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Assay Detail

CHEMBL5346244

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

Binding
Binding affinity to human recombinant full length N-terminal Alexa647-NHS labeled cardiac troponin C expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant incubated for 20 mins by microscale thermophoresis analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Troponin C, slow skeletal and cardiac muscles (CHEMBL2066)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Biophysical Characterization of Fingolimod Derivatives as Cardiac Troponin Antagonists.
Kondacs L, Parijat P, Cobb AJA, Kampourakis T.
ACS Med Chem Lett (2024) 15 : 413 -417
PubMed 38505838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 5.10 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169107 1 5.82
CHEMBL1191567 1 5.72
CHEMBL314854 FINGOLIMOD 4.0 1 5.30
CHEMBL485099 1 5.08
CHEMBL5430893 1 4.59
CHEMBL5429897 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169107 Kd = 1500.0 nM 5.82
CHEMBL1191567 Kd = 1900.0 nM 5.72
CHEMBL314854 FINGOLIMOD Kd = 5000.0 nM 5.30
CHEMBL485099 Kd = 8400.0 nM 5.08
CHEMBL5430893 Kd = 25700.0 nM 4.59
CHEMBL5429897 Kd = 77300.0 nM 4.11