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Compound Detail

CHEMBL4285275

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CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]4CSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)CNC1=O)C(=O)N[C@@H](CO)C(=O)N4)NC(=O)[C@@H]1CCCN1C(=O)[C@H]([C@@H](C)CC)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC3=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1CCC[C@H]1C(=O)N2

Basic Information

ChEMBL ID CHEMBL4285275
Phase Preclinical
Structure Type MOL
InChI Key LNKLNUAMTRHBLB-CGJDGIRVSA-N
12
Targets
16
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

3140.7
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C133H207N37O39S6
MW 3140.74

Activity Summary

IC50 16 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
U-937
CHEMBL612794
IC50 6.58 6.58 260.0 1
HUVEC
CHEMBL613979
IC50 6.46 6.34 350.0 2
U-87 MG
CHEMBL614247
IC50 6.35 5.65 450.0 3
MM96L
CHEMBL614170
IC50 6.19 6.19 650.0 1
HeLa
CHEMBL399
IC50 6.16 6.16 700.0 1
PC-3
CHEMBL390
IC50 6.1 6.1 800.0 1
U-251
CHEMBL615022
IC50 6.1 6.1 790.0 1
HT-29
CHEMBL384
IC50 6.06 6.06 870.0 1
HFF-1
CHEMBL4296427
IC50 5.89 5.89 1300.0 1
MDA-MB-231
CHEMBL400
IC50 5.82 5.82 1500.0 1
SH-SY5Y
CHEMBL614910
IC50 5.67 5.59 2150.0 2
Erythrocyte
CHEMBL4296518
IC50 4.44 4.44 36000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
U-937 IC50 = 260.0 nM 6.58 Cytotoxicity against human U-937 cells assessed as inhibition of cell growth inc... 36525646
HUVEC IC50 = 350.0 nM 6.46 Cytotoxicity against HUVEC after 24 hrs by MTT assay 30387611
U-87 MG IC50 = 450.0 nM 6.35 Cytotoxicity against human U-87 MG cells by sulforhodamine B assay 35044783
HUVEC IC50 = 600.0 nM 6.22 Cytotoxicty against HUVEC after 24 hrs by MTT assay 32437150
MM96L IC50 = 650.0 nM 6.19 Cytotoxicity against human MM96L after 24 hrs by MTT assay 30387611
HeLa IC50 = 700.0 nM 6.16 Cytotoxicty against human HeLa cells after 24 hrs by MTT assay 32437150
PC-3 IC50 = 800.0 nM 6.1 Cytotoxicty against human PC3 cells after 24 hrs by MTT assay 32437150
U-251 IC50 = 790.0 nM 6.1 Cytotoxicity against human U-251 cells by sulforhodamine B assay 35044783
HT-29 IC50 = 870.0 nM 6.06 Cytotoxicity against human HT-29 after 24 hrs by MTT assay 30387611
HFF-1 IC50 = 1300.0 nM 5.89 Cytotoxicity against human HFF1 after 24 hrs by MTT assay 30387611
MDA-MB-231 IC50 = 1500.0 nM 5.82 Cytotoxicity against human MDA-MB-231 after 24 hrs by MTT assay 30387611
SH-SY5Y IC50 = 2150.0 nM 5.67 Cytotoxicity against human SH-SY5Y cells using best fit nonlinear regression ana... 35044783
SH-SY5Y IC50 = 3070.0 nM 5.51 Cytotoxicity against human SH-SY5Y cells assessed as cell viability using raw in... 35044783
U-87 MG IC50 = 4500.0 nM 5.35 Cytotoxicity against human U-87 MG cells using best fit nonlinear regression ana... 35044783
U-87 MG IC50 = 5660.0 nM 5.25 Cytotoxicity against human U-87 MG cells assessed as cell viability using raw in... 35044783
Erythrocyte IC50 = 36000.0 nM 4.44 Hemolytic activity against human RBC after 1 hr 30387611

Literature References

Data from ChEMBL 36 via Core Engine