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Compound Detail

CHEMBL506201

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CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL506201
Phase Preclinical
Structure Type MOL
InChI Key DNNOGHVXPYIKFW-UHFFFAOYSA-N
Parent Compound CHEMBL498942
Active Moiety CHEMBL498942
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

564.6
MW (Da)
5.89
ALogP
6
HBA
1
HBD
87.9
PSA (Ų)
0.27
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H30F4N4O6
MW 678.64
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.41

Activity Summary

EC50 1 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gastrin/cholecystokinin type B receptor
CHEMBL2854
EC50 8.82 8.82 1.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gastrin/cholecystokinin type B receptor EC50 = 1.5 nM 8.82 Agonist activity against mouse CCK1 receptor 18614364

Literature References

PubMed DOI Target Context # Activities
18614364 10.1016/j.bmcl.2008.06.057 Mus musculus 2
18614364 10.1016/j.bmcl.2008.06.057 Gastrin/cholecystokinin type B receptor 1

Data from ChEMBL 36 via Core Engine