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Assay Detail

CHEMBL3295545

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to full length Glu-plasminogen in human plasma assessed as inhibition of interaction with fibrin in presence of tPA
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasminogen (CHEMBL1801)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
Cheng L, Pettersen D, Ohlsson B, Schell P, Karle M, Evertsson E, Pahlén S, Jonforsen M, Plowright AT, Boström J, Fex T, Thelin A, Hilgendorf C, Xue Y, Wahlund G, Lindberg W, Larsson LO, Gustafsson D.
ACS Med Chem Lett (2014) 5 : 538 -543
PubMed 24900876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.77 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3287849 1 6.55
CHEMBL3287856 1 6.44
CHEMBL3287854 1 6.41
CHEMBL3287851 2 6.36
CHEMBL3287857 1 6.35
CHEMBL3287847 1 6.24
CHEMBL3287852 1 6.11
CHEMBL311761 1 6.10
CHEMBL3287850 1 5.99
CHEMBL3287853 1 5.97
CHEMBL3287855 1 5.90
CHEMBL144416 1 5.70
CHEMBL3287844 1 5.68
CHEMBL877 TRANEXAMIC ACID 4.0 1 5.51
CHEMBL3287843 1 4.40
CHEMBL1046 AMINOCAPROIC ACID 4.0 1 4.40
CHEMBL3287842 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3287849 IC50 = 280.0 nM 6.55
CHEMBL3287856 IC50 = 360.0 nM 6.44
CHEMBL3287854 IC50 = 390.0 nM 6.41
CHEMBL3287851 IC50 = 440.0 nM 6.36
CHEMBL3287857 IC50 = 450.0 nM 6.35
CHEMBL3287847 IC50 = 580.0 nM 6.24
CHEMBL3287852 IC50 = 770.0 nM 6.11
CHEMBL311761 IC50 = 800.0 nM 6.10
CHEMBL3287850 IC50 = 1020.0 nM 5.99
CHEMBL3287853 IC50 = 1060.0 nM 5.97
CHEMBL3287855 IC50 = 1260.0 nM 5.90
CHEMBL3287851 IC50 = 1500.0 nM 5.82
CHEMBL144416 IC50 = 2000.0 nM 5.70
CHEMBL3287844 IC50 = 2100.0 nM 5.68
CHEMBL877 TRANEXAMIC ACID IC50 = 3100.0 nM 5.51
CHEMBL1046 AMINOCAPROIC ACID IC50 = 40000.0 nM 4.40
CHEMBL3287843 IC50 = 40000.0 nM 4.40
CHEMBL3287842 IC50 = 100000.0 nM 4.00