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Compound Detail

CHEMBL372554

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CC(=O)Nc1ccc([C@H](C(=O)NC(C)(C)C)N2C(=O)[C@@H](C3Cc4ccccc4C3)NC(=O)[C@H]2CC(C)C)cc1

Basic Information

ChEMBL ID CHEMBL372554
Phase Preclinical
Structure Type MOL
InChI Key AUWMENUQFJRYPU-ZONZVBGPSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

532.7
MW (Da)
3.76
ALogP
4
HBA
3
HBD
107.6
PSA (Ų)
0.50
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H40N4O4
MW 532.69
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -0.30

Activity Summary

Ki 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
Ki 8.7 8.7 2.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 59.0 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 = 1.995 nM 8.7 Displacement of [3H]oxytocin from human Oxytocin receptor 16250654

Literature References

PubMed DOI Target Context # Activities
16250654 10.1021/jm050557v Oxytocin receptor 1
16250654 10.1021/jm050557v ADMET 1
16250654 10.1021/jm050557v No relevant target 1

Data from ChEMBL 36 via Core Engine