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Compound Detail

CHEMBL265502

SURAMIN
🧪 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

Basic Information

ChEMBL ID CHEMBL265502
Name SURAMIN
Phase Phase III
Structure Type MOL
InChI Key FIAFUQMPZJWCLV-UHFFFAOYSA-N

Known Names

Farma FARMA-939 Fourneau Metaret Naganol NSC-34936 Suramin Suramine
72
Targets
260
Activities
4
Assay Types
11
PK Parameters
20
Publications
8
Known Names
1
Indications

Molecular Properties

1297.3
MW (Da)

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Natural Product
USAN Year 1997

Extended Properties

Molecular Formula C51H40N6O23S6
MW 1297.30

Indications

Carcinoma, Non-Small-Cell Lung

Activity Summary

IC50 191 meas. best 8.4
EC50 38 meas. best 8.4
Ki 26 meas. best 7.4
Kd 5 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metalloproteinase inhibitor 3
CHEMBL5465289
Kd 8.72 8.72 1.9 1
Trypanosoma brucei
CHEMBL612849
IC50 8.4 7.008 4.0 10
Trypanosoma brucei
CHEMBL612849
EC50 8.4 7.8333 4.0 3
Trypanosoma brucei brucei
CHEMBL612851
IC50 8.3 7.3752 5.0 23
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 8.12 7.564 7.5 10
Unchecked
CHEMBL612545
IC50 7.6 6.3113 25.0 8
NAD-dependent protein deacetylase sirtuin-1
CHEMBL4506
IC50 7.57 6.1785 27.0 13
Trypanosoma brucei brucei
CHEMBL612851
EC50 7.55 7.4267 28.0 9
Trypanosoma brucei rhodesiense
CHEMBL612348
EC50 7.48 7.2525 33.0 4
NON-PROTEIN TARGET
CHEMBL3879801
IC50 7.42 6.67 38.0 2
Ectonucleotide pyrophosphatase/phosphodiesterase family member 3
CHEMBL5580
Ki 7.4 7.4 40.0 1
Dengue virus
CHEMBL613757
Kd 7.4 7.4 40.0 1
Trypanosoma brucei gambiense
CHEMBL613768
IC50 7.19 7.19 64.0 1
P2Y purinoceptor 11
CHEMBL4867
Ki 6.95 6.735 112.2 2
NON-PROTEIN TARGET
CHEMBL3879801
EC50 6.92 6.92 120.0 1
Ectonucleotide pyrophosphatase/phosphodiesterase family member 1
CHEMBL5925
Ki 6.58 6.3017 260.0 6
Replicase polyprotein 1ab
CHEMBL4523582
IC50 6.58 6.58 260.0 3
Hepatitis B virus
CHEMBL613497
IC50 6.57 6.57 270.0 1
Trypanosoma evansi
CHEMBL1075362
IC50 6.42 6.42 380.0 1
Protein argonaute-2
CHEMBL4680043
IC50 6.16 6.16 690.0 1
Genome polyprotein
CHEMBL5980
Ki 6.12 6.12 750.0 2
Ectonucleotide pyrophosphatase/phosphodiesterase family member 3
CHEMBL5580
IC50 6.05 5.9643 890.0 7
P2X purinoceptor 1
CHEMBL2530
EC50 6.0 6.0 1000.0 1
P2X purinoceptor 1
CHEMBL2530
IC50 6.0 5.665 1000.0 2
Unchecked
CHEMBL612545
Ki 5.96 5.695 1100.0 4
NAD-dependent protein deacetylase sirtuin-2
CHEMBL4462
IC50 5.96 5.25 1100.0 10
Pyruvate kinase PKLR
CHEMBL1075126
Ki 5.96 5.96 1100.0 1
Nuclear receptor subfamily 1 group I member 2
CHEMBL3401
EC50 5.89 5.89 1300.0 1
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
IC50 5.85 5.695 1420.0 2
DNA-dependent protein kinase catalytic subunit
CHEMBL3142
IC50 5.77 5.77 1700.0 1
Nonstructural protein 3
CHEMBL4523954
EC50 5.71 5.71 1930.0 1
NAD-dependent protein lipoamidase sirtuin-4, mitochondrial
CHEMBL2163185
IC50 5.7 5.7 2000.0 1
NAD-dependent protein deacylase sirtuin-5, mitochondrial
CHEMBL2163183
IC50 5.7 4.7732 2000.0 19
Pyruvate kinase PKLR
CHEMBL1075126
IC50 5.66 5.66 2200.0 1
SARS-CoV-2
CHEMBL4303835
EC50 5.53 5.115 2930.0 2
ATP-dependent 6-phosphofructokinase
CHEMBL5686
IC50 5.52 5.52 3000.0 1
P2X purinoceptor 3
CHEMBL2998
EC50 5.52 5.175 3000.0 2
P2X purinoceptor 2
CHEMBL2135
IC50 5.4 4.9 4000.0 2
P2Y purinoceptor 12
CHEMBL2188
EC50 5.4 5.4 4000.0 1
P2X purinoceptor 5
CHEMBL2495
EC50 5.4 5.4 4000.0 1
P2X purinoceptor 1
CHEMBL2094
IC50 5.37 5.37 4270.0 2
Ectonucleoside triphosphate diphosphohydrolase 3
CHEMBL5897
IC50 5.37 5.37 4300.0 2
P2X purinoceptor 4
CHEMBL2104
IC50 5.33 5.29 4730.0 2
Tyrosyl-DNA phosphodiesterase 1
CHEMBL1075138
IC50 5.3 5.3 5000.0 2
Protein arginine N-methyltransferase 1
CHEMBL5524
IC50 5.27 5.005 5330.0 2
Chikungunya virus
CHEMBL4296563
IC50 5.25 5.25 5680.0 1
RmtA
CHEMBL1075069
IC50 5.23 5.23 5900.0 1
Putative silent information regulator 2
CHEMBL2311240
IC50 5.16 5.16 7000.0 1
Trypanosoma congolense
CHEMBL4296607
IC50 5.14 5.14 7200.0 1
HSP60/HSP10
CHEMBL4106131
IC50 5.14 5.05 7200.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 0.0057 mL.min-1.kg-1 Homo sapiens
CL 0.0011 mL.min-1.kg-1 Homo sapiens
CL 0.0057 mL.min-1.kg-1 Homo sapiens
CL 0.0057 mL.min-1.kg-1 Homo sapiens
Cmax 2300.0 nM Rattus norvegicus
Fu 0.003 - Homo sapiens
Fu 0.001 - Homo sapiens
Ka - - -
Ka - - -
MRT 1400.0 hr Homo sapiens
T1/2 1200.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Metalloproteinase inhibitor 3 Kd = 1.9 nM 8.72 Binding affinity to FLAG-tagged human TIMP3 expressed in HEK293 cells assessed a... 37517101
Trypanosoma brucei EC50 = 4.0 nM 8.4 Antitrypanosomal activity against Trypanosoma brucei 32527539
Trypanosoma brucei IC50 = 4.0 nM 8.4 Antitrypanosomal activity against Trypanosoma brucei 427 bloodstream forms asses... 29609908
Trypanosoma brucei brucei IC50 = 5.0 nM 8.3 Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei ... 33725631
Trypanosoma brucei brucei IC50 = 5.0 nM 8.3 Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei ... 31732256
Trypanosoma brucei brucei IC50 = 5.0 nM 8.3 Antitrypanosomal activity against Trypanosoma brucei brucei 427 after 72 hrs by ... 24826816
Trypanosoma brucei brucei IC50 = 5.0 nM 8.3 Antitrypanosomal activity against bloodstream-form Trypanosoma brucei brucei 427... 21322634
Trypanosoma brucei rhodesiense IC50 = 7.5 nM 8.12 Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodst... 25746816
Trypanosoma brucei rhodesiense IC50 = 7.5 nM 8.12 Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 16889962
Trypanosoma brucei EC50 = 20.0 nM 7.7 Effective concentration in vitro against the bloodstream trypomastigote form of ... 12540242
Trypanosoma brucei IC50 = 20.0 nM 7.7 Antitrypanosomal activity against suramin-sensitive Trypanosoma brucei Squib 427... 30638761
Trypanosoma brucei brucei IC50 = 20.0 nM 7.7 Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei bru... 29885575
Trypanosoma brucei rhodesiense IC50 = 20.0 nM 7.7 Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB-900 after ... 29197735
Trypanosoma brucei brucei IC50 = 20.0 nM 7.7 Antitrypanosomal activity against suramin-sensitive Trypanosoma brucei brucei Sq... 29197735
Trypanosoma brucei rhodesiense IC50 = 20.0 nM 7.7 Antiparasitic activity against suramin-sensitive trypomastigote stage of Trypano... 26922226
Trypanosoma brucei rhodesiense IC50 = 20.0 nM 7.7 Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesien... 25199582
Trypanosoma brucei brucei IC50 = 20.0 nM 7.7 Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Sq... 25199582
Unchecked IC50 = 25.0 nM 7.6 Inhibition of human Norovirus RNA-dependent RNA polymerase assessed as decrease ... 32294613
NAD-dependent protein deacetylase sirtuin-1 IC50 = 27.0 nM 7.57 Inhibition of human N-terminal His-tagged SIRT1 (183 to 664 residues) expressed ... 32163813
Trypanosoma brucei brucei EC50 = 28.0 nM 7.55 Antitrypanosomal activity against Trypanosoma brucei brucei assessed as reductio... 31931339

Literature References

PubMed DOI Target Context # Activities
17576845 10.1128/aac.00372-07 ADMET 23
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
37517101 10.1016/j.bmc.2023.117424 Unchecked 8
20070106 10.1021/jm901371v Homo sapiens 8
30108800 10.1039/C7MD00015D Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 6
16250663 10.1021/jm050301p P2Y purinoceptor 11 6
25818461 10.1016/j.bmcl.2015.03.018 NAD-dependent protein deacylase sirtuin-5, mitochondrial 6
30925051 10.1021/acs.jmedchem.9b00142 Zika virus 6
17880175 10.1021/np0702281 Leishmania donovani 5
20966043 10.1124/dmd.110.035105 Nuclear receptor subfamily 1 group I member 2 5
7265110 10.1021/jm00135a003 Rattus norvegicus 5
19786604 10.1128/aac.00422-09 Trypanosoma evansi 5
29604541 10.1016/j.ejmech.2018.03.048 Trypanosoma brucei brucei 4
18426954 10.1124/dmd.108.020479 ADMET 4
27720295 10.1016/j.bmcl.2016.09.051 NON-PROTEIN TARGET 4
1704064 10.1021/jm00105a033 Human immunodeficiency virus type 1 reverse transcriptase 4
25199582 10.1016/j.bmc.2014.08.005 Trypanosoma brucei brucei 4
30852084 10.1016/j.bmcl.2019.02.028 GroEL/GroES 4
29197735 10.1016/j.ejmech.2017.11.075 Trypanosoma brucei brucei 4

Data from ChEMBL 36 via Core Engine