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Compound Detail

CHEMBL3099952

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O=C1CCc2cccc(OC[C@@H](O)CN3CCC4(CC3)Cc3cc(Cl)ccc3O4)c2N1

Basic Information

ChEMBL ID CHEMBL3099952
Phase Preclinical
Structure Type MOL
InChI Key SYOVYMUIPNLGAP-IBGZPJMESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

442.9
MW (Da)
3.43
ALogP
5
HBA
2
HBD
71.0
PSA (Ų)
0.74
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 C24H27ClN2O4
MW 442.94
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.48

Activity Summary

IC50 2 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 1
CHEMBL2413
IC50 7.5 7.5 32.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 6.3 6.3 500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24332486 10.1016/j.bmcl.2013.11.062 C-C chemokine receptor type 1 2
24332486 10.1016/j.bmcl.2013.11.062 Voltage-gated inwardly rectifying potassium channel KCNH2 1
24332486 10.1016/j.bmcl.2013.11.062 Caco-2 1
24332486 10.1016/j.bmcl.2013.11.062 Hepatocyte 1
24332486 10.1016/j.bmcl.2013.11.062 Liver microsome 1

Data from ChEMBL 36 via Core Engine