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Compound Detail

CHEMBL1089504

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COC(=O)c1sc2c([N+](=O)[O-])c(O)c(O)cc2c1Cl

Basic Information

ChEMBL ID CHEMBL1089504
Phase Preclinical
Structure Type MOL
InChI Key UTYMOZJIQPIDGC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

303.7
MW (Da)
2.66
ALogP
7
HBA
2
HBD
109.9
PSA (Ų)
0.38
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H6ClNO6S
MW 303.68
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.70

Activity Summary

Ki 1 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Catechol O-methyltransferase
CHEMBL2023
Ki 8.66 8.66 2.2 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.33 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Catechol O-methyltransferase Ki = 2.2 nM 8.66 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 8
20231095 10.1016/j.bmcl.2010.02.057 Serum 1
20231095 10.1016/j.bmcl.2010.02.057 Liver 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