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Compound Detail

CHEMBL18222

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c1ccc(CCN2CCC(Cc3ccccc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL18222
Phase Preclinical
Structure Type MOL
InChI Key FKVJGSPOLUAUNN-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

279.4
MW (Da)
4.18
ALogP
1
HBA
0
HBD
3.2
PSA (Ų)
0.79
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25N
MW 279.43
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -0.57

Activity Summary

IC50 3 meas. best 6.54
Ki 2 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 7.66 7.66 22.0 1
Glutamate NMDA receptor
CHEMBL1907608
IC50 6.54 6.54 290.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 6.46 6.46 347.0 1
5-hydroxytryptamine receptor 2C
CHEMBL324
Ki 5.75 5.75 1760.0 1
C-C chemokine receptor type 3
CHEMBL3473
IC50 5.15 5.15 7100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12166951 10.1021/jm0201767 C-C chemokine receptor type 1 1
12166951 10.1021/jm0201767 C-C chemokine receptor type 3 1
7707322 10.1021/jm00007a016 5-hydroxytryptamine receptor 2A 1
7707322 10.1021/jm00007a016 5-hydroxytryptamine receptor 2C 1
7707322 10.1021/jm00007a016 Serotonin receptor 2a and 2c (5HT2A and 5HT2C) 1
1681106 10.1021/jm00114a018 Glutamate NMDA receptor 1
1681106 10.1021/jm00114a018 Adrenergic receptor alpha-1 1
1681106 10.1021/jm00114a018 ADMET 1
38318365 10.1016/j.isci.2024.108907 Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 1

Data from ChEMBL 36 via Core Engine