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Compound Detail

CHEMBL5089580

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Nc1nc(-c2ccc(OCCCN3CCCCC3)cc2)c2c(n1)-c1ccccc1C2=O

Basic Information

ChEMBL ID CHEMBL5089580
Phase Preclinical
Structure Type MOL
InChI Key OYWQMDWRCCYZOE-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
4.19
ALogP
6
HBA
1
HBD
81.3
PSA (Ų)
0.48
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 C25H26N4O2
MW 414.51
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.70

Activity Summary

Ki 4 meas. best 9.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 9.55 9.55 0.3 1
Adenosine receptor A2a
CHEMBL251
Ki 7.45 7.45 35.5 1
Adenosine receptor A1
CHEMBL226
Ki 6.88 6.88 133.0 1
Adenosine receptor A2b
CHEMBL255
Ki 6.48 6.48 331.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34107215 10.1021/acs.jmedchem.0c00914 Adenosine receptor A3 2
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 Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine