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Compound Detail

CHEMBL62994

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Fc1ccc(C2=CC3CCC(C2)N3CCCCc2cn(-c3ccc(F)cc3)c3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL62994
Phase Preclinical
Structure Type MOL
InChI Key NRZHEKZOMMPQDG-UHFFFAOYSA-N
7
Targets
7
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

468.6
MW (Da)
7.55
ALogP
2
HBA
0
HBD
8.2
PSA (Ų)
0.25
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 C31H30F2N2
MW 468.59
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.57

Activity Summary

IC50 5 meas. best 8.6
Ki 2 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.6 8.6 2.5 1
Sigma 2 receptor
CHEMBL613288
IC50 8.6 8.6 2.5 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 6.46 6.46 350.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 5.92 5.92 1200.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL3602
IC50 5.92 5.92 1200.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
IC50 5.43 5.43 3700.0 1
D(2) dopamine receptor
CHEMBL339
IC50 5.1 5.1 8000.0 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
23734634 10.1021/jm301545c Unchecked 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
23734634 10.1021/jm301545c Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine