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Compound Detail

CHEMBL460680

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CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCOC(=O)NCCCCO

Basic Information

ChEMBL ID CHEMBL460680
Phase Preclinical
Structure Type MOL
InChI Key ATQNZOMJKQGZHT-QGZVFWFLSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
2
Publications
0
Known Names

Molecular Properties

497.6
MW (Da)
1.64
ALogP
9
HBA
4
HBD
157.3
PSA (Ų)
0.29
QED
0
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H33F2N7O4
MW 497.55
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.11

Activity Summary

EC50 1 meas. best 9.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Growth hormone secretagogue receptor type 1
CHEMBL4616
EC50 9.57 9.57 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 448.29 ng.hr.mL-1 Rattus norvegicus
AUC 118.91 ng.hr.mL-1 Rattus norvegicus
AUC 2.4 hr Rattus norvegicus
CL 183.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 166.0 nM Rattus norvegicus
F 26.0 % Rattus norvegicus
MRT 1.4 hr Rattus norvegicus
Tmax 1.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Growth hormone secretagogue receptor type 1 EC50 = 0.27 nM 9.57 Agonist activity at GHS receptor 18554903

Literature References

PubMed DOI Target Context # Activities
18554903 10.1016/j.bmcl.2008.05.100 Rattus norvegicus 10
18554903 10.1016/j.bmcl.2008.05.100 Growth hormone secretagogue receptor type 1 1

Data from ChEMBL 36 via Core Engine