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Compound Detail

CHEMBL15855

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COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1

Basic Information

ChEMBL ID CHEMBL15855
Phase Preclinical
Structure Type MOL
InChI Key RATYOZVXDGPQTC-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
4.34
ALogP
4
HBA
2
HBD
63.8
PSA (Ų)
0.62
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 C26H33N5O2
MW 447.58
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.30

Activity Summary

IC50 4 meas. best 7.3
Kd 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oryctolagus cuniculus
CHEMBL374
Kd 7.7 7.7 19.9 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 7.3 7.3 50.0 1
Rattus norvegicus
CHEMBL376
IC50 6.7 6.7 200.0 1
5-hydroxytryptamine receptor 1D
CHEMBL5450
IC50 6.63 6.63 233.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10737747 10.1021/jm9811054 5-hydroxytryptamine receptor 1D 1
10737747 10.1021/jm9811054 5-hydroxytryptamine receptor 1B 1
10737747 10.1021/jm9811054 5-hydroxytryptamine receptor 1A 1
10737747 10.1021/jm9811054 Rattus norvegicus 1
10737747 10.1021/jm9811054 Oryctolagus cuniculus 1
10737747 10.1021/jm9811054 Cavia porcellus 1

Data from ChEMBL 36 via Core Engine