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Compound Detail

CHEMBL590580

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Cc1cccc2c1C(=O)NC1CCNCCN21

Basic Information

ChEMBL ID CHEMBL590580
Phase Preclinical
Structure Type MOL
InChI Key IDTOIAGIXRXDMI-UHFFFAOYSA-N
4
Targets
7
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

231.3
MW (Da)
0.86
ALogP
3
HBA
2
HBD
44.4
PSA (Ų)
0.70
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H17N3O
MW 231.30
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness 0.07

Activity Summary

EC50 4 meas. best 8.7
Ki 3 meas. best 8.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 8.7 8.7 2.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 8.54 8.54 2.9 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 8.0 8.0 10.0 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 7.21 7.21 61.0 1
5-hydroxytryptamine receptor 2C
CHEMBL324
EC50 7.21 7.21 61.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 7.16 7.16 70.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.85 6.85 141.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20022752 10.1016/j.bmcl.2009.12.014 5-hydroxytryptamine receptor 2C 6
20022752 10.1016/j.bmcl.2009.12.014 5-hydroxytryptamine receptor 2B 3
20022752 10.1016/j.bmcl.2009.12.014 5-hydroxytryptamine receptor 2A 3

Data from ChEMBL 36 via Core Engine