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Compound Detail

CHEMBL192242

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COc1ccc(N2CCN(CCNC(=O)c3ccncc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL192242
Phase Preclinical
Structure Type MOL
InChI Key FCHSRCPWEMMVOW-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

340.4
MW (Da)
1.64
ALogP
5
HBA
1
HBD
57.7
PSA (Ų)
0.87
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H24N4O2
MW 340.43
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.70

Activity Summary

Ki 3 meas. best 6.04
Kd 1 meas. best 5.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.04 6.04 911.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 5.95 5.95 1122.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 5.9 5.9 1270.0 1
5-hydroxytryptamine receptor 2C
CHEMBL324
Ki 5.88 5.88 1330.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15935663 10.1016/j.bmcl.2005.05.003 Adrenergic receptor alpha-1 1
26820556 10.1016/j.ejmech.2016.01.021 5-hydroxytryptamine receptor 1A 1
26820556 10.1016/j.ejmech.2016.01.021 5-hydroxytryptamine receptor 2A 1
26820556 10.1016/j.ejmech.2016.01.021 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine