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Assay Detail

CHEMBL703580

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

Binding
Binding affinity against human plasma kallikrein.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasma kallikrein (CHEMBL2000)
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 18 5.77 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111567 1 6.95
CHEMBL108447 1 6.84
CHEMBL442201 1 6.64
CHEMBL111338 1 6.40
CHEMBL109367 1 6.36
CHEMBL323387 1 6.07
CHEMBL109535 1 5.87
CHEMBL111471 1 5.86
CHEMBL320749 1 5.61
CHEMBL104937 1 5.60
CHEMBL111432 1 5.59
CHEMBL111575 1 5.57
CHEMBL418839 1 5.48
CHEMBL111543 1 5.37
CHEMBL324168 1 5.14
CHEMBL109287 1 5.10
CHEMBL111660 1 4.74
CHEMBL105171 1 4.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111567 Ki = 112.0 nM 6.95
CHEMBL108447 Ki = 145.0 nM 6.84
CHEMBL442201 Ki = 230.0 nM 6.64
CHEMBL111338 Ki = 400.0 nM 6.40
CHEMBL109367 Ki = 436.0 nM 6.36
CHEMBL323387 Ki = 849.0 nM 6.07
CHEMBL109535 Ki = 1350.0 nM 5.87
CHEMBL111471 Ki = 1370.0 nM 5.86
CHEMBL320749 Ki = 2430.0 nM 5.61
CHEMBL104937 Ki = 2500.0 nM 5.60
CHEMBL111432 Ki = 2570.0 nM 5.59
CHEMBL111575 Ki = 2720.0 nM 5.57
CHEMBL418839 Ki = 3330.0 nM 5.48
CHEMBL111543 Ki = 4300.0 nM 5.37
CHEMBL324168 Ki = 7170.0 nM 5.14
CHEMBL109287 Ki = 8000.0 nM 5.10
CHEMBL111660 Ki = 18100.0 nM 4.74
CHEMBL105171 Ki = 22500.0 nM 4.65