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Compound Detail

CHEMBL481280

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O=C(O)C1CCN(Cc2ccc(Oc3nc4ccccc4s3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL481280
Phase Preclinical
Structure Type MOL
InChI Key BUZBVOKDNAZIIM-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

368.5
MW (Da)
4.39
ALogP
5
HBA
1
HBD
62.7
PSA (Ų)
0.72
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20N2O3S
MW 368.46
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.49

Activity Summary

IC50 2 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Leukotriene A-4 hydrolase
CHEMBL4618
IC50 7.96 7.96 11.0 1
Leukotriene A-4 hydrolase
CHEMBL3738
IC50 7.06 7.06 88.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18588282 10.1021/jm701575k Unchecked 14
18588282 10.1021/jm701575k Rattus norvegicus 3
18588282 10.1021/jm701575k C-C chemokine receptor type 1 2
18588282 10.1021/jm701575k Sodium-dependent dopamine transporter 2
18588282 10.1021/jm701575k Leukotriene A-4 hydrolase 2
18588282 10.1021/jm701575k Adenosine receptor A3 1
23127888 10.1016/j.bmcl.2012.10.036 Voltage-gated inwardly rectifying potassium channel KCNH2 1
18588282 10.1021/jm701575k Substance-K receptor 1
18588282 10.1021/jm701575k Melanocortin receptor 4 1
18588282 10.1021/jm701575k C-X-C chemokine receptor type 2 1
18588282 10.1021/jm701575k Galanin receptor type 2 1
18588282 10.1021/jm701575k D(1A) dopamine receptor 1
18588282 10.1021/jm701575k B2 bradykinin receptor 1
18588282 10.1021/jm701575k Endothelin-1 receptor 1
18588282 10.1021/jm701575k Type-1 angiotensin II receptor 1
18588282 10.1021/jm701575k Beta-1 adrenergic receptor 1
18588282 10.1021/jm701575k Adenosine receptor A1 1
18588282 10.1021/jm701575k 5-hydroxytryptamine receptor 6 1
18588282 10.1021/jm701575k Histamine H1 receptor 1
18588282 10.1021/jm701575k Adenosine receptor A2a 1

Data from ChEMBL 36 via Core Engine