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Assay Detail

CHEMBL866005

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

Binding
Antagonist like activity at skeletal junction sarcoplasmic reticulum RyR1/FKBP12 complex assessed as decrease in [3H]ryanodine binding
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Simplified cyclic analogues of bastadin-5. Structure-activity relationships for modulation of the RyR1/FKBP12 Ca2+ channel complex.
Masuno MN, Pessah IN, Olmstead MM, Molinski TF.
J Med Chem (2006) 49 : 4497 -4511
PubMed 16854055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.58 5.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL213853 1 5.21
CHEMBL209335 1 4.33
CHEMBL379795 1 4.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL213853 IC50 = 6200.0 nM 5.21
CHEMBL209335 IC50 = 47000.0 nM 4.33
CHEMBL379795 IC50 = 63000.0 nM 4.20