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Compound Detail

CHEMBL3142692

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CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc(Cl)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O

Basic Information

ChEMBL ID CHEMBL3142692
Phase Preclinical
Structure Type BOTH
InChI Key LPACLEPUQLVYSR-CUPIEXAXSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

847.4
MW (Da)
3.91
ALogP
8
HBA
9
HBD
262.9
PSA (Ų)
0.06
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 C42H51ClN8O9
MW 847.37
Aromatic Rings 4
Heavy Atoms 60
NP-Likeness -0.56

Activity Summary

IC50 2 meas. best 7.29
EC50 1 meas. best 8.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cavia porcellus
CHEMBL369
EC50 8.36 8.36 4.4 1
Cholecystokinin receptor type A
CHEMBL3501
IC50 7.29 7.29 51.0 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
IC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1716682 10.1021/jm00113a023 Cavia porcellus 2
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