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Compound Detail

CHEMBL413376

SURAMIN HEXASODIUM
🧪 Phase III
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🧪 Phase III
Cc1ccc(C(=O)Nc2ccc(S(=O)(=O)[O-])c3cc(S(=O)(=O)[O-])cc(S(=O)(=O)[O-])c23)cc1NC(=O)c1cccc(NC(=O)Nc2cccc(C(=O)Nc3cc(C(=O)Nc4ccc(S(=O)(=O)[O-])c5cc(S(=O)(=O)[O-])cc(S(=O)(=O)[O-])c45)ccc3C)c2)c1.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL413376
Name SURAMIN HEXASODIUM
Phase Phase III
Structure Type MOL
InChI Key VAPNKLKDKUDFHK-UHFFFAOYSA-H
Parent Compound CHEMBL265502
Active Moiety CHEMBL265502

Known Names

BAY-205 BAYER-205 CI-1003 FOURNEAU 309 FOURNEAU-309 Nagananinum Naphuride NF-060 NSC-758165 Suramin hexasodium Suramin sodium Suramina de sodio +2 more
13
Targets
20
Activities
2
Assay Types
0
PK Parameters
20
Publications
14
Known Names
15
Indications
1
Mechanisms

Molecular Properties

1297.3
MW (Da)

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Year 1997

Extended Properties

Molecular Formula C51H34N6Na6O23S6
MW 1429.19

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Acidic fibroblast growth factor inhibitor INHIBITOR Fibroblast growth factor 1

Indications

Leishmaniasis Prostatic Neoplasms, Castration-Resistant Trypanosomiasis Acute Kidney Injury Adrenal Cortex Neoplasms Carcinoma, Non-Small-Cell Lung Central Nervous System Neoplasms Child Development Disorders, Pervasive Multiple Myeloma Prostatic Neoplasms Breast Neoplasms Carcinoma, Renal Cell Colorectal Neoplasms Hand, Foot and Mouth Disease Urinary Bladder Neoplasms

ATC Classification

P01CX02
suramin sodium
Level 1: ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
Level 2: ANTIPROTOZOALS

Activity Summary

IC50 17 meas. best 7.37
EC50 3 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 7.57 7.57 27.0 1
Trypanosoma brucei
CHEMBL612849
IC50 7.37 7.37 43.0 1
NAD-dependent protein deacetylase sirtuin-1
CHEMBL4506
IC50 6.52 6.52 300.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 6.52 6.5133 300.0 3
dengue virus type 2
CHEMBL613966
EC50 6.46 6.46 350.0 1
NAD-dependent protein deacetylase sirtuin-2
CHEMBL4462
IC50 5.92 5.92 1200.0 2
P2Y purinoceptor 13
CHEMBL3321651
IC50 5.64 5.64 2300.0 1
Replicase polyprotein 1ab
CHEMBL4523582
IC50 5.19 5.19 6500.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 5.09 5.09 8200.0 1
Signal transducer and activator of transcription 1-alpha/beta
CHEMBL6101
IC50 5.04 5.04 9100.0 1
Signal transducer and activator of transcription 5A
CHEMBL5403
IC50 5.03 5.03 9400.0 1
Plasmodium falciparum
CHEMBL364
IC50 5.0 4.92 10000.0 5
Signal transducer and activator of transcription 5B
CHEMBL5817
IC50 4.98 4.98 10400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 27.0 nM 7.57 Inhibition of Norovirus RNA dependent RNA polymerase by spectrophotometry 26258852
Trypanosoma brucei IC50 = 43.0 nM 7.37 In vitro anti-protozoal parasite activity against Trypanosoma brucei TB-1 12781185
Trypanosoma brucei brucei IC50 = 300.0 nM 6.52 Antitrypanosomal activity against Trypanosoma brucei brucei after 48 hrs 17239596
NAD-dependent protein deacetylase sirtuin-1 IC50 = 300.0 nM 6.52 Inhibition of SIRT1 21080630
Trypanosoma brucei brucei IC50 = 310.0 nM 6.51 Trypanocidal activity against Trypanosoma brucei brucei after 48 hrs 16516467
Trypanosoma brucei brucei IC50 = 310.0 nM 6.51 Antitrypanosomal activity against Trypanosoma brucei brucei TC221 infected in mo... 22376072
dengue virus type 2 EC50 = 350.0 nM 6.46 Antiviral activity against DENV2 New Guinea C infected in golden hamster BHK-21 ... 36167010
NAD-dependent protein deacetylase sirtuin-2 IC50 = 1200.0 nM 5.92 Inhibition of SIRT2 21080630
NAD-dependent protein deacetylase sirtuin-2 IC50 = 1200.0 nM 5.92 Inhibition of human recombinant SIRT2 25515955
P2Y purinoceptor 13 IC50 = 2300.0 nM 5.64 Antagonist activity at P2Y13 (unknown origin) 27413802
Replicase polyprotein 1ab IC50 = 6500.0 nM 5.19 Inhibition of N-terminal His6-tagged recombinant full length SARS-CoV-2 3CLpro e... 37244162
Human immunodeficiency virus 1 EC50 = 8200.0 nM 5.09 Antiviral activity against HIV-1 (HTLV-IIIB) in MT-4 cells 8336338
Signal transducer and activator of transcription 1-alpha/beta IC50 = 9100.0 nM 5.04 Inhibition of 5-carboxyfluorescein-GpYDKPHVL-OH binding to STAT1 (unknown origin... 28624143
Signal transducer and activator of transcription 5A IC50 = 9400.0 nM 5.03 Inhibition of 5-carboxyfluorescein-GpYLVLDKW-OH binding to C-terminal 6x-His-tag... 28624143
Plasmodium falciparum IC50 = 10000.0 nM 5.0 Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... 19734910
Signal transducer and activator of transcription 5B IC50 = 10400.0 nM 4.98 Inhibition of 5-carboxyfluorescein-GpYLVLDKW-OH binding to STAT5B SH2 domain (un... 28624143
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910

Literature References

PubMed DOI Target Context # Activities
19734910 10.1038/nchembio.215 Plasmodium falciparum 5
- 10.6019/CHEMBL5724709 Fibroblast 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
31727469 10.1016/j.ejmech.2019.111789 P2Y purinoceptor 2 2
31727469 10.1016/j.ejmech.2019.111789 Uracil nucleotide/cysteinyl leukotriene receptor 2
28624143 10.1016/j.bmcl.2017.06.012 Signal transducer and activator of transcription 5A 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL5724709 U2OS 2
- 10.6019/CHEMBL5724709 HEK-293T 2
16516467 10.1016/j.bmcl.2006.02.026 J774 2
16516467 10.1016/j.bmcl.2006.02.026 Trypanosoma brucei brucei 2
8336338 10.1021/jm00066a008 Human immunodeficiency virus 1 2
21306904 10.1016/j.bmc.2011.01.010 Trypanosoma brucei brucei 1
- 10.6019/CHEMBL5724796 Bromodomain-containing protein 4 1
21080630 10.1021/jm100861p NAD-dependent protein deacetylase sirtuin-2 1
21080630 10.1021/jm100861p NAD-dependent protein deacetylase sirtuin-1 1
25515955 10.1016/j.bmc.2014.11.027 NAD-dependent protein deacetylase sirtuin-2 1
26258852 10.1021/acs.jmedchem.5b00762 Unchecked 1
17417631 10.1038/nchembio873 Unchecked 1
16516467 10.1016/j.bmcl.2006.02.026 Rhodesain 1

Data from ChEMBL 36 via Core Engine