target Context # Activities
16584130 10.1208/aapsj080125 Cyclin-A2 1
16584130 10.1208/aapsj080125 Cyclin-dependent kinase 2/cyclin A 1

Data from ChEMBL 36 via Core Engine