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Compound Detail

CHEMBL3318132

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CSCC[C@@H]1NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H]3CSSC[C@H](NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC3=O)C(=O)N2

Basic Information

ChEMBL ID CHEMBL3318132
Phase Preclinical
Structure Type BOTH
InChI Key XOAUGYVLRSCGBG-ZJDFQAAZSA-N
9
Targets
13
Activities
1
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

3826.7
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C168H250N46O41S8
MW 3826.66

Activity Summary

IC50 13 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 9 subunit alpha
CHEMBL4296
IC50 9.52 9.0133 0.3 3
Sodium channel protein type 7 subunit alpha
CHEMBL3585
IC50 9.1 9.1 0.8 1
Sodium channel protein type 1 subunit alpha
CHEMBL1845
IC50 7.8 7.8 16.0 1
Sodium channel protein type 3 subunit alpha
CHEMBL5163
IC50 7.6 7.6 25.0 1
Sodium channel protein type 4 subunit alpha
CHEMBL2072
IC50 7.52 7.31 30.0 2
Sodium channel protein type 8 subunit alpha
CHEMBL5202
IC50 7.5 7.5 32.0 1
Sodium channel protein type 2 subunit alpha
CHEMBL4187
IC50 7.1 7.1 79.0 1
Sodium channel protein type 5 subunit alpha
CHEMBL1980
IC50 7.05 6.725 90.0 2
Sodium channel protein type 2 subunit alpha
CHEMBL3399
IC50 6.98 6.98 105.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium channel protein type 9 subunit alpha IC50 = 0.3 nM 9.52 Inhibition of human Nav1.7 expressed in HEK293 cells at holding potential of -12... 30139550
Sodium channel protein type 7 subunit alpha IC50 = 0.8 nM 9.1 Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 9 subunit alpha IC50 = 1.0 nM 9.0 Inhibition of human Nav1.7 expressed in HEK-293 cells at -130 to -110 mV holding... 25026046
Sodium channel protein type 9 subunit alpha IC50 = 3.0 nM 8.52 Inhibition of human NaV1.7 at -140 mV holding potential by whole-cell patch clam... 25658507
Sodium channel protein type 1 subunit alpha IC50 = 16.0 nM 7.8 Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 3 subunit alpha IC50 = 25.0 nM 7.6 Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 4 subunit alpha IC50 = 30.0 nM 7.52 Inhibition of human NaV1.4 at -140 mV holding potential by whole-cell patch clam... 25658507
Sodium channel protein type 8 subunit alpha IC50 = 32.0 nM 7.5 Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 2 subunit alpha IC50 = 79.0 nM 7.1 Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 4 subunit alpha IC50 = 79.0 nM 7.1 Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 5 subunit alpha IC50 = 90.0 nM 7.05 Inhibition of human NaV1.5 at -140 mV holding potential by whole-cell patch clam... 25658507
Sodium channel protein type 2 subunit alpha IC50 = 105.0 nM 6.98 Inhibition of rat Nav1.7 expressed in HEK-293 cells at -130 to -110 mV holding p... 25026046
Sodium channel protein type 5 subunit alpha IC50 = 400.0 nM 6.4 Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay 31012583

Literature References

PubMed DOI Target Context # Activities
31012583 10.1021/acs.jmedchem.8b01906 Unchecked 6
30139550 10.1016/j.bmcl.2018.08.007 Unchecked 6
31012583 10.1021/acs.jmedchem.8b01906 Rattus norvegicus 4
25026046 10.1021/jm500687u Sodium channel protein type 9 subunit alpha 2
25026046 10.1021/jm500687u No relevant target 2
25658507 10.1021/jm501765v Sodium channel protein type 5 subunit alpha 1
25658507 10.1021/jm501765v Sodium channel protein type 9 subunit alpha 1
25658507 10.1021/jm501765v Sodium channel protein type 4 subunit alpha 1
25026046 10.1021/jm500687u Unchecked 1
30139550 10.1016/j.bmcl.2018.08.007 Sodium channel protein type 9 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 7 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 1 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 2 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 3 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 4 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 5 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 8 subunit alpha 1
25026046 10.1021/jm500687u Sodium channel protein type 2 subunit alpha 1

Data from ChEMBL 36 via Core Engine