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Compound Detail

CHEMBL289489

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CC(=O)Nc1ccc(Cc2noc(-c3ccc4[nH]cc(CCN)c4c3)n2)cc1

Basic Information

ChEMBL ID CHEMBL289489
Phase Preclinical
Structure Type MOL
InChI Key MPSISMSDHLPFGV-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

375.4
MW (Da)
3.27
ALogP
5
HBA
3
HBD
109.8
PSA (Ų)
0.48
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 C21H21N5O2
MW 375.43
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.13

Activity Summary

IC50 4 meas. best 9.3
EC50 1 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1D
CHEMBL4105
IC50 9.3 9.3 0.5 1
5-hydroxytryptamine receptor 1A
CHEMBL214
IC50 8.3 8.3 5.0 1
Oryctolagus cuniculus
CHEMBL374
EC50 7.9 7.9 12.6 1
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
IC50 6.4 6.4 398.1 1
5-hydroxytryptamine receptor 2C
CHEMBL225
IC50 5.8 5.8 1584.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8496922 10.1021/jm00063a003 Oryctolagus cuniculus 2
8496922 10.1021/jm00063a003 5-hydroxytryptamine receptor 1D 1
8496922 10.1021/jm00063a003 No relevant target 1
8496922 10.1021/jm00063a003 5-hydroxytryptamine receptor 1A 1
8496922 10.1021/jm00063a003 5-hydroxytryptamine receptor 2C 1
8496922 10.1021/jm00063a003 Serotonin 2 (5-HT2) receptor 1
8496922 10.1021/jm00063a003 Serotonin 3 (5-HT3) receptor 1

Data from ChEMBL 36 via Core Engine