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Compound Detail

CHEMBL4105437

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COc1ccc2c(c1)c(CC(=O)O[C@H]1c3cc4c(cc3[C@@H](c3cc(OC)c(OC)c(OC)c3)[C@H]3C(=O)OC[C@@H]31)OCO4)c(C)n2C(=O)c1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL4105437
Phase Preclinical
Structure Type MOL
InChI Key RIWQYRZCIUKJGO-XGABHMDESA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

754.2
MW (Da)
6.82
ALogP
12
HBA
0
HBD
130.0
PSA (Ų)
0.15
QED
3
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H36ClNO11
MW 754.19
Aromatic Rings 5
Heavy Atoms 54
NP-Likeness 0.49

Activity Summary

IC50 4 meas. best 5.73

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L02
CHEMBL4296457
IC50 5.73 5.73 1858.0 1
Bel7402/5-FU
CHEMBL4483230
IC50 5.67 5.67 2159.0 1
Bel-7402
CHEMBL614279
IC50 5.23 5.23 5870.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28301815 10.1016/j.ejmech.2017.03.011 Bel7402/5-FU 31
28301815 10.1016/j.ejmech.2017.03.011 Bel-7402 1
28301815 10.1016/j.ejmech.2017.03.011 Unchecked 1
28301815 10.1016/j.ejmech.2017.03.011 L02 1
28301815 10.1016/j.ejmech.2017.03.011 Mitogen-activated protein kinase; ERK1/ERK2 1
28301815 10.1016/j.ejmech.2017.03.011 Signal transducer and activator of transcription 3 1
28301815 10.1016/j.ejmech.2017.03.011 RAC-alpha serine/threonine-protein kinase 1
38107170 10.1039/d3md00560g Bel-7402 1

Data from ChEMBL 36 via Core Engine