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Compound Detail

CHEMBL494648

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COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1

Basic Information

ChEMBL ID CHEMBL494648
Phase Preclinical
Structure Type MOL
InChI Key XVSFXGNIAZCOPM-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

299.4
MW (Da)
1.49
ALogP
6
HBA
1
HBD
67.5
PSA (Ų)
0.93
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 C16H21N5O
MW 299.38
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.34

Activity Summary

EC50 1 meas. best 6.94
Ki 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H4 receptor
CHEMBL3759
Ki 7.8 7.8 15.8 1
Histamine H4 receptor
CHEMBL4468
EC50 6.94 6.94 114.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18811133 10.1021/jm8005959 Histamine H4 receptor 3
- 10.1039/C2MD20212C Histamine H4 receptor 1

Data from ChEMBL 36 via Core Engine