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Compound Detail

CHEMBL555148

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Cc1ccc([C@H](C(=O)NC(C)C)N2C(=O)[C@@H](C3Cc4ccccc4C3)NC(=O)[C@H]2CC(C)C)cc1

Basic Information

ChEMBL ID CHEMBL555148
Phase Preclinical
Structure Type MOL
InChI Key ISAYVWZUNKTFRK-TWJOJJKGSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

475.6
MW (Da)
3.72
ALogP
3
HBA
2
HBD
78.5
PSA (Ų)
0.64
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H37N3O3
MW 475.63
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.14

Activity Summary

Ki 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
Ki 8.4 8.4 4.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - ng.hr.mL-1 Rattus norvegicus
T1/2 0.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor Ki = 3.981 nM 8.4 Displacement of [3H]oxytocin from human Oxytocin receptor 16250654

Literature References

PubMed DOI Target Context # Activities
16250654 10.1021/jm050557v ADMET 4
16250654 10.1021/jm050557v Oxytocin receptor 1
16250654 10.1021/jm050557v No relevant target 1

Data from ChEMBL 36 via Core Engine