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Compound Detail

CHEMBL331086

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COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CNC(=O)OCc1ccc(OC(=O)CCOCCOCCO)cc1)C[C@@H]3OC1CC(N)C(O)C(C)O1

Basic Information

ChEMBL ID CHEMBL331086
Phase Preclinical
Structure Type MOL
InChI Key JEYJRMMVJFMYPM-BBVQXZGQSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

852.8
MW (Da)
1.26
ALogP
18
HBA
7
HBD
289.2
PSA (Ų)
0.03
QED
3
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H48N2O17
MW 852.84
Aromatic Rings 3
Heavy Atoms 61
NP-Likeness 0.83

Activity Summary

IC50 1 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P388
CHEMBL389
IC50 8.1 8.1 8.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 24.0 hr -
T1/2 0.4 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P388 IC50 = 8.0 nM 8.1 Compound was evaluated for cytotoxicity against P388 leukemia cell line. 10479297

Literature References

PubMed DOI Target Context # Activities
10479297 10.1021/jm990166e Mus musculus 2
10479297 10.1021/jm990166e ADMET 1
10479297 10.1021/jm990166e Rattus norvegicus 1
10479297 10.1021/jm990166e P388 1

Data from ChEMBL 36 via Core Engine