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Compound Detail

CHEMBL281720

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O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2ncccn2)CC1

Basic Information

ChEMBL ID CHEMBL281720
Phase Preclinical
Structure Type MOL
InChI Key QFMFYDYACBTMIQ-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

365.4
MW (Da)
1.67
ALogP
6
HBA
0
HBD
69.6
PSA (Ų)
0.57
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 C20H23N5O2
MW 365.44
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.49

Activity Summary

Ki 2 meas. best 7.44
IC50 1 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.44 7.44 36.0 2
5-hydroxytryptamine receptor 1A
CHEMBL214
IC50 7.22 7.22 60.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.4467 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2874226 10.1021/jm00158a026 Rattus norvegicus 3
3172131 10.1021/jm00118a018 5-hydroxytryptamine receptor 1A 2
15026055 10.1016/j.bmcl.2004.01.045 5-hydroxytryptamine receptor 1A 1
15026055 10.1016/j.bmcl.2004.01.045 ADMET 1
8568799 10.1021/jm950410b 5-hydroxytryptamine receptor 1A 1
2874226 10.1021/jm00158a026 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine