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Assay Detail

CHEMBL917015

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

Binding
Inhibition of human tPA
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines.
Fish PV, Barber CG, Brown DG, Butt R, Collis MG, Dickinson RP, Henry BT, Horne VA, Huggins JP, King E, O'Gara M, McCleverty D, McIntosh F, Phillips C, Webster R.
J Med Chem (2007) 50 : 2341 -2351
PubMed 17447747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 4.54 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL227781 1 4.82
CHEMBL228173 1 4.64
CHEMBL227607 1 4.64
CHEMBL227583 1 4.62
CHEMBL226714 1 4.46
CHEMBL228113 1 4.46
CHEMBL227422 1 4.42
CHEMBL374378 1 4.42
CHEMBL227421 1 4.40
CHEMBL228051 1 -
CHEMBL227890 1 -
CHEMBL223864 1 -
CHEMBL227426 1 -
CHEMBL227606 1 -
CHEMBL376763 1 -
CHEMBL227931 1 -
CHEMBL227782 1 -
CHEMBL388780 1 -
CHEMBL228238 1 -
CHEMBL389032 1 -
CHEMBL390133 1 -
CHEMBL228204 1 -
CHEMBL228052 1 -
CHEMBL427456 1 -
CHEMBL227769 1 -
CHEMBL390310 1 -
CHEMBL227940 1 -
CHEMBL374623 1 -
CHEMBL227770 1 -
CHEMBL224689 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL227781 Ki = 15000.0 nM 4.82
CHEMBL228173 Ki = 23000.0 nM 4.64
CHEMBL227607 Ki = 23000.0 nM 4.64
CHEMBL227583 Ki = 24000.0 nM 4.62
CHEMBL226714 Ki = 34700.0 nM 4.46
CHEMBL228113 Ki = 34400.0 nM 4.46
CHEMBL227422 Ki = 38000.0 nM 4.42
CHEMBL374378 Ki = 38000.0 nM 4.42
CHEMBL227421 Ki = 40000.0 nM 4.40
CHEMBL227931 Ki = 108000.0 nM -
CHEMBL227584 Ki > 100000.0 nM -
CHEMBL227782 Ki > 100000.0 nM -
CHEMBL388780 Ki > 100000.0 nM -
CHEMBL228238 Ki > 100000.0 nM -
CHEMBL227990 Ki > 100000.0 nM -
CHEMBL227666 Ki > 100000.0 nM -
CHEMBL227976 Ki > 100000.0 nM -
CHEMBL228170 Ki > 100000.0 nM -
CHEMBL226716 Ki > 30000.0 nM -
CHEMBL266435 Ki > 100000.0 nM -
CHEMBL389056 Ki > 100000.0 nM -
CHEMBL227425 Ki > 100000.0 nM -
CHEMBL227995 Ki > 100000.0 nM -
CHEMBL228172 Ki > 100000.0 nM -
CHEMBL227664 Ki > 100000.0 nM -
CHEMBL228204 Ki - -
CHEMBL224689 Ki > 100000.0 nM -
CHEMBL227770 Ki - -
CHEMBL374623 Ki > 100000.0 nM -
CHEMBL227940 Ki > 30000.0 nM -
CHEMBL390310 Ki > 30000.0 nM -
CHEMBL227769 Ki - -
CHEMBL427456 Ki - -
CHEMBL228052 Ki - -
CHEMBL376763 Ki > 100000.0 nM -
CHEMBL390133 Ki - -
CHEMBL389032 Ki - -
CHEMBL228051 Ki - -
CHEMBL227890 Ki - -
CHEMBL223864 Ki - -
CHEMBL227426 Ki - -
CHEMBL227606 Ki - -