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Compound Detail

CHEMBL5084333

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CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)CN)CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CCCCN)C(=O)N4C[C@@H](O)C[C@H]4C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]4CCCN4C1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N3)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC2=O

Basic Information

ChEMBL ID CHEMBL5084333
Phase Preclinical
Structure Type MOL
InChI Key UAZZCOHRYBPQRO-UVTNKDQESA-N
9
Targets
9
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

3327.8
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C135H204N42O43S7
MW 3327.84

Activity Summary

EC50 9 meas. best 8.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 8.02 8.02 9.5 1
Sodium channel protein type 2 subunit alpha
CHEMBL3399
EC50 7.3 7.3 50.4 1
Sodium channel protein type 9 subunit alpha
CHEMBL4296
EC50 6.89 6.89 129.0 1
Sodium channel protein type 8 subunit alpha
CHEMBL1914275
EC50 6.83 6.83 147.6 1
Sodium channel protein type 5 subunit alpha
CHEMBL1980
EC50 6.81 6.81 155.6 1
Sodium channel protein type 1 subunit alpha
CHEMBL1845
EC50 6.77 6.77 171.5 1
Sodium channel protein type 3 subunit alpha
CHEMBL4966
EC50 6.77 6.77 170.2 1
Sodium channel protein type 4 subunit alpha
CHEMBL3509
EC50 6.09 6.09 810.6 1
Artemia salina
CHEMBL612341
EC50 5.21 5.21 6100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34445875 10.1021/acs.jnatprod.1c00104 Artemia salina 1
34445875 10.1021/acs.jnatprod.1c00104 Sodium channel protein type 1 subunit alpha 1
34445875 10.1021/acs.jnatprod.1c00104 Sodium channel protein type 2 subunit alpha 1
34445875 10.1021/acs.jnatprod.1c00104 Sodium channel protein type 3 subunit alpha 1
34445875 10.1021/acs.jnatprod.1c00104 Sodium channel protein type 4 subunit alpha 1
34445875 10.1021/acs.jnatprod.1c00104 Sodium channel protein type 5 subunit alpha 1
34445875 10.1021/acs.jnatprod.1c00104 Sodium channel protein type 8 subunit alpha 1
34445875 10.1021/acs.jnatprod.1c00104 Sodium channel protein type 9 subunit alpha 1
34445875 10.1021/acs.jnatprod.1c00104 Sodium channel protein type 10 subunit alpha 1
34445875 10.1021/acs.jnatprod.1c00104 Unchecked 1

Data from ChEMBL 36 via Core Engine