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Assay Detail

CHEMBL4372183

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Binding
Inhibition of human plasmin using Ac-RM(O2)YR-pNA as substrate after 30 mins
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Plasminogen (CHEMBL1801)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.
Swedberg JE, Wu G, Mahatmanto T, Durek T, Caradoc-Davies TT, Whisstock JC, Law RHP, Craik DJ.
J Med Chem (2019) 62 : 552 -560
PubMed 30520638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.89 10.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4569923 1 10.39
CHEMBL4439523 1 10.29
CHEMBL4588827 1 9.85
CHEMBL4454304 1 9.68
CHEMBL4579797 1 9.35
CHEMBL4592533 1 9.21
CHEMBL4435567 1 9.18
CHEMBL4443353 1 9.18
CHEMBL4453437 1 8.96
CHEMBL4471930 1 8.92
CHEMBL4515559 1 8.74
CHEMBL4550948 1 8.70
CHEMBL4563203 1 8.60
CHEMBL4585149 1 8.33
CHEMBL4483688 1 8.08
CHEMBL4558203 1 7.80
CHEMBL4580142 1 7.80
CHEMBL4458397 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4569923 Ki = 0.041 nM 10.39
CHEMBL4439523 Ki = 0.051 nM 10.29
CHEMBL4588827 Ki = 0.14 nM 9.85
CHEMBL4454304 Ki = 0.21 nM 9.68
CHEMBL4579797 Ki = 0.45 nM 9.35
CHEMBL4592533 Ki = 0.61 nM 9.21
CHEMBL4435567 Ki = 0.66 nM 9.18
CHEMBL4443353 Ki = 0.66 nM 9.18
CHEMBL4453437 Ki = 1.1 nM 8.96
CHEMBL4471930 Ki = 1.2 nM 8.92
CHEMBL4515559 Ki = 1.8 nM 8.74
CHEMBL4550948 Ki = 2.0 nM 8.70
CHEMBL4563203 Ki = 2.5 nM 8.60
CHEMBL4585149 Ki = 4.7 nM 8.33
CHEMBL4483688 Ki = 8.3 nM 8.08
CHEMBL4558203 Ki = 16.0 nM 7.80
CHEMBL4580142 Ki = 16.0 nM 7.80
CHEMBL4458397 Ki = 120.0 nM 6.92