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Compound Detail

CHEMBL386212

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CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL386212
Phase Preclinical
Structure Type MOL
InChI Key KYWMQIRORZGHDH-QOIWPSRPSA-N
6
Targets
14
Activities
3
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

1032.2
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C53H65N11O11
MW 1032.17

Activity Summary

IC50 8 meas. best 8.59
Ki 4 meas. best 8.96
EC50 2 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 8.96 8.96 1.1 1
Delta-type opioid receptor
CHEMBL236
IC50 8.59 8.145 2.6 2
Delta-type opioid receptor
CHEMBL3222
IC50 7.92 7.92 12.0 1
Mu-type opioid receptor
CHEMBL270
Ki 7.89 7.89 13.0 1
Delta-type opioid receptor
CHEMBL236
EC50 7.72 7.72 19.0 1
Mu-type opioid receptor
CHEMBL270
IC50 7.54 7.335 28.8 2
Mu-type opioid receptor
CHEMBL270
EC50 7.12 7.12 75.0 1
Mu-type opioid receptor
CHEMBL4354
IC50 7.03 7.03 93.0 1
Cholecystokinin receptor type A
CHEMBL1901
Ki 5.16 5.16 7000.0 1
Cholecystokinin receptor type A
CHEMBL1901
IC50 5.15 5.15 7079.5 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
IC50 5.11 5.11 7762.5 1
Gastrin/cholecystokinin type B receptor
CHEMBL298
Ki 5.11 5.11 7700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Delta-type opioid receptor Ki = 1.1 nM 8.96 Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 c... 17201419
Delta-type opioid receptor IC50 = 2.57 nM 8.59 Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 c... 17201419
Delta-type opioid receptor IC50 = 12.0 nM 7.92 Activity at delta opioid receptor in ICR mouse by MVD assay 17201419
Mu-type opioid receptor Ki = 13.0 nM 7.89 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells 17201419
Delta-type opioid receptor EC50 = 19.0 nM 7.72 Activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma... 17201419
Delta-type opioid receptor IC50 = 19.95 nM 7.7 Activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma... 17201419
Mu-type opioid receptor IC50 = 28.84 nM 7.54 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells 17201419
Mu-type opioid receptor IC50 = 74.13 nM 7.13 Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS bind... 17201419
Mu-type opioid receptor EC50 = 75.0 nM 7.12 Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS bind... 17201419
Mu-type opioid receptor IC50 = 93.0 nM 7.03 Activity at mu opioid receptor assessed as contraction of electrically-stimulate... 17201419
Cholecystokinin receptor type A Ki = 7000.0 nM 5.16 Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cell... 17201419
Cholecystokinin receptor type A IC50 = 7079.46 nM 5.15 Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cell... 17201419
Gastrin/cholecystokinin type B receptor IC50 = 7762.47 nM 5.11 Displacement of [125I]CCK8-SO3 from human CCK2 receptor expressed in HEK293 cell... 17201419
Gastrin/cholecystokinin type B receptor Ki = 7700.0 nM 5.11 Displacement of [125I]CCK8-SO3 from human CCK2 receptor expressed in HEK293 cell... 17201419

Literature References

PubMed DOI Target Context # Activities
17201419 10.1021/jm061268p Delta-type opioid receptor 6
17201419 10.1021/jm061268p Mu-type opioid receptor 6
17201419 10.1021/jm061268p Cholecystokinin receptor type A 2
17201419 10.1021/jm061268p Gastrin/cholecystokinin type B receptor 2

Data from ChEMBL 36 via Core Engine