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Compound Detail

CHEMBL5723323

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CC(C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@H](C=O)CC(=O)O.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL5723323
Phase Preclinical
Structure Type MOL
InChI Key YLSRAFBNEHVRLB-PGKYVIAHSA-N
Parent Compound CHEMBL6070851
Active Moiety CHEMBL6070851
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

516.5
MW (Da)
-0.45
ALogP
8
HBA
6
HBD
217.3
PSA (Ų)
0.16
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H37F3N4O12
MW 630.57
Aromatic Rings 0
Heavy Atoms 36
NP-Likeness 0.26

Activity Summary

Ki 4 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Caspase-8
CHEMBL3776
Ki 8.8 8.8 1.6 1
Caspase-3
CHEMBL2334
Ki 7.38 7.38 42.0 1
Caspase-9
CHEMBL2273
Ki 7.32 7.32 48.0 1
Caspase-6
CHEMBL3308
Ki 7.28 7.28 52.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724709 HEK-293T 2
- 10.6019/CHEMBL5724709 U2OS 2
- 10.6019/CHEMBL5724709 Fibroblast 2
- 10.6019/CHEMBL5724796 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5724796 Bromodomain-containing protein 4 1
- 10.6019/CHEMBL5724796 Transcription intermediary factor 1-alpha 1
- 10.6019/CHEMBL5724796 Peregrin 1
- 10.6019/CHEMBL5724796 Fibroblast growth factor receptor 2 1
- 10.6019/CHEMBL5724796 Tyrosine-protein kinase ABL1 1
- 10.6019/CHEMBL5724796 Aurora kinase A 1
- 10.6019/CHEMBL5724796 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5724796 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5723035 Caspase-1 1
- 10.6019/CHEMBL5724796 Casein kinase I isoform delta 1
- 10.6019/CHEMBL5723035 Caspase-9 1
- 10.6019/CHEMBL5723035 Caspase-8 1
- 10.6019/CHEMBL5723035 Caspase-6 1
- 10.6019/CHEMBL5723035 Caspase-3 1

Data from ChEMBL 36 via Core Engine