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Compound Detail

CHEMBL310360

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c1ccc(CCc2c[nH]cn2)nc1

Basic Information

ChEMBL ID CHEMBL310360
Phase Preclinical
Structure Type MOL
InChI Key KZRQLGIMXSUKBW-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

173.2
MW (Da)
1.59
ALogP
2
HBA
1
HBD
41.6
PSA (Ų)
0.77
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H11N3
MW 173.22
Aromatic Rings 2
Heavy Atoms 13
NP-Likeness -1.07

Activity Summary

EC50 2 meas. best 5.87
Ki 2 meas. best 5.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 5.93 5.93 1174.9 1
Histamine H3 receptor
CHEMBL264
EC50 5.87 5.87 1349.0 1
Histamine H4 receptor
CHEMBL3759
Ki 4.91 4.91 12302.7 1
Histamine H4 receptor
CHEMBL3759
EC50 4.23 4.23 58884.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15115383 10.1021/jm049932u Histamine receptor (H3 and H4) 3
15115383 10.1021/jm049932u Histamine H3 receptor 2
15115383 10.1021/jm049932u Histamine H4 receptor 2

Data from ChEMBL 36 via Core Engine