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Compound Detail

CHEMBL237352

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COc1ccc2cc(-c3nc(-c4ccc([S+](C)[O-])cc4)[nH]c3-c3ccncc3)ccc2c1

Basic Information

ChEMBL ID CHEMBL237352
Phase Preclinical
Structure Type MOL
InChI Key SINQIEAULQKUPD-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
5.70
ALogP
4
HBA
1
HBD
73.9
PSA (Ų)
0.36
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H21N3O2S
MW 439.54
Aromatic Rings 5
Heavy Atoms 32
NP-Likeness -0.56

Activity Summary

IC50 2 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.6 6.6 250.0 1
Unchecked
CHEMBL612545
IC50 4.3 4.3 50000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiopoietin-1 receptor IC50 = 250.0 nM 6.6 Inhibition of Tie2 kinase by autophosphorylation assay 17618114
Unchecked IC50 = 50000.0 nM 4.3 Inhibition of P38 kinase 17618114

Literature References

PubMed DOI Target Context # Activities
17618114 10.1016/j.bmcl.2007.06.068 Unchecked 4
17618114 10.1016/j.bmcl.2007.06.068 Mus musculus 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
17618114 10.1016/j.bmcl.2007.06.068 Angiopoietin-1 receptor 1
17618114 10.1016/j.bmcl.2007.06.068 MOPC 315 1
17826092 10.1016/j.bmcl.2007.08.052 Angiopoietin-1 receptor 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
38157838 10.1016/j.bmc.2023.117561 Unchecked 1

Data from ChEMBL 36 via Core Engine