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Compound Detail

CHEMBL576978

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COC(=O)[C@@H](CC(C)C)NC(=O)O[C@@H]1CC[C@]2(CO2)[C@H]([C@@]2(C)O[C@@H]2CC=C(C)C)[C@@H]1OC

Basic Information

ChEMBL ID CHEMBL576978
Phase Preclinical
Structure Type MOL
InChI Key VQEZAFGBHLSOAM-FRTLKMCASA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

453.6
MW (Da)
3.38
ALogP
7
HBA
1
HBD
98.9
PSA (Ų)
0.32
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H39NO7
MW 453.58
Aromatic Rings 0
Heavy Atoms 32
NP-Likeness 2.14

Activity Summary

IC50 2 meas. best 10.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HUVEC
CHEMBL613979
IC50 10.42 10.42 0.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 9.93 9.93 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HUVEC IC50 = 0.038 nM 10.42 Antiproliferative activity against HUVEC after 72 hrs by MTT assay 19929003
NON-PROTEIN TARGET IC50 = 0.118 nM 9.93 Antiproliferative activity against BAEC 19929003

Literature References

PubMed DOI Target Context # Activities
19929003 10.1021/jm901260k Rattus norvegicus 2
19929003 10.1021/jm901260k NON-PROTEIN TARGET 1
19929003 10.1021/jm901260k HUVEC 1
19929003 10.1021/jm901260k Methionine aminopeptidase 2 1

Data from ChEMBL 36 via Core Engine