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Compound Detail

CHEMBL416506

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Fc1ccc(N2CCN(CCCCc3cn(-c4ccc(F)cc4)c4ccccc34)CC2)cc1

Basic Information

ChEMBL ID CHEMBL416506
Phase Preclinical
Structure Type MOL
InChI Key NSJANYUTRNGXRW-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

445.6
MW (Da)
6.05
ALogP
3
HBA
0
HBD
11.4
PSA (Ų)
0.32
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29F2N3
MW 445.56
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.15

Activity Summary

IC50 5 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma 2 receptor
CHEMBL613288
IC50 8.12 8.12 7.5 1
5-hydroxytryptamine receptor 2A
CHEMBL322
IC50 6.6 6.6 250.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 6.38 6.38 420.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL3602
IC50 6.36 6.36 440.0 1
D(2) dopamine receptor
CHEMBL339
IC50 5.52 5.52 3000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7783131 10.1021/jm00011a019 Sigma non-opioid intracellular receptor 1 2
7783131 10.1021/jm00011a019 Sigma 2 receptor 1
7783131 10.1021/jm00011a019 5-hydroxytryptamine receptor 1A 1
7783131 10.1021/jm00011a019 5-hydroxytryptamine receptor 2A 1
7783131 10.1021/jm00011a019 D(2) dopamine receptor 1
7783131 10.1021/jm00011a019 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine