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Compound Detail

CHEMBL503822

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CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL503822
Phase Preclinical
Structure Type MOL
InChI Key XLDJSOMVSODMFR-UHFFFAOYSA-N
Parent Compound CHEMBL453083
Active Moiety CHEMBL453083
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

517.6
MW (Da)
5.76
ALogP
6
HBA
0
HBD
63.5
PSA (Ų)
0.29
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 C34H32F3N5O4
MW 631.66
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -1.60

Activity Summary

EC50 1 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gastrin/cholecystokinin type B receptor
CHEMBL2854
EC50 8.68 8.68 2.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gastrin/cholecystokinin type B receptor EC50 = 2.1 nM 8.68 Agonist activity against mouse CCK1 receptor 18614364

Literature References

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

Data from ChEMBL 36 via Core Engine