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Compound Detail

CHEMBL5270846

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CCOC(=O)CCCCO/N=C(/c1cccnc1)c1cccc(CNS(=O)(=O)c2ccc(Cn3c(C)nc4ccccc43)cc2)c1

Basic Information

ChEMBL ID CHEMBL5270846
Phase Preclinical
Structure Type MOL
InChI Key RDUJSUBECFEVDI-IGIMMJHKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

639.8
MW (Da)
5.77
ALogP
9
HBA
1
HBD
124.8
PSA (Ų)
0.07
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H37N5O5S
MW 639.78
Aromatic Rings 5
Heavy Atoms 46
NP-Likeness -1.26

Activity Summary

IC50 2 meas. best 8.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thromboxane-A synthase
CHEMBL1835
IC50 8.33 8.33 4.7 1
Unchecked
CHEMBL612545
IC50 7.17 7.17 68.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thromboxane-A synthase IC50 = 4.7 nM 8.33 Inhibition of TXA2 synthetase (unknown origin) 34313432
Unchecked IC50 = 68.0 nM 7.17 Inhibition of PAF (unknown origin) 34313432

Literature References

PubMed DOI Target Context # Activities
34313432 10.1021/acs.jmedchem.1c00683 Thromboxane-A synthase 1
34313432 10.1021/acs.jmedchem.1c00683 Unchecked 1

Data from ChEMBL 36 via Core Engine