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Compound Detail

CHEMBL268818

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CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NCc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)O

Basic Information

ChEMBL ID CHEMBL268818
Phase Preclinical
Structure Type BOTH
InChI Key SCUDNMPTYPZVCN-RSZDUZASSA-N
6
Targets
12
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

1452.8
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C70H109N21O13
MW 1452.78

Activity Summary

Ki 8 meas. best 10.54
IC50 4 meas. best 8.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL3952
Ki 10.54 8.7567 0.0 3
Kappa-type opioid receptor
CHEMBL3952
IC50 8.13 7.1767 7.3 3
Kappa-type opioid receptor
CHEMBL3614
Ki 7.83 7.83 14.8 1
Mu-type opioid receptor
CHEMBL270
Ki 7.51 7.26 31.1 2
Delta-type opioid receptor
CHEMBL269
Ki 6.75 6.75 176.0 1
Delta-type opioid receptor
CHEMBL3222
Ki 6.46 6.46 345.0 1
Cavia porcellus
CHEMBL369
IC50 6.0 6.0 990.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Kappa-type opioid receptor Ki = 0.029 nM 10.54 Affinity against Opioid receptor kappa 1 was determined by measuring the inhibit... 9276018
Kappa-type opioid receptor Ki = 3.24 nM 8.49 Affinity against Opioid receptor kappa 1 was determined by measuring the inhibit... 9276018
Kappa-type opioid receptor IC50 = 7.32 nM 8.13 Binding affinity towards Opioid receptor kappa 1 using [3H]diprenorphine as radi... 9276018
Kappa-type opioid receptor Ki = 14.8 nM 7.83 Displacement of [3H]diprenorphine from rat kappa opioid receptor expressed in CH... 19807094
Mu-type opioid receptor Ki = 31.1 nM 7.51 Affinity against Opioid receptor mu 1 was determined by measuring the inhibition... 9276018
Kappa-type opioid receptor Ki = 58.1 nM 7.24 Affinity against Opioid receptor kappa 3 was determined by measuring the inhibit... 9276018
Kappa-type opioid receptor IC50 = 93.7 nM 7.03 Binding affinity towards Opioid receptor kappa 1 using [3H]diprenorphine as radi... 9276018
Mu-type opioid receptor Ki = 98.1 nM 7.01 Displacement of [3H]DAMGO from rat mu opioid receptor expressed in CHO cells 19807094
Delta-type opioid receptor Ki = 176.0 nM 6.75 Affinity against Opioid receptor delta 1 was determined by measuring the inhibit... 9276018
Delta-type opioid receptor Ki = 345.0 nM 6.46 Displacement of [3H]DPDPE from mouse delta opioid receptor expressed in CHO cell... 19807094
Kappa-type opioid receptor IC50 = 427.0 nM 6.37 Affinity against Opioid receptor kappa 2 was determined by measuring the inhibit... 9276018
Cavia porcellus IC50 = 990.0 nM 6.0 The opioid activity by guinea pig ileum assay 9276018

Literature References

PubMed DOI Target Context # Activities
9276018 10.1021/jm960747t Kappa-type opioid receptor 7
19807094 10.1021/jm900715m Unchecked 2
19807094 10.1021/jm900715m Kappa-type opioid receptor 2
9276018 10.1021/jm960747t Mu-type opioid receptor 1
9276018 10.1021/jm960747t Delta-type opioid receptor 1
9276018 10.1021/jm960747t Cavia porcellus 1
9276018 10.1021/jm960747t Opioid receptors; mu/kappa/delta 1
9276018 10.1021/jm960747t Unchecked 1
19807094 10.1021/jm900715m Delta-type opioid receptor 1
19807094 10.1021/jm900715m Mu-type opioid receptor 1

Data from ChEMBL 36 via Core Engine