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Compound Detail

CHEMBL84942

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CN1CCC(c2c[nH]c3ccc(Nc4ncccc4[N+](=O)[O-])cc23)C1

Basic Information

ChEMBL ID CHEMBL84942
Phase Preclinical
Structure Type MOL
InChI Key GKTWNPQNDWIPDK-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

337.4
MW (Da)
3.63
ALogP
5
HBA
2
HBD
87.1
PSA (Ų)
0.56
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 C18H19N5O2
MW 337.38
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.44

Activity Summary

EC50 2 meas. best 8.7
IC50 2 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1D
CHEMBL5450
EC50 8.7 8.7 2.0 1
5-hydroxytryptamine receptor 1D
CHEMBL5450
IC50 7.82 7.82 15.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 6.5 6.5 320.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
EC50 6.05 6.05 885.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8057297 10.1021/jm00042a003 5-hydroxytryptamine receptor 1A 2
8057297 10.1021/jm00042a003 5-hydroxytryptamine receptor 1D 2
8057297 10.1021/jm00042a003 Unchecked 2

Data from ChEMBL 36 via Core Engine