nafamostat
inhibitor of trypsin, plasmin, pancreatic kallikrein, plasma kallikrein & thrombin; strongly inhibits esterolytic activities of C1r & C1 esterase complement-mediated hemolysis; antineoplastic; RN given refers to parent cpd
Ligand Summary
UNII: Y25LQ0H97D
PubChem: 11961431
PubChem: 4413
Guide to Pharmacology: 4262
ChEMBL: CHEMBL3989553
ChEMBL: CHEMBL273264
DrugCentral: 1867
LyCHI: TS79G7GAB2QX
Target Activities
HGFAC
Hepatocyte growth factor activator
5 Activities
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1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.6 | ACS Med. Chem. Lett., (2014) 5:11:1219 | ||||
Ki | 7.6 | Bioorg. Med. Chem., (2015) 23:10:2328 | ||||
IC50 | 6.82 | Bioorg. Med. Chem., (2015) 23:10:2328 | ||||
EC50 | 6.31 | ACS Med. Chem. Lett., (2014) 5:11:1219 | ||||
Ki | 7.6 | |||||
C1R
Complement C1r subcomponent
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 4.92 | |||||
IC50 | 6.1 | J Med Chem, (2018) 61:8:3253 | ||||
IC50 | 6 | Bioorg. Med. Chem. Lett., (1996) 6:6:679 | ||||
IC50 | 6 | INHIBITOR | ||||
PRSS1
Trypsin-1
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.77 | |||||
IC50 | 7.77 | Bioorg. Med. Chem. Lett., (1999) 9:6:815 | ||||
IC50 | 7.7 | Bioorg. Med. Chem. Lett., (1996) 6:6:679 | ||||
IC50 | 7.77 | INHIBITOR | ||||
HPN
Serine protease hepsin
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9.28 | ACS Med. Chem. Lett., (2014) 5:11:1219 | ||||
Ki | 9.28 | Bioorg. Med. Chem., (2015) 23:10:2328 | ||||
IC50 | 8.3 | J Med Chem, (2018) 61:10:4335 | ||||
Ki | 9.28 | |||||
ST14
Suppressor of tumorigenicity 14 protein
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 10.7 | ACS Med. Chem. Lett., (2014) 5:11:1219 | ||||
Ki | 10.7 | Bioorg. Med. Chem., (2015) 23:10:2328 | ||||
Ki | 10.7 | |||||
C1S
Complement C1s subcomponent
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.54 | J Med Chem, (2018) 61:8:3253 | ||||
IC50 | 6.85 | Bioorg. Med. Chem. Lett., (1996) 6:6:679 | ||||
IC50 | 6.85 | |||||
ASIC3
Acid-sensing ion channel 3
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.6 | |||||
IC50 | 5.6 | BLOCKER | ||||
TPSAB1
Tryptase alpha/beta-1
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 10 | |||||
IC50 | 10 | INHIBITOR | ||||
KLK1
Kallikrein-1
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.19 | Bioorg. Med. Chem. Lett., (1996) 6:6:679 | ||||
IC50 | 6.19 | |||||
PLG
Plasminogen
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.62 | Bioorg. Med. Chem. Lett., (1996) 6:6:679 | ||||
Ki | 6.39 | J Med Chem, (2020) 63:4:1445 | ||||
ASIC1
Acid-sensing ion channel 1
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 4.9 | |||||
ASIC2
Acid-sensing ion channel 2
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 4.2 | |||||
TRPM7
Transient receptor potential cation channel subfamily M member 7
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 3.21 | |||||
F2
Prothrombin
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.54 | Bioorg. Med. Chem. Lett., (1996) 6:6:679 | ||||
TMPRSS2
Transmembrane protease serine 2
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7 | INHIBITOR | ||||