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Compound Detail

CHEMBL4159562

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CCCNCC(O)COc1ccc(C(=O)NCCc2ccc(S(N)(=O)=O)cc2)cc1.Cl

Basic Information

ChEMBL ID CHEMBL4159562
Phase Preclinical
Structure Type MOL
InChI Key SKEGMIPRMMELBX-UHFFFAOYSA-N
Parent Compound CHEMBL4301089
Active Moiety CHEMBL4301089
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

435.6
MW (Da)
1.05
ALogP
6
HBA
4
HBD
130.8
PSA (Ų)
0.37
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H30ClN3O5S
MW 472.01
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.03

Activity Summary

Ki 4 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Carbonic anhydrase 12
CHEMBL3242
Ki 8.82 8.82 1.5 1
Carbonic anhydrase 9
CHEMBL3594
Ki 8.13 8.13 7.4 1
Carbonic anhydrase 2
CHEMBL205
Ki 7.74 7.74 18.4 1
Carbonic anhydrase 1
CHEMBL261
Ki 7.28 7.28 52.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29851481 10.1021/acs.jmedchem.8b00625 Carbonic anhydrase 2 1
29851481 10.1021/acs.jmedchem.8b00625 Carbonic anhydrase 1 1
29851481 10.1021/acs.jmedchem.8b00625 Carbonic anhydrase 9 1
29851481 10.1021/acs.jmedchem.8b00625 Carbonic anhydrase 12 1
29851481 10.1021/acs.jmedchem.8b00625 Beta-1 adrenergic receptor 1
29851481 10.1021/acs.jmedchem.8b00625 Beta-2 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine