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Compound Detail

CHEMBL211443

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CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N1CCOCC1)c1ccc(F)cc1F

Basic Information

ChEMBL ID CHEMBL211443
Phase Preclinical
Structure Type MOL
InChI Key MJSYADMDNDGJIS-TWJOJJKGSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
4
Publications
0
Known Names

Molecular Properties

525.6
MW (Da)
3.02
ALogP
4
HBA
1
HBD
79.0
PSA (Ų)
0.63
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H33F2N3O4
MW 525.60
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.56

Activity Summary

Ki 1 meas. best 8.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
Ki 8.9 8.9 1.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 100.0 ng.hr.mL-1 Canis lupus familiaris
AUC 2150.0 ng.hr.mL-1 Rattus norvegicus
CL 8.0 mL.min-1.kg-1 Canis lupus familiaris
CL 16.0 mL.min-1.kg-1 Rattus norvegicus
F 7.0 % Canis lupus familiaris
F 41.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor Ki = 1.259 nM 8.9 Displacement of [3H]oxytocin from human OTR 16821776

Literature References

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

Data from ChEMBL 36 via Core Engine