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Compound Detail

CHEMBL32568

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COc1cc([C@@H]2c3cc4c(cc3[C@@H](Oc3ccc(F)cc3)[C@H]3COC(=O)[C@H]23)OCO4)cc(OC)c1O

Basic Information

ChEMBL ID CHEMBL32568
Phase Preclinical
Structure Type MOL
InChI Key UMMMPHSPVYALOO-DLTDCEFJSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

494.5
MW (Da)
4.33
ALogP
8
HBA
1
HBD
92.7
PSA (Ų)
0.52
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23FO8
MW 494.47
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness 1.02

Activity Summary

EC50 1 meas. best 6.35
IC50 1 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
H9
CHEMBL614806
EC50 6.35 6.35 450.0 1
H9
CHEMBL614806
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
H9 EC50 = 450.0 nM 6.35 Evaluation for anti-HIV activity using T cell line (H9). -
H9 IC50 = 800.0 nM 6.1 Cytotoxicity against H9 cell line -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)10108-1 H9 2
1331331 10.1021/np50086a011 DNA topoisomerase 2-alpha 2
8691468 10.1021/jm9503052 DNA topoisomerase II 1
- 10.1016/S0960-894X(97)10108-1 ADMET 1
2167985 10.1021/jm00171a050 ADMET 1
2167985 10.1021/jm00171a050 DNA topoisomerase II 1
2167985 10.1021/jm00171a050 Nucleic Acid 1
12014968 10.1021/jm0105427 DNA topoisomerase II 1
1331331 10.1021/np50086a011 KB 1

Data from ChEMBL 36 via Core Engine