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Compound Detail

CHEMBL566187

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COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC

Basic Information

ChEMBL ID CHEMBL566187
Phase Preclinical
Structure Type MOL
InChI Key FARHQDUFBHCIDC-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

471.6
MW (Da)
3.82
ALogP
6
HBA
0
HBD
62.3
PSA (Ų)
0.49
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29N3O4
MW 471.56
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.09

Activity Summary

IC50 1 meas. best 6.82
Ki 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urotensin-2 receptor
CHEMBL4921
IC50 6.82 6.82 150.0 1
Urotensin-2 receptor
CHEMBL3764
Ki 6.8 6.8 160.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.05 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19731961 10.1021/jm900683d Urotensin-2 receptor 2
19731961 10.1021/jm900683d Liver microsomes 1

Data from ChEMBL 36 via Core Engine