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Compound Detail

CHEMBL413729

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CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCCCN)C(N)=O

Basic Information

ChEMBL ID CHEMBL413729
Phase Preclinical
Structure Type BOTH
InChI Key FWFMDUHCMOVSLZ-LKYFVMGBSA-N
4
Targets
8
Activities
2
Assay Types
1
PK Parameters
9
Publications
0
Known Names

Molecular Properties

1401.7
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C66H108N22O12
MW 1401.73

Activity Summary

Ki 6 meas. best 8.62
IC50 2 meas. best 6.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
Ki 8.62 7.71 2.4 2
Kappa-type opioid receptor
CHEMBL237
IC50 6.36 6.36 440.0 1
Unchecked
CHEMBL612545
IC50 5.66 5.66 2200.0 1
Mu-type opioid receptor
CHEMBL233
Ki 5.28 5.18 5250.0 2
Delta-type opioid receptor
CHEMBL236
Ki 5.15 5.1 7100.0 2

Pharmacokinetic Data

Parameter Value Units Species
Ke 494.0 nM Cavia porcellus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12747782 10.1021/jm020125+ Kappa-type opioid receptor 4
12747782 10.1021/jm020125+ Mu-type opioid receptor 2
10893307 10.1021/jm990442p Unchecked 2
12747782 10.1021/jm020125+ Delta-type opioid receptor 1
12747782 10.1021/jm020125+ Opioid receptors; mu/kappa/delta 1
10893307 10.1021/jm990442p Kappa-type opioid receptor 1
10893307 10.1021/jm990442p Mu-type opioid receptor 1
10893307 10.1021/jm990442p Delta-type opioid receptor 1
10893307 10.1021/jm990442p Opioid receptors; mu/kappa/delta 1

Data from ChEMBL 36 via Core Engine