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Assay Detail

CHEMBL3768085

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

Binding
Displacement of TAMRA-TRTK12 from recombinant rat calcium loaded S100-B by fluorescence polarization competition assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein S100-B (CHEMBL3763006)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Small Molecule Inhibitors of Ca(2+)-S100B Reveal Two Protein Conformations.
Cavalier MC, Ansari MI, Pierce AD, Wilder PT, McKnight LE, Raman EP, Neau DB, Bezawada P, Alasady MJ, Charpentier TH, Varney KM, Toth EA, MacKerell AD, Coop A, Weber DJ.
J Med Chem (2016) 59 : 592 -608
PubMed 26727270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.60 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764851 1 5.17
CHEMBL3764285 1 4.74
CHEMBL3765382 1 4.29
CHEMBL289577 1 4.18
CHEMBL3765054 1 -
CHEMBL3765771 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764851 IC50 = 6700.0 nM 5.17
CHEMBL3764285 IC50 = 18300.0 nM 4.74
CHEMBL3765382 IC50 = 51100.0 nM 4.29
CHEMBL289577 IC50 = 66600.0 nM 4.18
CHEMBL3765054 IC50 = 981700.0 nM -
CHEMBL3765771 IC50 = 2222100.0 nM -