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Compound Detail

CHEMBL5094263

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

Basic Information

ChEMBL ID CHEMBL5094263
Phase Preclinical
Structure Type MOL
InChI Key CQKVWEYZUVUWJT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

386.5
MW (Da)
4.16
ALogP
5
HBA
1
HBD
64.3
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 C24H26N4O
MW 386.50
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.96

Activity Summary

Ki 2 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 7.96 7.96 11.0 1
Adenosine receptor A1
CHEMBL226
Ki 6.08 6.08 828.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34107215 10.1021/acs.jmedchem.0c00914 Adenosine receptor A2a 2
34107215 10.1021/acs.jmedchem.0c00914 Adenosine receptor A2b 2
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 Histamine H3 receptor 1
34107215 10.1021/acs.jmedchem.0c00914 SH-SY5Y 1

Data from ChEMBL 36 via Core Engine