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Assay Detail

CHEMBL4736708

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Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Bicyclic Ligand-Biased Agonists of S1P: Exploring Side Chain Modifications to Modulate the PK, PD, and Safety Profiles.
Gilmore JL,Xiao HY,Dhar TGM,Yang M,Xiao Z,Yang X,Taylor TL,McIntyre KW,Warrack BM,Shi H,Levesque PC,Marino AM,Cornelius G,Mathur A,Shen DR,Pang J,Cvijic ME,Lehman-McKeeman LD,Sun H,Xie J,Salter-Cid L,Carter PH,Dyckman AJ
J Med Chem (2021) 64 : 1454 -1480
PubMed 33492963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.47 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114606 1 9.17
CHEMBL4752394 1 8.44
CHEMBL4786296 1 8.31
CHEMBL3806205 1 7.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114606 EC50 = 0.67 nM 9.17
CHEMBL4752394 EC50 = 3.6 nM 8.44
CHEMBL4786296 EC50 = 4.9 nM 8.31
CHEMBL3806205 EC50 = 10.7 nM 7.97