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Compound Detail

CHEMBL53128

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CN(C)CCc1c[nH]c2ccc(Cc3nnnn3C)cc12

Basic Information

ChEMBL ID CHEMBL53128
Phase Preclinical
Structure Type MOL
InChI Key YOPSWVMUSWBXTO-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

284.4
MW (Da)
1.39
ALogP
5
HBA
1
HBD
62.6
PSA (Ų)
0.77
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H20N6
MW 284.37
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.31

Activity Summary

IC50 4 meas. best 7.6
EC50 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1D
CHEMBL4105
IC50 7.6 7.6 25.1 1
5-hydroxytryptamine receptor 1A
CHEMBL214
IC50 6.7 6.7 199.5 1
Oryctolagus cuniculus
CHEMBL374
EC50 6.6 6.6 251.2 1
Serotonin 3 (5-HT3) receptor
CHEMBL2094116
IC50 5.3 5.3 5011.9 1
5-hydroxytryptamine receptor 2C
CHEMBL225
IC50 5.3 5.3 5011.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7752204 10.1021/jm00010a025 5-hydroxytryptamine receptor 1D 1
7752204 10.1021/jm00010a025 No relevant target 1
7752204 10.1021/jm00010a025 5-hydroxytryptamine receptor 1A 1
7752204 10.1021/jm00010a025 5-hydroxytryptamine receptor 2C 1
7752204 10.1021/jm00010a025 5-hydroxytryptamine receptor 2A 1
7752204 10.1021/jm00010a025 Serotonin 3 (5-HT3) receptor 1
7752204 10.1021/jm00010a025 Oryctolagus cuniculus 1
7752204 10.1021/jm00010a025 Unchecked 1

Data from ChEMBL 36 via Core Engine