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Compound Detail

CHEMBL512955

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C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O

Basic Information

ChEMBL ID CHEMBL512955
Phase Preclinical
Structure Type BOTH
InChI Key FMYKJNQXBIJPPV-DFQATESRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

534.6
MW (Da)
0.45
ALogP
6
HBA
6
HBD
183.6
PSA (Ų)
0.22
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H34N6O5
MW 534.62
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.20

Activity Summary

Ki 1 meas. best 7.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
Ki 7.14 7.14 72.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mu-type opioid receptor Ki = 72.7 nM 7.14 Displacement of [3H]DAMGO from mu opioid receptor in human SH-SY5Y cells 18329886

Literature References

PubMed DOI Target Context # Activities
18329886 10.1016/j.bmc.2008.02.074 Mu-type opioid receptor 3

Data from ChEMBL 36 via Core Engine