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Compound Detail

CHEMBL516452

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O=C(Nc1ccc(Oc2cccnc2Cl)nc1)c1c[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL516452
Phase Preclinical
Structure Type MOL
InChI Key SMRGPXRMTZVWME-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

364.8
MW (Da)
4.66
ALogP
4
HBA
2
HBD
79.9
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H13ClN4O2
MW 364.79
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.67

Activity Summary

IC50 2 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
IC50 9.3 7.765 0.5 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18602261 10.1016/j.bmcl.2008.06.064 Unchecked 6
18602261 10.1016/j.bmcl.2008.06.064 5-hydroxytryptamine receptor 2C 2
18602261 10.1016/j.bmcl.2008.06.064 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1
18602261 10.1016/j.bmcl.2008.06.064 5-hydroxytryptamine receptor 1A 1
18602261 10.1016/j.bmcl.2008.06.064 5-hydroxytryptamine receptor 2A 1
18602261 10.1016/j.bmcl.2008.06.064 5-hydroxytryptamine receptor 6 1
18602261 10.1016/j.bmcl.2008.06.064 5-hydroxytryptamine receptor 7 1
18602261 10.1016/j.bmcl.2008.06.064 D(2) dopamine receptor 1
18602261 10.1016/j.bmcl.2008.06.064 D(3) dopamine receptor 1
18602261 10.1016/j.bmcl.2008.06.064 D(4) dopamine receptor 1

Data from ChEMBL 36 via Core Engine