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Compound Detail

CHEMBL451930

PLITIDEPSIN
💊 Approved Drug
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💊 Approved Drug
CC[C@H](C)[C@H]1NC(=O)[C@@H](NC(=O)[C@@H](CC(C)C)N(C)C(=O)[C@@H]2CCCN2C(=O)C(C)=O)[C@@H](C)OC(=O)[C@H](Cc2ccc(OC)cc2)N(C)C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)C(=O)[C@H](C(C)C)OC(=O)C[C@@H]1O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL451930
Name PLITIDEPSIN
Phase Approved
Structure Type MOL
InChI Key UUSZLLQJYRSZIS-LXNNNBEUSA-N

Known Names

Aplidine Plitidepsin Plitidepsina Plitidepsine
6
Targets
12
Activities
2
Assay Types
0
PK Parameters
10
Publications
4
Known Names
7
Indications
1
Mechanisms

Molecular Properties

1110.4
MW (Da)

Drug Information

Molecule Type Small molecule
First Approval 2018
Availability Unknown
Chirality Single Enantiomer

Flags

Natural Product
USAN Stem -depsin

Extended Properties

Molecular Formula C57H87N7O15
MW 1110.36

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Elongation factor 1-alpha 2 inhibitor INHIBITOR Elongation factor 1-alpha 2 ✓ ✓

Indications

Multiple Myeloma Neoplasms Severe Acute Respiratory Syndrome Liposarcoma Lymphoma Primary Myelofibrosis Prostatic Neoplasms, Castration-Resistant

ATC Classification

L01XX57
plitidepsin
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS

Activity Summary

IC50 8 meas. best 9.7
EC50 4 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P388
CHEMBL389
 IC50 9.7 7.6667 0.2 3
A549
CHEMBL392
 IC50 9.7 9.7 0.2 1
HT-29
CHEMBL384
 IC50 9.3 9.3 0.5 1
SK-MEL-28
CHEMBL614919
 IC50 9.3 9.3 0.5 1
SARS-CoV-2
CHEMBL4303835
 EC50 9.15 7.94 0.7 4
Unchecked
CHEMBL612545
 IC50 8.8 7.55 1.6 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P388 IC50 = 0.2 nM 9.7 Antiproliferative activity against mouse P388 cells assessed as cell growth inhi... 33592144
A549 IC50 = 0.2 nM 9.7 Antiproliferative activity against human A549 cells assessed as cell growth inhi... 33592144
HT-29 IC50 = 0.5 nM 9.3 Antiproliferative activity against human HT-29 cells assessed as cell growth inh... 33592144
SK-MEL-28 IC50 = 0.5 nM 9.3 Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth... 33592144
SARS-CoV-2 EC50 = 0.7 nM 9.15 Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 c... 37229831
SARS-CoV-2 EC50 = 0.7 nM 9.15 Antiviral activity against SARS-CoV-2 infected in African green monkey Vero cell... 38160620
Unchecked IC50 = 1.6 nM 8.8 Cytotoxicity against human 293T/ACE2 cells assessed as reduction in cell growth ... 37229831
SARS-CoV-2 EC50 = 100.0 nM 7.0 Antiviral activity against SARS-CoV-2 infected in human A549-ACE2 cells assessed... 37229831
P388 IC50 = 100.0 nM 7.0 Inhibition of DNA synthesis in mouse P388 cells measured after 72 hrs 33592144
SARS-CoV-2 EC50 = 350.0 nM 6.46 Antiviral activity against luciferase-expressing pseudovirus encoding SARS-CoV-2... 37229831
Unchecked IC50 = 500.0 nM 6.3 Inhibition of EIF1A (unknown origin) 33592144
P388 IC50 = 500.0 nM 6.3 Inhibition of protein synthesis in mouse P388 cells measured after 72 hrs 33592144

Literature References

PubMed DOI Target Context # Activities
33592144 10.1021/acs.jmedchem.0c01746 P388 4
37229831 10.1016/j.ejmech.2023.115503 SARS-CoV-2 3
1812209 10.1021/np50078a001 Leukemia cell 1
1812209 10.1021/np50078a001 Melanoma cell 1
33592144 10.1021/acs.jmedchem.0c01746 Unchecked 1
33592144 10.1021/acs.jmedchem.0c01746 A549 1
33592144 10.1021/acs.jmedchem.0c01746 HT-29 1
33592144 10.1021/acs.jmedchem.0c01746 SK-MEL-28 1
37229831 10.1016/j.ejmech.2023.115503 Unchecked 1
38160620 10.1016/j.ejmech.2023.116069 SARS-CoV-2 1

Data from ChEMBL 36 via Core Engine