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Compound Detail

CHEMBL26447

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COc1ccccc1N1CCN(CCNC(=O)c2cccnc2)CC1

Basic Information

ChEMBL ID CHEMBL26447
Phase Preclinical
Structure Type MOL
InChI Key RPFDZEAPDWUCAQ-UHFFFAOYSA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

340.4
MW (Da)
1.64
ALogP
5
HBA
1
HBD
57.7
PSA (Ų)
0.87
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 C19H24N4O2
MW 340.43
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.77

Activity Summary

Ki 5 meas. best 6.85
Kd 1 meas. best 7.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 7.87 7.87 13.5 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.85 6.6967 140.0 3
D(2) dopamine receptor
CHEMBL339
Ki 6.3 6.27 501.2 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9022796 10.1021/jm960496o 5-hydroxytryptamine receptor 1A 2
9022796 10.1021/jm960496o D(2) dopamine receptor 2
7731013 10.1021/jm00008a005 5-hydroxytryptamine receptor 1A 1
9022796 10.1021/jm960496o No relevant target 1
15935663 10.1016/j.bmcl.2005.05.003 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine