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Assay Detail

CHEMBL3380163

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Functional
Agonist activity at monkey S1P1 receptor assessed as cAMP accumulation by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Macaca mulatta
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL3559675)
Type SINGLE PROTEIN
Organism Macaca mulatta

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 2 10.33 10.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3359522 1 10.42
CHEMBL3359523 1 10.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3359522 EC50 = 0.038 nM 10.42
CHEMBL3359523 EC50 = 0.058 nM 10.24