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Compound Detail

CHEMBL146735

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COc1ccc(NC(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1

Basic Information

ChEMBL ID CHEMBL146735
Phase Preclinical
Structure Type MOL
InChI Key QXLNAYIFEMXTDZ-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

497.6
MW (Da)
5.03
ALogP
7
HBA
1
HBD
83.7
PSA (Ų)
0.40
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31N5O3
MW 497.60
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.46

Activity Summary

IC50 2 meas. best 9.03
Kd 1 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 9.1 9.1 0.8 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 9.03 9.03 0.9 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
IC50 7.43 7.43 37.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10669578 10.1021/jm990397l No relevant target 2
10669578 10.1021/jm990397l 5-hydroxytryptamine receptor 1D 1
10669578 10.1021/jm990397l 5-hydroxytryptamine receptor 1B 1
10669578 10.1021/jm990397l 5-hydroxytryptamine receptor 1A 1
10669578 10.1021/jm990397l Sodium-dependent serotonin transporter 1
10669578 10.1021/jm990397l Unchecked 1
10669578 10.1021/jm990397l Serotonin (5-HT) receptor 1

Data from ChEMBL 36 via Core Engine