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Compound Detail

CHEMBL382349

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CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL382349
Phase Preclinical
Structure Type BOTH
InChI Key LFIFGNCFEBAIHA-XSAWFYHVSA-N
6
Targets
16
Activities
3
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

884.0
MW (Da)
0.28
ALogP
10
HBA
10
HBD
308.2
PSA (Ų)
0.05
QED
2
Ro5 Violations
24
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C45H57N9O10
MW 884.00
Aromatic Rings 4
Heavy Atoms 64
NP-Likeness 0.03

Activity Summary

EC50 6 meas. best 8.34
IC50 6 meas. best 8.79
Ki 4 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gastrin/cholecystokinin type B receptor
CHEMBL298
Ki 8.8 8.8 1.6 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
IC50 8.79 8.79 1.6 1
Delta-type opioid receptor
CHEMBL236
Ki 8.66 8.66 2.2 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
EC50 8.34 8.34 4.6 2
Delta-type opioid receptor
CHEMBL236
IC50 8.28 8.28 5.2 1
Mu-type opioid receptor
CHEMBL270
EC50 7.75 7.75 17.8 2
Mu-type opioid receptor
CHEMBL270
Ki 7.41 7.41 39.0 1
Delta-type opioid receptor
CHEMBL3222
IC50 7.18 7.18 66.0 1
Mu-type opioid receptor
CHEMBL270
IC50 7.05 7.05 89.1 1
Delta-type opioid receptor
CHEMBL236
EC50 6.94 6.93 114.8 2
Mu-type opioid receptor
CHEMBL4354
IC50 6.33 6.33 470.0 1
Cholecystokinin receptor type A
CHEMBL1901
IC50 5.29 5.29 5128.6 1
Cholecystokinin receptor type A
CHEMBL1901
Ki 5.29 5.29 5100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gastrin/cholecystokinin type B receptor Ki = 1.6 nM 8.8 Displacement of [125I]CCK-8(SO3) from human CCK2 receptor expressed in HEK293 ce... 16686530
Gastrin/cholecystokinin type B receptor IC50 = 1.622 nM 8.79 Displacement of [125I]CCK-8(SO3) from human CCK2 receptor expressed in HEK293 ce... 16686530
Delta-type opioid receptor Ki = 2.2 nM 8.66 Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 c... 16686530
Gastrin/cholecystokinin type B receptor EC50 = 4.571 nM 8.34 Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accum... 16686530
Gastrin/cholecystokinin type B receptor EC50 = 4.6 nM 8.34 Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accum... 16686530
Delta-type opioid receptor IC50 = 5.248 nM 8.28 Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 c... 16686530
Mu-type opioid receptor EC50 = 17.78 nM 7.75 Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in... 16686530
Mu-type opioid receptor EC50 = 18.0 nM 7.75 Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in... 16686530
Mu-type opioid receptor Ki = 39.0 nM 7.41 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells 16686530
Delta-type opioid receptor IC50 = 66.0 nM 7.18 Agonist activity at delta opioid receptor assessed as inhibition of electrically... 16686530
Mu-type opioid receptor IC50 = 89.13 nM 7.05 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells 16686530
Delta-type opioid receptor EC50 = 114.82 nM 6.94 Activity against [35S]GTP-gamma-S binding to human delta opioid receptor express... 16686530
Delta-type opioid receptor EC50 = 120.0 nM 6.92 Activity against [35S]GTP-gamma-S binding to human delta opioid receptor express... 16686530
Mu-type opioid receptor IC50 = 470.0 nM 6.33 Agonist activity at mu opioid receptor assessed as inhibition of electrically st... 16686530
Cholecystokinin receptor type A IC50 = 5128.61 nM 5.29 Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 ce... 16686530
Cholecystokinin receptor type A Ki = 5100.0 nM 5.29 Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 ce... 16686530

Literature References

PubMed DOI Target Context # Activities
16686530 10.1021/jm050921q Delta-type opioid receptor 6
16686530 10.1021/jm050921q Mu-type opioid receptor 6
16686530 10.1021/jm050921q Gastrin/cholecystokinin type B receptor 5
16686530 10.1021/jm050921q Cholecystokinin receptor type A 3

Data from ChEMBL 36 via Core Engine