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Compound Detail

CHEMBL218327

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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](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL218327
Phase Preclinical
Structure Type BOTH
InChI Key KKPFQTRKARZYLE-YKEIYGJZSA-N
6
Targets
16
Activities
3
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

960.1
MW (Da)
1.50
ALogP
10
HBA
10
HBD
308.2
PSA (Ų)
0.04
QED
2
Ro5 Violations
26
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C51H61N9O10
MW 960.10
Aromatic Rings 5
Heavy Atoms 70
NP-Likeness 0.06

Activity Summary

EC50 6 meas. best 8.56
IC50 6 meas. best 9.0
Ki 4 meas. best 9.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 9.38 9.38 0.4 1
Delta-type opioid receptor
CHEMBL236
IC50 9.0 9.0 1.0 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
IC50 8.96 8.96 1.1 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
Ki 8.96 8.96 1.1 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
EC50 8.56 8.555 2.8 2
Mu-type opioid receptor
CHEMBL270
Ki 8.23 8.23 5.9 1
Mu-type opioid receptor
CHEMBL270
IC50 7.86 7.86 13.8 1
Delta-type opioid receptor
CHEMBL3222
IC50 7.62 7.62 24.0 1
Delta-type opioid receptor
CHEMBL236
EC50 7.54 7.54 28.8 2
Mu-type opioid receptor
CHEMBL4354
IC50 7.15 7.15 71.0 1
Mu-type opioid receptor
CHEMBL270
EC50 6.28 6.28 524.8 2
Cholecystokinin receptor type A
CHEMBL1901
IC50 5.96 5.96 1096.5 1
Cholecystokinin receptor type A
CHEMBL1901
Ki 5.96 5.96 1100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Delta-type opioid receptor Ki = 0.42 nM 9.38 Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 c... 16686530
Delta-type opioid receptor IC50 = 1.0 nM 9.0 Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 c... 16686530
Gastrin/cholecystokinin type B receptor IC50 = 1.096 nM 8.96 Displacement of [125I]CCK-8(SO3) from human CCK2 receptor expressed in HEK293 ce... 16686530
Gastrin/cholecystokinin type B receptor Ki = 1.1 nM 8.96 Displacement of [125I]CCK-8(SO3) from human CCK2 receptor expressed in HEK293 ce... 16686530
Gastrin/cholecystokinin type B receptor EC50 = 2.754 nM 8.56 Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accum... 16686530
Gastrin/cholecystokinin type B receptor EC50 = 2.8 nM 8.55 Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accum... 16686530
Mu-type opioid receptor Ki = 5.9 nM 8.23 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells 16686530
Mu-type opioid receptor IC50 = 13.8 nM 7.86 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells 16686530
Delta-type opioid receptor IC50 = 24.0 nM 7.62 Agonist activity at delta opioid receptor assessed as inhibition of electrically... 16686530
Delta-type opioid receptor EC50 = 28.84 nM 7.54 Activity against [35S]GTP-gamma-S binding to human delta opioid receptor express... 16686530
Delta-type opioid receptor EC50 = 29.0 nM 7.54 Activity against [35S]GTP-gamma-S binding to human delta opioid receptor express... 16686530
Mu-type opioid receptor IC50 = 71.0 nM 7.15 Agonist activity at mu opioid receptor assessed as inhibition of electrically st... 16686530
Mu-type opioid receptor EC50 = 524.81 nM 6.28 Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in... 16686530
Mu-type opioid receptor EC50 = 530.0 nM 6.28 Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in... 16686530
Cholecystokinin receptor type A IC50 = 1096.48 nM 5.96 Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 ce... 16686530
Cholecystokinin receptor type A Ki = 1100.0 nM 5.96 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