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Compound Detail

CHEMBL209917

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

Basic Information

ChEMBL ID CHEMBL209917
Phase Preclinical
Structure Type MOL
InChI Key VFUCISRJYLDARP-XPWALMASSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

442.5
MW (Da)
3.15
ALogP
3
HBA
2
HBD
69.6
PSA (Ų)
0.72
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 C25H28F2N2O3
MW 442.51
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.05

Activity Summary

Ki 1 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
Ki 7.9 7.9 12.6 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 567.0 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor Ki = 12.59 nM 7.9 Displacement of [3H]oxytocin from human OTR 16821776

Literature References

PubMed DOI Target Context # Activities
16821776 10.1021/jm060073e Rattus norvegicus 1
16821776 10.1021/jm060073e Oxytocin receptor 1

Data from ChEMBL 36 via Core Engine