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Compound Detail

CHEMBL438609

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CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(N)=O)c1ccc(F)cc1F

Basic Information

ChEMBL ID CHEMBL438609
Phase Preclinical
Structure Type MOL
InChI Key LXXOYJPGMZQIHX-YPAWHYETSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

455.5
MW (Da)
2.65
ALogP
3
HBA
2
HBD
92.5
PSA (Ų)
0.70
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27F2N3O3
MW 455.51
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.23

Activity Summary

Ki 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
Ki 9.3 9.3 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 560.0 ng.hr.mL-1 Rattus norvegicus
CL 33.0 mL.min-1.kg-1 Rattus norvegicus
F 22.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor Ki = 0.5012 nM 9.3 Displacement of [3H]oxytocin from human OTR 16821776

Literature References

PubMed DOI Target Context # Activities
16821776 10.1021/jm060073e Rattus norvegicus 3
16821776 10.1021/jm060073e No relevant target 2
16821776 10.1021/jm060073e Oxytocin receptor 1

Data from ChEMBL 36 via Core Engine