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Compound Detail

CHEMBL2178088

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NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC=C[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL2178088
Phase Preclinical
Structure Type MOL
InChI Key FFXSSGPCMCLJML-QZLCNWOESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

583.7
MW (Da)
1.26
ALogP
6
HBA
6
HBD
176.6
PSA (Ų)
0.17
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H37N5O5
MW 583.69
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness 0.21

Activity Summary

Ki 1 meas. best 5.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL270
Ki 5.67 5.67 2158.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mu-type opioid receptor Ki = 2158.0 nM 5.67 Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes 22957923

Literature References

PubMed DOI Target Context # Activities
22957923 10.1021/jm300836n Delta-type opioid receptor 2
22957923 10.1021/jm300836n Mu-type opioid receptor 2

Data from ChEMBL 36 via Core Engine