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Compound Detail

CHEMBL475331

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CN1CCN(c2nc(N)c3ccccc3n2)CC1

Basic Information

ChEMBL ID CHEMBL475331
Phase Preclinical
Structure Type MOL
InChI Key KJVGBWURWKYDCH-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

243.3
MW (Da)
0.96
ALogP
5
HBA
1
HBD
58.3
PSA (Ų)
0.81
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 C13H17N5
MW 243.31
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -1.38

Activity Summary

Ki 3 meas. best 10.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 3A
CHEMBL1899
Ki 10.29 10.29 0.1 1
Histamine H4 receptor
CHEMBL3759
Ki 5.76 5.715 1737.8 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23006041 10.1021/jm300801u Unchecked 14
- 10.6019/CHEMBL5303304 U2OS 9
- 10.6019/CHEMBL5303304 Fibroblast 4
- 10.6019/CHEMBL5303304 HEK-293T 3
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 1B 1
- 10.6019/CHEMBL5665443 Uracil-DNA glycosylase 1
- 10.6019/CHEMBL5665443 Methyl-CpG-binding domain protein 4 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 3A 1
23006041 10.1021/jm300801u GABA-A receptor; alpha-1/beta-2/gamma-2 1
23006041 10.1021/jm300801u Neuronal acetylcholine receptor; alpha4/beta2 1
23006041 10.1021/jm300801u Neuronal acetylcholine receptor subunit alpha-7 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 1A 1
19053770 10.1021/jm800876b Histamine H4 receptor 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 1D 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 2A 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 2B 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 2C 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 4 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 6 1
23006041 10.1021/jm300801u 5-hydroxytryptamine receptor 7 1

Data from ChEMBL 36 via Core Engine