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Compound Detail

CHEMBL351321

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Fc1ccc(C(OCCN2CCN(CCCc3nc4ccccc4[nH]3)CC2)c2ccc(F)cc2)cc1

Basic Information

ChEMBL ID CHEMBL351321
Phase Preclinical
Structure Type MOL
InChI Key RGFIOTJNFCFPOX-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

490.6
MW (Da)
5.20
ALogP
4
HBA
1
HBD
44.4
PSA (Ų)
0.33
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32F2N4O
MW 490.60
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.20

Activity Summary

IC50 4 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL338
IC50 8.6 7.94 2.5 3
Sodium-dependent serotonin transporter
CHEMBL313
IC50 7.55 7.55 28.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9057857 10.1021/jm9606599 Sodium-dependent dopamine transporter 4
9057857 10.1021/jm9606599 Monoamine transporters; serotonin & dopamine 2
9057857 10.1021/jm9606599 Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine