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Compound Detail

CHEMBL3215982

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Cl.Cl.Fc1ccc(CN[C@@H]2CC[C@H](C(c3ccccc3)c3ccccc3)NC2)cc1

Basic Information

ChEMBL ID CHEMBL3215982
Phase Preclinical
Structure Type MOL
InChI Key DSLSDIGWABEKHU-NILKIKDOSA-N
Parent Compound CHEMBL302547
Active Moiety CHEMBL302547
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

374.5
MW (Da)
4.87
ALogP
2
HBA
2
HBD
24.1
PSA (Ų)
0.64
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29Cl2FN2
MW 447.43
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.30

Activity Summary

IC50 4 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 6.85 6.85 142.0 1
Sodium-dependent dopamine transporter
CHEMBL338
IC50 6.64 6.64 229.0 1
Norepinephrine transporter
CHEMBL304
IC50 5.64 5.64 2290.0 1
Sodium-dependent serotonin transporter
CHEMBL313
IC50 5.45 5.45 3540.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12747792 10.1021/jm020561w Sodium-dependent dopamine transporter 1
12747792 10.1021/jm020561w Sodium-dependent serotonin transporter 1
12747792 10.1021/jm020561w Norepinephrine transporter 1
12747792 10.1021/jm020561w Rattus norvegicus 1
12747792 10.1021/jm020561w Monoamine transporters; serotonin & dopamine 1
12747792 10.1021/jm020561w Monoamine transporters; Norepininephrine & dopamine 1
12747792 10.1021/jm020561w Unchecked 1

Data from ChEMBL 36 via Core Engine