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Assay Detail

CHEMBL815712

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Binding
Binding affinity towards tissue type plasminogen activator
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Wendt MD, Geyer A, McClellan WJ, Rockway TW, Weitzberg M, Zhao X, Mantei R, Stewart K, Nienaber V, Klinghofer V, Giranda VL.
Bioorg Med Chem Lett (2004) 14 : 3063 -3068
PubMed 15149645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.53 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421214 1 6.89
CHEMBL319047 1 6.75
CHEMBL104166 1 6.17
CHEMBL104505 1 6.09
CHEMBL105395 1 6.06
CHEMBL320233 1 5.80
CHEMBL104211 1 5.48
CHEMBL320817 1 5.13
CHEMBL321319 1 5.08
CHEMBL104904 1 4.75
CHEMBL103043 1 4.62
CHEMBL319264 1 4.57
CHEMBL104937 1 4.50
CHEMBL105171 1 -
CHEMBL321944 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421214 Ki = 130.0 nM 6.89
CHEMBL319047 Ki = 180.0 nM 6.75
CHEMBL104166 Ki = 680.0 nM 6.17
CHEMBL104505 Ki = 810.0 nM 6.09
CHEMBL105395 Ki = 870.0 nM 6.06
CHEMBL320233 Ki = 1600.0 nM 5.80
CHEMBL104211 Ki = 3300.0 nM 5.48
CHEMBL320817 Ki = 7400.0 nM 5.13
CHEMBL321319 Ki = 8300.0 nM 5.08
CHEMBL104904 Ki = 18000.0 nM 4.75
CHEMBL103043 Ki = 24000.0 nM 4.62
CHEMBL319264 Ki = 27000.0 nM 4.57
CHEMBL104937 Ki = 32000.0 nM 4.50
CHEMBL105171 Ki > 100000.0 nM -
CHEMBL321944 Ki > 100000.0 nM -