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Compound Detail

CHEMBL128088

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Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1

Basic Information

ChEMBL ID CHEMBL128088
Phase Preclinical
Structure Type MOL
InChI Key XJMMCJLQDZQDAQ-UHFFFAOYSA-N
1
Targets
8
Activities
3
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

257.3
MW (Da)
1.86
ALogP
2
HBA
1
HBD
39.3
PSA (Ų)
0.85
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H19N3O
MW 257.34
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -1.48

Activity Summary

Ki 5 meas. best 7.34
IC50 2 meas.
Kd 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H4 receptor
CHEMBL3759
Kd 7.7 7.7 19.9 1
Histamine H4 receptor
CHEMBL3759
Ki 7.34 7.33 46.0 4

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3988442 Unchecked 5
16366610 10.1021/jm0502081 Histamine H4 receptor 2
- 10.1007/s00044-004-0106-7 Histamine H4 receptor 2
- 10.6019/CHEMBL4513160 Pseudomonas aeruginosa 2
12954048 10.1021/jm0341047 Histamine H4 receptor 1
22749391 10.1016/j.ejmech.2012.06.016 Histamine H4 receptor 1
- 10.6019/CHEMBL3301361 No relevant target 1
- 10.6019/CHEMBL4513160 Acinetobacter baumannii 1

Data from ChEMBL 36 via Core Engine