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Compound Detail

CHEMBL222660

5-METHOXYISATIN
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COc1ccc2c(c1)C(=O)C(=O)N2

Basic Information

ChEMBL ID CHEMBL222660
Name 5-METHOXYISATIN
Phase Preclinical
Structure Type MOL
InChI Key DMHGXMPXHPOXBF-UHFFFAOYSA-N
1
Targets
3
Activities
2
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

177.2
MW (Da)
0.83
ALogP
3
HBA
1
HBD
55.4
PSA (Ų)
0.65
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C9H7NO3
MW 177.16
Aromatic Rings 1
Heavy Atoms 13
NP-Likeness 0.07

Activity Summary

IC50 2 meas.
Ki 1 meas. best 4.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 4.57 4.57 26700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 26700.0 nM 4.57 Inhibition of rabbit liver carboxylesterase expressed in sf21 cells 17378546

Literature References

PubMed DOI Target Context # Activities
17378546 10.1021/jm061471k Unchecked 2
21838297 10.1021/jf2021607 Brassica rapa subsp. oleifera 2
17378546 10.1021/jm061471k Liver carboxylesterase 1 1
17378546 10.1021/jm061471k Acetylcholinesterase 1
17378546 10.1021/jm061471k Cholinesterase 1
17088067 10.1016/j.bmc.2006.10.035 U-937 1
20056518 10.1016/j.ejmech.2009.12.010 U-937 1
21838297 10.1021/jf2021607 Acetolactate synthase, chloroplastic 1
24316352 10.1016/j.bmc.2013.11.028 Replicase polyprotein 1ab 1
24360564 10.1016/j.bmcl.2013.12.001 HT-29 1
24360564 10.1016/j.bmcl.2013.12.001 HepG2 1
24360564 10.1016/j.bmcl.2013.12.001 K562 1
26890120 10.1016/j.ejmech.2015.12.050 Jurkat 1
30055465 10.1016/j.ejmech.2018.07.032 K562 1
30055465 10.1016/j.ejmech.2018.07.032 HepG2 1

Data from ChEMBL 36 via Core Engine