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Compound Detail

CHEMBL568358

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COc1ccc([C@@H](CCCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC

Basic Information

ChEMBL ID CHEMBL568358
Phase Preclinical
Structure Type MOL
InChI Key KOLWWPAODLKMSJ-PDDLMNHVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

656.8
MW (Da)
6.62
ALogP
8
HBA
1
HBD
100.7
PSA (Ų)
0.17
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H48N4O6
MW 656.82
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness -0.84

Activity Summary

IC50 1 meas. best 4.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urotensin-2 receptor
CHEMBL4921
IC50 4.19 4.19 65000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Urotensin-2 receptor IC50 = 65000.0 nM 4.19 Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assesse... 19731961

Literature References

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

Data from ChEMBL 36 via Core Engine