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Assay Detail

CHEMBL817634

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

Binding
Inhibitory activity against human urokinase plasminogen activator expressed as dissociation constant
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Urokinase-type plasminogen activator (CHEMBL3286)
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 25 4.83 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL356007 1 6.39
CHEMBL148317 1 5.85
CHEMBL154985 1 5.80
CHEMBL106079 1 5.70
CHEMBL357079 1 5.47
CHEMBL357067 1 5.35
CHEMBL347493 1 5.03
CHEMBL358441 1 4.80
CHEMBL422147 1 4.60
CHEMBL153412 1 4.58
CHEMBL97597 1 4.51
CHEMBL348443 1 4.47
CHEMBL153732 1 4.46
CHEMBL104241 1 4.42
CHEMBL356216 1 4.40
CHEMBL104970 1 4.39
CHEMBL319868 1 4.32
CHEMBL423770 1 4.31
CHEMBL348266 1 4.26
CHEMBL153334 1 4.25
CHEMBL153565 1 4.11
CHEMBL358387 1 -
CHEMBL346607 1 -
CHEMBL20936 BENZAMIDINE 1 -
CHEMBL346222 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL356007 Ki = 410.0 nM 6.39
CHEMBL148317 Ki = 1400.0 nM 5.85
CHEMBL154985 Ki = 1600.0 nM 5.80
CHEMBL106079 Ki = 2000.0 nM 5.70
CHEMBL357079 Ki = 3400.0 nM 5.47
CHEMBL357067 Ki = 4500.0 nM 5.35
CHEMBL347493 Ki = 9300.0 nM 5.03
CHEMBL358441 Ki = 16000.0 nM 4.80
CHEMBL422147 Ki = 25000.0 nM 4.60
CHEMBL153412 Ki = 26000.0 nM 4.58
CHEMBL97597 Ki = 31000.0 nM 4.51
CHEMBL348443 Ki = 34000.0 nM 4.47
CHEMBL153732 Ki = 35000.0 nM 4.46
CHEMBL104241 Ki = 38000.0 nM 4.42
CHEMBL356216 Ki = 40000.0 nM 4.40
CHEMBL104970 Ki = 41000.0 nM 4.39
CHEMBL319868 Ki = 48000.0 nM 4.32
CHEMBL423770 Ki = 49000.0 nM 4.31
CHEMBL348266 Ki = 55000.0 nM 4.26
CHEMBL153334 Ki = 56000.0 nM 4.25
CHEMBL153565 Ki = 78000.0 nM 4.11
CHEMBL358387 Ki = 800000.0 nM -
CHEMBL346607 Ki > 1000000.0 nM -
CHEMBL20936 BENZAMIDINE Ki = 180000.0 nM -
CHEMBL346222 Ki > 1000000.0 nM -