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Compound Detail

CHEMBL1241136

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

Basic Information

ChEMBL ID CHEMBL1241136
Phase Preclinical
Structure Type BOTH
InChI Key FHDYESQEQLMXSO-KTHKBMNISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

721.9
MW (Da)
-1.08
ALogP
8
HBA
11
HBD
302.5
PSA (Ų)
0.04
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 C33H56FN11O6
MW 721.88
Aromatic Rings 1
Heavy Atoms 51
NP-Likeness -0.07

Activity Summary

IC50 2 meas. best 6.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 6.28 6.28 520.0 1
Cyclin-A2
CHEMBL2582
IC50 6.23 6.23 590.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2/cyclin A IC50 = 520.0 nM 6.28 Inhibition of CDK2/cyclin A 16584130
Cyclin-A2 IC50 = 590.0 nM 6.23 Binding affinity to Cyclin A by competitive binding assay 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