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Compound Detail

CHEMBL5181027

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C=C[C@@]1(C)C=C(C)[C@@H]2[C@@H]3[C@@H](Oc4ccc(cc4)C[C@@]4(O)C/C(=C(/O)[C@H]31)C(=O)N4)[C@@H]1[C@@H](C)C[C@@H](C)C[C@]12C

Basic Information

ChEMBL ID CHEMBL5181027
Phase Preclinical
Structure Type MOL
InChI Key RHWUVEFQIICMCY-LWZBBKNSSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

503.7
MW (Da)
5.71
ALogP
4
HBA
3
HBD
78.8
PSA (Ų)
0.43
QED
2
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H41NO4
MW 503.68
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness 2.10

Activity Summary

IC50 5 meas. best 4.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NCI-H1975
CHEMBL614348
IC50 4.14 4.14 72000.0 1
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
IC50 4.05 4.05 89000.0 1
Tyrosine-protein phosphatase non-receptor type 2
CHEMBL3807
IC50 4.04 4.04 92000.0 1
Tyrosine-protein phosphatase non-receptor type 6
CHEMBL3166
IC50 4.0 4.0 100000.0 1
Receptor-type tyrosine-protein phosphatase C
CHEMBL3243
IC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35930265 10.1021/acs.jnatprod.2c00473 Staphylococcus aureus 2
35930265 10.1021/acs.jnatprod.2c00473 Tyrosine-protein phosphatase non-receptor type 6 1
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