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Assay Detail

CHEMBL813568

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

Binding
Binding affinity against human alpha thrombin.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.
Wendt MD, Rockway TW, Geyer A, McClellan W, Weitzberg M, Zhao X, Mantei R, Nienaber VL, Stewart K, Klinghofer V, Giranda VL.
J Med Chem (2004) 47 : 303 -324
PubMed 14711304 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.05 5.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320749 1 5.63
CHEMBL111471 1 5.46
CHEMBL109367 1 5.30
CHEMBL323387 1 5.28
CHEMBL111575 1 5.25
CHEMBL104937 1 5.25
CHEMBL442201 1 5.24
CHEMBL108447 1 5.19
CHEMBL111567 1 5.16
CHEMBL109535 1 5.14
CHEMBL111338 1 4.99
CHEMBL109287 1 4.75
CHEMBL418839 1 4.67
CHEMBL111543 1 4.66
CHEMBL111432 1 4.46
CHEMBL111660 1 4.36
CHEMBL324168 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320749 Ki = 2350.0 nM 5.63
CHEMBL111471 Ki = 3490.0 nM 5.46
CHEMBL109367 Ki = 4990.0 nM 5.30
CHEMBL323387 Ki = 5310.0 nM 5.28
CHEMBL111575 Ki = 5580.0 nM 5.25
CHEMBL104937 Ki = 5640.0 nM 5.25
CHEMBL442201 Ki = 5720.0 nM 5.24
CHEMBL108447 Ki = 6440.0 nM 5.19
CHEMBL111567 Ki = 6920.0 nM 5.16
CHEMBL109535 Ki = 7310.0 nM 5.14
CHEMBL111338 Ki = 10160.0 nM 4.99
CHEMBL109287 Ki = 17600.0 nM 4.75
CHEMBL418839 Ki = 21600.0 nM 4.67
CHEMBL111543 Ki = 21700.0 nM 4.66
CHEMBL111432 Ki = 35100.0 nM 4.46
CHEMBL111660 Ki = 43700.0 nM 4.36
CHEMBL324168 Ki > 100000.0 nM -