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Assay Detail

CHEMBL4767228

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Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P) Modulator Advanced into Clinical Trials.
Gilmore JL,Xiao HY,Dhar TGM,Yang MG,Xiao Z,Xie J,Lehman-McKeeman LD,Gong L,Sun H,Lecureux L,Chen C,Wu DR,Dabros M,Yang X,Taylor TL,Zhou XD,Heimrich EM,Thomas R,McIntyre KW,Borowski V,Warrack BM,Li Y,Shi H,Levesque PC,Yang Z,Marino AM,Cornelius G,D'Arienzo CJ,Mathur A,Rampulla R,Gupta A,Pragalathan B,Shen DR,Cvijic ME,Salter-Cid LM,Carter PH,Dyckman AJ
J Med Chem (2019) 62 : 2265 -2285
PubMed 30785748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.53 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366208 FTY720-P -1.0 1 9.17
CHEMBL4637401 1 8.46
CHEMBL3806205 1 7.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366208 FTY720-P EC50 = 0.67 nM 9.17
CHEMBL4637401 EC50 = 3.5 nM 8.46
CHEMBL3806205 EC50 = 10.7 nM 7.97