Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL458220

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL458220
Phase Preclinical
Structure Type MOL
InChI Key OZAJLQLEAWUZSC-UHFFFAOYSA-N
10
Targets
10
Activities
2
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

514.0
MW (Da)
4.58
ALogP
6
HBA
2
HBD
79.3
PSA (Ų)
0.39
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 C29H28ClN5O2
MW 514.03
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.51

Activity Summary

Ki 9 meas. best 7.28
EC50 1 meas. best 6.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 7.28 7.28 52.5 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 7.01 7.01 97.7 1
Mas-related G-protein coupled receptor member X1
CHEMBL5850
EC50 6.9 6.9 125.9 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.52 6.52 302.0 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 6.34 6.34 457.1 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
Ki 6.23 6.23 588.8 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 5.84 5.84 1445.4 1
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 5.47 5.47 3388.4 1
D(3) dopamine receptor
CHEMBL234
Ki 5.45 5.45 3548.1 1
D(2) dopamine receptor
CHEMBL217
Ki 5.29 5.29 5128.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19146417 10.1021/jm800962k 5-hydroxytryptamine receptor 1B 1
19146417 10.1021/jm800962k 5-hydroxytryptamine receptor 1D 1
19146417 10.1021/jm800962k 5-hydroxytryptamine receptor 2A 1
19146417 10.1021/jm800962k 5-hydroxytryptamine receptor 2B 1
19146417 10.1021/jm800962k 5-hydroxytryptamine receptor 2C 1
19146417 10.1021/jm800962k 5-hydroxytryptamine receptor 6 1
19146417 10.1021/jm800962k Alpha-1B adrenergic receptor 1
19146417 10.1021/jm800962k Beta-2 adrenergic receptor 1
19146417 10.1021/jm800962k D(2) dopamine receptor 1
19146417 10.1021/jm800962k D(3) dopamine receptor 1
19146417 10.1021/jm800962k Mas-related G-protein coupled receptor member X1 1

Data from ChEMBL 36 via Core Engine