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Compound Detail

CHEMBL503688

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CC(C)[C@H]1C(=O)Nc2ccc(NCc3ccccc3)cc2-c2nc3cc(C(=O)N(C)C4CCN(C)CC4)ccc3n21

Basic Information

ChEMBL ID CHEMBL503688
Phase Preclinical
Structure Type MOL
InChI Key PKXKCWSYPLCFKQ-PMERELPUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

550.7
MW (Da)
5.63
ALogP
6
HBA
2
HBD
82.5
PSA (Ų)
0.33
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H38N6O2
MW 550.71
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.12

Activity Summary

EC50 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mas-related G-protein coupled receptor member X2
CHEMBL5849
EC50 6.8 6.8 158.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mas-related G-protein coupled receptor member X2 EC50 = 158.49 nM 6.8 Agonist activity at human MrgX2 receptor 19230660

Literature References

PubMed DOI Target Context # Activities
19230660 10.1016/j.bmcl.2009.01.085 Mas-related G-protein coupled receptor member X2 2
19230660 10.1016/j.bmcl.2009.01.085 Mas-related G-protein coupled receptor member X1 1

Data from ChEMBL 36 via Core Engine