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Assay Detail

CHEMBL3373702

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

Binding
Activation of Inward rectifier potassium channel in human atrial myocytes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Buzard DJ, Kim SH, Lopez L, Kawasaki A, Zhu X, Moody J, Thoresen L, Calderon I, Ullman B, Han S, Lehmann J, Gharbaoui T, Sengupta D, Calvano L, Montalban AG, Ma YA, Sage C, Gao Y, Semple G, Edwards J, Barden J, Morgan M, Chen W, Usmani K, Chen C, Sadeque A, Christopher RJ, Thatte J, Fu L, Solomon M, Mills D, Whelan K, Al-Shamma H, Gatlin J, Le M, Gaidarov I, Anthony T, Unett DJ, Blackburn A, Rueter J, Stirn S, Behan DP, Jones RM.
ACS Med Chem Lett (2014) 5 : 1313 -1317
PubMed 25516790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.10 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225155 1 8.68
CHEMBL3358920 ETRASIMOD 4.0 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225155 EC50 = 2.1 nM 8.68
CHEMBL3358920 ETRASIMOD EC50 = 29.9 nM 7.52