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Assay Detail

CHEMBL3380330

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Functional
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
ChEMBL ↗
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 19 8.76 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3358920 ETRASIMOD 4.0 1 10.40
CHEMBL225155 — — 1 10.21
CHEMBL3358912 — — 1 10.14
CHEMBL3358911 — — 1 10.11
CHEMBL3358910 — — 1 10.06
CHEMBL3358919 — — 1 10.05
CHEMBL3358917 — — 1 9.36
CHEMBL3358913 — — 1 9.35
CHEMBL3358915 — — 1 9.31
CHEMBL3358906 — — 1 8.77
CHEMBL3358914 — — 1 8.43
CHEMBL3358918 — — 1 8.34
CHEMBL3358904 — — 1 7.80
CHEMBL3358905 — — 1 7.58
CHEMBL3358916 — — 1 7.25
CHEMBL3358907 — — 1 6.92
CHEMBL3358908 — — 1 6.85
CHEMBL3358909 — — 1 6.80
CHEMBL366208 FTY720-P -1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3358920 ETRASIMOD EC50 = 0.04 nM 10.40
CHEMBL225155 — EC50 = 0.062 nM 10.21
CHEMBL3358912 — EC50 = 0.073 nM 10.14
CHEMBL3358911 — EC50 = 0.077 nM 10.11
CHEMBL3358910 — EC50 = 0.087 nM 10.06
CHEMBL3358919 — EC50 = 0.09 nM 10.05
CHEMBL3358917 — EC50 = 0.44 nM 9.36
CHEMBL3358913 — EC50 = 0.45 nM 9.35
CHEMBL3358915 — EC50 = 0.49 nM 9.31
CHEMBL3358906 — EC50 = 1.7 nM 8.77
CHEMBL3358914 — EC50 = 3.68 nM 8.43
CHEMBL3358918 — EC50 = 4.58 nM 8.34
CHEMBL3358904 — EC50 = 16.0 nM 7.80
CHEMBL3358905 — EC50 = 26.0 nM 7.58
CHEMBL3358916 — EC50 = 55.8 nM 7.25
CHEMBL3358907 — EC50 = 120.0 nM 6.92
CHEMBL3358908 — EC50 = 141.0 nM 6.85
CHEMBL3358909 — EC50 = 159.0 nM 6.80
CHEMBL366208 FTY720-P EC50 = 0.006 nM -