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Compound Detail

CHEMBL145815

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COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL145815
Phase Preclinical
Structure Type MOL
InChI Key ORVWUZVNKPDYHT-MHZLTWQESA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

458.6
MW (Da)
4.12
ALogP
6
HBA
2
HBD
71.0
PSA (Ų)
0.37
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H34N6O
MW 458.61
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.13

Activity Summary

IC50 2 meas. best 8.52
EC50 1 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1D
CHEMBL1983
EC50 9.05 9.05 0.9 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
IC50 8.52 8.52 3.0 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
IC50 6.68 6.68 210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10585208 10.1021/jm9910021 5-hydroxytryptamine receptor 1D 3
10585208 10.1021/jm9910021 5-hydroxytryptamine receptor 1B 1
10585208 10.1021/jm9910021 Unchecked 1

Data from ChEMBL 36 via Core Engine