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Compound Detail

CHEMBL438739

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CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O

Basic Information

ChEMBL ID CHEMBL438739
Phase Preclinical
Structure Type MOL
InChI Key VEGZKBKISJJLJC-FCVZMFCYSA-N
6
Targets
14
Activities
3
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

1212.4
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C64H77N9O15
MW 1212.37

Activity Summary

IC50 6 meas. best 8.11
EC50 4 meas. best 8.25
Ki 4 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 8.47 8.47 3.4 1
Delta-type opioid receptor
CHEMBL236
EC50 8.25 8.25 5.6 2
Delta-type opioid receptor
CHEMBL236
IC50 8.11 8.11 7.8 1
Mu-type opioid receptor
CHEMBL270
Ki 7.8 7.8 16.0 1
Mu-type opioid receptor
CHEMBL270
IC50 7.43 7.43 37.1 1
Delta-type opioid receptor
CHEMBL3222
IC50 7.08 7.08 84.0 1
Mu-type opioid receptor
CHEMBL270
EC50 6.62 6.62 239.9 2
Cholecystokinin receptor type A
CHEMBL1901
Ki 6.25 6.25 560.0 1
Cholecystokinin receptor type A
CHEMBL1901
IC50 6.24 6.24 575.4 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
IC50 6.03 6.03 933.2 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
Ki 6.03 6.03 930.0 1
Mu-type opioid receptor
CHEMBL4354
IC50 5.92 5.92 1200.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 150.0 nM Cavia porcellus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Delta-type opioid receptor Ki = 3.4 nM 8.47 Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 c... 16509592
Delta-type opioid receptor EC50 = 5.623 nM 8.25 Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed ... 16509592
Delta-type opioid receptor EC50 = 5.6 nM 8.25 Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed ... 16509592
Delta-type opioid receptor IC50 = 7.762 nM 8.11 Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 c... 16509592
Mu-type opioid receptor Ki = 16.0 nM 7.8 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells 16509592
Mu-type opioid receptor IC50 = 37.15 nM 7.43 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells 16509592
Delta-type opioid receptor IC50 = 84.0 nM 7.08 Agonist activity at delta opioid receptor by inhibition of muscle contraction in... 16509592
Mu-type opioid receptor EC50 = 239.88 nM 6.62 Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CH... 16509592
Mu-type opioid receptor EC50 = 240.0 nM 6.62 Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CH... 16509592
Cholecystokinin receptor type A Ki = 560.0 nM 6.25 Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells 16509592
Cholecystokinin receptor type A IC50 = 575.44 nM 6.24 Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells 16509592
Gastrin/cholecystokinin type B receptor IC50 = 933.25 nM 6.03 Displacement of [125I]CCK8 from human CCK2 receptor expressed in HEK293 cells 16509592
Gastrin/cholecystokinin type B receptor Ki = 930.0 nM 6.03 Displacement of [125I]CCK8 from human CCK2 receptor expressed in HEK293 cells 16509592
Mu-type opioid receptor IC50 = 1200.0 nM 5.92 Agonist activity at mu opioid receptor by inhibition of muscle contraction in el... 16509592

Literature References

PubMed DOI Target Context # Activities
16509592 10.1021/jm050851n Delta-type opioid receptor 6
16509592 10.1021/jm050851n Mu-type opioid receptor 6
16509592 10.1021/jm050851n Cholecystokinin receptor type A 2
16509592 10.1021/jm050851n Gastrin/cholecystokinin type B receptor 2
16509592 10.1021/jm050851n Cholecystokinin receptor 2

Data from ChEMBL 36 via Core Engine