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Compound Detail

CHEMBL115710

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Fc1ccc(C(OC2CC3CCC(C2)N3CCOCCN2CCOCC2)c2ccc(F)cc2)cc1

Basic Information

ChEMBL ID CHEMBL115710
Phase Preclinical
Structure Type MOL
InChI Key ABQQJUQDHRDZGR-UHFFFAOYSA-N
6
Targets
6
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

486.6
MW (Da)
4.42
ALogP
5
HBA
0
HBD
34.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H36F2N2O3
MW 486.60
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.78

Activity Summary

Ki 5 meas. best 6.18
IC50 1 meas. best 6.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL238
Ki 6.18 6.18 660.7 1
Rattus norvegicus
CHEMBL376
IC50 6.18 6.18 659.0 1
Sodium-dependent dopamine transporter
CHEMBL338
Ki 5.79 5.79 1620.0 1
Muscarinic acetylcholine receptor M1
CHEMBL276
Ki 4.8 4.8 15800.0 1
Sodium-dependent serotonin transporter
CHEMBL313
Ki 4.64 4.64 23000.0 1
Norepinephrine transporter
CHEMBL304
Ki 4.55 4.55 28100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15189035 10.1021/jm030646c Sodium-dependent dopamine transporter 1
15189035 10.1021/jm030646c Sodium-dependent serotonin transporter 1
15189035 10.1021/jm030646c Norepinephrine transporter 1
15189035 10.1021/jm030646c Muscarinic acetylcholine receptor M1 1
15189035 10.1021/jm030646c Rattus norvegicus 1
15189035 10.1021/jm030646c Monoamine transporters; serotonin & dopamine 1
15189035 10.1021/jm030646c Monoamine transporters; Norepininephrine & dopamine 1
15189035 10.1021/jm030646c Unchecked 1
15189035 10.1021/jm030646c No relevant target 1
15808487 10.1016/j.bmcl.2005.02.012 Sodium-dependent dopamine transporter 1

Data from ChEMBL 36 via Core Engine