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Compound Detail

CHEMBL503367

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CCCCCCC(NC(=O)[C@H](Cc1ccccc1)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 CHEMBL503367
Phase Preclinical
Structure Type MOL
InChI Key IMYCMDVCSHAEQG-WBHZCIDJSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

751.9
MW (Da)
3.13
ALogP
7
HBA
7
HBD
212.7
PSA (Ų)
0.07
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H53N7O6
MW 751.93
Aromatic Rings 4
Heavy Atoms 55
NP-Likeness -0.02

Activity Summary

Ki 1 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
Ki 6.92 6.92 121.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.05833 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mu-type opioid receptor Ki = 121.0 nM 6.92 Displacement of [3H]DAMGO from mu opioid receptor in human SHSY5Y cells 18468445

Literature References

PubMed DOI Target Context # Activities
18468445 10.1016/j.bmc.2008.04.020 Caco-2 2
18468445 10.1016/j.bmc.2008.04.020 Mu-type opioid receptor 2

Data from ChEMBL 36 via Core Engine