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Assay Detail

CHEMBL1006192

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Binding
Binding affinity to RYR1 channels by calcium mobilization assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Ryanodine receptor 1 (CHEMBL1846)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Open-chain half-bastadins mimic the effects of cyclic bastadins on calcium homeostasis in cultured neurons.
Zieminska E, Lazarewicz JW, Couladouros EA, Moutsos VI, Pitsinos EN.
Bioorg Med Chem Lett (2008) 18 : 5734 -5734
PubMed 18851910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.27 5.66
IC50 1 5.22 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439151 BASTADIN 5 1 5.66
CHEMBL213853 1 5.22
CHEMBL360190 BASTADIN 7 1 5.20
CHEMBL386905 1 4.96
CHEMBL506286 BASTADIN 19 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439151 BASTADIN 5 EC50 = 2200.0 nM 5.66
CHEMBL213853 IC50 = 6000.0 nM 5.22
CHEMBL360190 BASTADIN 7 EC50 = 6300.0 nM 5.20
CHEMBL386905 EC50 = 11000.0 nM 4.96
CHEMBL506286 BASTADIN 19 EC50 > 100000.0 nM -