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Compound Detail

CHEMBL4243000

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CC(C)C[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O

Basic Information

ChEMBL ID CHEMBL4243000
Phase Preclinical
Structure Type MOL
InChI Key JQUZDQQKHRFDRA-DKTXOJPGSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

979.2
MW (Da)
-3.21
ALogP
14
HBA
15
HBD
403.7
PSA (Ų)
0.02
QED
3
Ro5 Violations
29
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H70N12O12S
MW 979.17
Aromatic Rings 1
Heavy Atoms 68
NP-Likeness 0.20

Activity Summary

IC50 3 meas. best 6.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
2008
CHEMBL612818
IC50 6.02 6.02 960.0 1
C13
CHEMBL614863
IC50 5.45 5.45 3550.0 1
IGROV-1
CHEMBL613984
IC50 5.37 5.37 4320.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
2008 IC50 = 960.0 nM 6.02 Cytotoxicity against human 2008 cells 30035541
C13 IC50 = 3550.0 nM 5.45 Cytotoxicity against human C13 cells after 72 hrs 30035541
IGROV-1 IC50 = 4320.0 nM 5.37 Cytotoxicity against human IGROV1 cells after 72 hrs 30035541

Literature References

Data from ChEMBL 36 via Core Engine