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Compound Detail

CHEMBL4757140

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C=C[C@@]1(C)C=C(C)[C@@H]2[C@@H]3[C@H](Oc4ccc(cc4)C[C@@H]4C(=O)NC(=O)[C@@H]4C(=O)[C@H]31)[C@@H]1[C@@H](C)C[C@@H](C)C[C@]12C

Basic Information

ChEMBL ID CHEMBL4757140
Phase Preclinical
Structure Type MOL
InChI Key GAPPHVJLWSRLAC-VBMKUXCYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

501.7
MW (Da)
5.15
ALogP
4
HBA
1
HBD
72.5
PSA (Ų)
0.33
QED
2
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C32H39NO4
MW 501.67
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness 2.31

Activity Summary

IC50 6 meas. best 5.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein phosphatase C
CHEMBL3243
IC50 5.09 5.09 8100.0 1
A549
CHEMBL392
IC50 4.99 4.99 10300.0 1
Tyrosine-protein phosphatase non-receptor type 2
CHEMBL3807
IC50 4.85 4.85 14000.0 1
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
IC50 4.6 4.6 25000.0 1
NCI-H157
CHEMBL614783
IC50 4.42 4.42 38500.0 1
NCI-H1975
CHEMBL614348
IC50 4.12 4.12 75000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33691166 10.1016/j.bmcl.2021.127915 NCI-H157 2
33691166 10.1016/j.bmcl.2021.127915 A549 2
35930265 10.1021/acs.jnatprod.2c00473 Staphylococcus aureus 2
35930265 10.1021/acs.jnatprod.2c00473 Receptor-type tyrosine-protein phosphatase C 1
35930265 10.1021/acs.jnatprod.2c00473 Tyrosine-protein phosphatase non-receptor type 1 1
35930265 10.1021/acs.jnatprod.2c00473 Tyrosine-protein phosphatase non-receptor type 2 1
35930265 10.1021/acs.jnatprod.2c00473 Receptor-type tyrosine-protein phosphatase F 1
35930265 10.1021/acs.jnatprod.2c00473 NCI-H1975 1
35930265 10.1021/acs.jnatprod.2c00473 Bacillus subtilis 1
35930265 10.1021/acs.jnatprod.2c00473 Bacillus amyloliquefaciens 1
35930265 10.1021/acs.jnatprod.2c00473 Escherichia coli 1
35930265 10.1021/acs.jnatprod.2c00473 Streptococcus agalactiae 1

Data from ChEMBL 36 via Core Engine