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Compound Detail

CHEMBL5081556

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Nc1nc(-c2ccccc2)c2c(n1)-c1ccc(OCCCN3CCCC3)cc1C2=O

Basic Information

ChEMBL ID CHEMBL5081556
Phase Preclinical
Structure Type MOL
InChI Key SWTVGVLYEISYND-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

400.5
MW (Da)
3.80
ALogP
6
HBA
1
HBD
81.3
PSA (Ų)
0.50
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24N4O2
MW 400.48
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.68

Activity Summary

Ki 5 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 7.51 7.51 31.0 1
Adenosine receptor A2a
CHEMBL251
Ki 6.98 6.98 104.0 1
Adenosine receptor A1
CHEMBL226
Ki 6.89 6.89 129.0 1
Adenosine receptor A2b
CHEMBL255
Ki 6.75 6.75 180.0 1
Adenosine receptor A3
CHEMBL256
Ki 6.07 6.07 846.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34107215 10.1021/acs.jmedchem.0c00914 Adenosine receptor A1 1
34107215 10.1021/acs.jmedchem.0c00914 Adenosine receptor A2a 1
34107215 10.1021/acs.jmedchem.0c00914 Adenosine receptor A2b 1
34107215 10.1021/acs.jmedchem.0c00914 Adenosine receptor A3 1
34107215 10.1021/acs.jmedchem.0c00914 Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine