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Compound Detail

CHEMBL4642730

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COc1cc(/C=C/C(=O)O)ccc1OCc1cn(-c2ccc(C)cc2)nn1

Basic Information

ChEMBL ID CHEMBL4642730
Phase Preclinical
Structure Type MOL
InChI Key SWXWXTJVPKKJQB-UXBLZVDNSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

365.4
MW (Da)
3.26
ALogP
6
HBA
1
HBD
86.5
PSA (Ų)
0.65
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19N3O4
MW 365.39
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.06

Activity Summary

IC50 3 meas. best 5.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Carbonic anhydrase 2
CHEMBL205
IC50 5.45 5.45 3560.0 1
Carbonic anhydrase 9
CHEMBL3594
IC50 5.38 5.38 4220.0 1
Carbonic anhydrase 5A, mitochondrial
CHEMBL4789
IC50 5.3 5.3 4970.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32209296 10.1016/j.bmc.2020.115424 Unchecked 2
32209296 10.1016/j.bmc.2020.115424 Carbonic anhydrase 2 1
32209296 10.1016/j.bmc.2020.115424 Carbonic anhydrase 9 1
32209296 10.1016/j.bmc.2020.115424 Carbonic anhydrase 5A, mitochondrial 1

Data from ChEMBL 36 via Core Engine