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Compound Detail

CHEMBL3609619

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C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL3609619
Phase Preclinical
Structure Type BOTH
InChI Key ADPQCWUGLGBPRO-ISCRSJHHSA-N
3
Targets
6
Activities
2
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

664.6
MW (Da)
4.76
ALogP
6
HBA
5
HBD
146.5
PSA (Ų)
0.12
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H30F6N4O5
MW 664.60
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -0.20

Activity Summary

Ki 4 meas. best 8.54
EC50 2 meas. best 7.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL4027
Ki 8.54 8.54 2.9 1
Delta-type opioid receptor
CHEMBL236
EC50 7.04 7.04 91.0 1
Delta-type opioid receptor
CHEMBL236
Ki 7.0 7.0 100.0 1
Mu-type opioid receptor
CHEMBL270
EC50 6.77 6.77 170.0 1
Mu-type opioid receptor
CHEMBL270
Ki 6.75 6.75 180.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 49.0 nM Cavia porcellus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26212775 10.1016/j.bmcl.2015.06.030 Mu-type opioid receptor 4
26212775 10.1016/j.bmcl.2015.06.030 Delta-type opioid receptor 4
26212775 10.1016/j.bmcl.2015.06.030 Substance-P receptor 3
26212775 10.1016/j.bmcl.2015.06.030 Unchecked 2

Data from ChEMBL 36 via Core Engine