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Compound Detail

CHEMBL1089537

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CC(C)C(=O)OCOC(=O)c1sc2c([N+](=O)[O-])c(O)c(O)cc2c1Cl

Basic Information

ChEMBL ID CHEMBL1089537
Phase Preclinical
Structure Type MOL
InChI Key NUZAARCKGCFLIV-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

389.8
MW (Da)
3.19
ALogP
9
HBA
2
HBD
136.2
PSA (Ų)
0.26
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 C14H12ClNO8S
MW 389.77
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.22

Activity Summary

Ki 1 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Catechol O-methyltransferase
CHEMBL2023
Ki 7.77 7.77 17.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.01667 hr Rattus norvegicus
T1/2 5.1 hr Homo sapiens
T1/2 7.6 hr -
T1/2 201.6 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Catechol O-methyltransferase Ki = 17.0 nM 7.77 Inhibition of human recombinant COMT by microplate screening assay 20231095

Literature References

PubMed DOI Target Context # Activities
20231095 10.1016/j.bmcl.2010.02.057 No relevant target 7
20231095 10.1016/j.bmcl.2010.02.057 Rattus norvegicus 1
20231095 10.1016/j.bmcl.2010.02.057 Liver 1
20231095 10.1016/j.bmcl.2010.02.057 Serum 1
20231095 10.1016/j.bmcl.2010.02.057 ADMET 1
20231095 10.1016/j.bmcl.2010.02.057 Catechol O-methyltransferase 1

Data from ChEMBL 36 via Core Engine