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Assay Detail

CHEMBL815718

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

Binding
Inhibitory activity against human tissue-type plasminogen activator expressed as dissociation constant
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tissue-type plasminogen activator (CHEMBL1873)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.
Renatus M, Bode W, Huber R, Stürzebecher J, Stubbs MT.
J Med Chem (1998) 41 : 5445 -5456
PubMed 9876114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.31 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL357079 1 7.46
CHEMBL356007 1 6.24
CHEMBL148317 1 6.02
CHEMBL154985 1 6.01
CHEMBL153565 1 4.64
CHEMBL357067 1 4.62
CHEMBL423770 1 4.48
CHEMBL346222 1 4.16
CHEMBL346607 1 4.16
CHEMBL348266 1 -
CHEMBL20936 BENZAMIDINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL357079 Ki = 35.0 nM 7.46
CHEMBL356007 Ki = 570.0 nM 6.24
CHEMBL148317 Ki = 950.0 nM 6.02
CHEMBL154985 Ki = 980.0 nM 6.01
CHEMBL153565 Ki = 23000.0 nM 4.64
CHEMBL357067 Ki = 24000.0 nM 4.62
CHEMBL423770 Ki = 33000.0 nM 4.48
CHEMBL346222 Ki = 69000.0 nM 4.16
CHEMBL346607 Ki = 70000.0 nM 4.16
CHEMBL348266 Ki = 120000.0 nM -
CHEMBL20936 BENZAMIDINE Ki = 910000.0 nM -