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Assay Detail

CHEMBL808464

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

Binding
Inhibitory activity against Tissue 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

Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Nantermet PG, Barrow JC, Newton CL, Pellicore JM, Young M, Lewis SD, Lucas BJ, Krueger JA, McMasters DR, Yan Y, Kuo LC, Vacca JP, Selnick HG.
Bioorg Med Chem Lett (2003) 13 : 2781 -2784
PubMed 12873514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.44 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92615 1 8.52
CHEMBL418965 1 8.22
CHEMBL94952 1 8.22
CHEMBL316901 1 7.70
CHEMBL96354 1 6.82
CHEMBL329266 1 6.44
CHEMBL94864 1 6.32
CHEMBL327421 1 6.19
CHEMBL96599 1 5.50
CHEMBL96801 1 5.41
CHEMBL96376 1 5.37
CHEMBL94622 1 5.25
CHEMBL2204325 1 5.11
CHEMBL93315 1 5.05
CHEMBL329912 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92615 Ki = 3.0 nM 8.52
CHEMBL418965 Ki = 6.0 nM 8.22
CHEMBL94952 Ki = 6.0 nM 8.22
CHEMBL316901 Ki = 20.0 nM 7.70
CHEMBL96354 Ki = 150.0 nM 6.82
CHEMBL329266 Ki = 360.0 nM 6.44
CHEMBL94864 Ki = 480.0 nM 6.32
CHEMBL327421 Ki = 640.0 nM 6.19
CHEMBL96599 Ki = 3200.0 nM 5.50
CHEMBL96801 Ki = 3900.0 nM 5.41
CHEMBL96376 Ki = 4300.0 nM 5.37
CHEMBL94622 Ki = 5600.0 nM 5.25
CHEMBL2204325 Ki = 7700.0 nM 5.11
CHEMBL93315 Ki = 8900.0 nM 5.05
CHEMBL329912 Ki = 165000.0 nM -