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Compound Detail

CHEMBL5291363

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COc1ccc(C2=NN(C(=O)c3ccc(S(N)(=O)=O)cc3)C(c3ccc(OC)cc3)C2)cc1

Basic Information

ChEMBL ID CHEMBL5291363
Phase Preclinical
Structure Type MOL
InChI Key ZTZZFLHUQWXMPB-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

465.5
MW (Da)
3.34
ALogP
6
HBA
1
HBD
111.3
PSA (Ų)
0.60
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23N3O5S
MW 465.53
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.23

Activity Summary

Ki 3 meas. best 8.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Carbonic anhydrase 9
CHEMBL3594
Ki 8.26 8.26 5.5 1
Carbonic anhydrase 2
CHEMBL205
Ki 7.5 7.5 31.7 1
Carbonic anhydrase 1
CHEMBL261
Ki 7.06 7.06 87.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Carbonic anhydrase 9 Ki = 5.5 nM 8.26 Inhibition of human CA9 32795767
Carbonic anhydrase 2 Ki = 31.7 nM 7.5 Inhibition of human CA2 32795767
Carbonic anhydrase 1 Ki = 87.8 nM 7.06 Inhibition of human CA1 32795767

Literature References

PubMed DOI Target Context # Activities
32795767 10.1016/j.ejmech.2020.112666 Carbonic anhydrase 1 1
32795767 10.1016/j.ejmech.2020.112666 Carbonic anhydrase 2 1
32795767 10.1016/j.ejmech.2020.112666 Carbonic anhydrase 9 1

Data from ChEMBL 36 via Core Engine