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Assay Detail

CHEMBL3380146

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

Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assay
8
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sphingosine 1-phosphate receptor 5 (CHEMBL2274)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.
Buzard DJ, Lopez L, Moody J, Kawasaki A, Schrader TO, Kasem M, Johnson B, Zhu X, Thoresen L, Kim SH, Gharbaoui T, Sengupta D, Calvano L, Krishnan A, Gao Y, Semple G, Edwards J, Barden J, Morgan M, Usmani K, Chen C, Sadeque A, Chen W, Christopher RJ, Thatte J, Fu L, Solomon M, Whelan K, Al-Shamma H, Gatlin J, Gaidarov I, Anthony T, Le M, Unett DJ, Stirn S, Blackburn A, Behan DP, Jones RM.
ACS Med Chem Lett (2014) 5 : 1334 -1339
PubMed 25516794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.75 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3359523 1 7.72
CHEMBL3359522 1 7.33
CHEMBL3358955 2 7.09
CHEMBL3359520 2 6.39
CHEMBL3359519 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3359523 EC50 = 19.0 nM 7.72
CHEMBL3359522 EC50 = 47.0 nM 7.33
CHEMBL3358955 EC50 = 81.0 nM 7.09
CHEMBL3358955 EC50 = 107.0 nM 6.97
CHEMBL3359520 EC50 = 410.0 nM 6.39
CHEMBL3359520 EC50 = 9800.0 nM 5.01
CHEMBL3359519 EC50 > 10000.0 nM -
CHEMBL3359519 EC50 > 10000.0 nM -