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Compound Detail

CHEMBL3142698

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Cc1ccccc1/N=C(/S)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O

Basic Information

ChEMBL ID CHEMBL3142698
Phase Preclinical
Structure Type BOTH
InChI Key SKYYDNPZYTUAFI-BBACVFHCSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

843.0
MW (Da)
3.95
ALogP
8
HBA
9
HBD
246.2
PSA (Ų)
0.03
QED
2
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H54N8O8S
MW 843.02
Aromatic Rings 4
Heavy Atoms 60
NP-Likeness -0.29

Activity Summary

IC50 2 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholecystokinin receptor type A
CHEMBL3501
IC50 6.66 6.66 220.0 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
IC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1716682 10.1021/jm00113a023 Cholecystokinin receptor type A 1
1716682 10.1021/jm00113a023 Gastrin/cholecystokinin type B receptor 1
1716682 10.1021/jm00113a023 Cholecystokinin receptor 1

Data from ChEMBL 36 via Core Engine