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Compound Detail

CHEMBL487360

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COc1cccc([C@H]2CC[C@@H](N3CCN(c4cccc5ccccc45)CC3)CC2)c1

Basic Information

ChEMBL ID CHEMBL487360
Phase Preclinical
Structure Type MOL
InChI Key RBBSEEBITXSZAO-PEPAQOBHSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

400.6
MW (Da)
5.70
ALogP
3
HBA
0
HBD
15.7
PSA (Ų)
0.56
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N2O
MW 400.57
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.81

Activity Summary

Ki 5 meas. best 7.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
CHEMBL5525
Ki 7.78 7.78 16.7 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.13 7.13 74.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL4153
Ki 6.62 6.62 240.0 1
D(2) dopamine receptor
CHEMBL339
Ki 5.88 5.88 1310.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 5.26 5.26 5540.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19053780 10.1021/jm800965b 5-hydroxytryptamine receptor 1A 1
19053780 10.1021/jm800965b D(2) dopamine receptor 1
19053780 10.1021/jm800965b Adrenergic receptor alpha-1 1
19053780 10.1021/jm800965b 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase 1
19053780 10.1021/jm800965b Sigma non-opioid intracellular receptor 1 1
19053780 10.1021/jm800965b PC-3 1

Data from ChEMBL 36 via Core Engine