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Compound Detail

CHEMBL5027912

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c1ccc(C2CCN(c3cnc4c(N5CCOCC5)nccn34)CC2)cc1

Basic Information

ChEMBL ID CHEMBL5027912
Phase Preclinical
Structure Type MOL
InChI Key OKTXMSSTNJXZII-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

363.5
MW (Da)
2.95
ALogP
6
HBA
0
HBD
45.9
PSA (Ų)
0.72
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25N5O
MW 363.47
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.29

Activity Summary

Ki 4 meas. best 5.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 5.74 5.74 1819.7 2
Sodium-dependent dopamine transporter
CHEMBL238
Ki 5.38 5.38 4132.4 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL5303304 Fibroblast 5
- 10.6019/CHEMBL5303304 HEK-293T 4
- 10.6019/CHEMBL4800727 GABA-A receptor; anion channel 4
- 10.6019/CHEMBL4800727 Sodium-dependent dopamine transporter 3
- 10.6019/CHEMBL5303304 U2OS 3
- 10.6019/CHEMBL4800727 5-hydroxytryptamine receptor 6 1
- 10.6019/CHEMBL4800727 5-hydroxytryptamine receptor 5A 1
- 10.6019/CHEMBL4800727 Alpha-2A adrenergic receptor 1
- 10.6019/CHEMBL4800727 Alpha-2B adrenergic receptor 1
- 10.6019/CHEMBL4800727 Alpha-2C adrenergic receptor 1
- 10.6019/CHEMBL4800727 5-hydroxytryptamine receptor 2C 1
- 10.6019/CHEMBL4800727 D(2) dopamine receptor 1
- 10.6019/CHEMBL4800727 D(4) dopamine receptor 1
- 10.6019/CHEMBL4800727 5-hydroxytryptamine receptor 1E 1
- 10.6019/CHEMBL4800727 Kappa-type opioid receptor 1
- 10.6019/CHEMBL4800727 Mu-type opioid receptor 1

Data from ChEMBL 36 via Core Engine