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Assay Detail

CHEMBL4736698

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

Binding
Displacement of [33P]-SIP from human recombinant S1P1 expressed in CHO cell membranes measured after 45 mins by TopCount scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333)
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
IC50 4 10.73 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3806205 1 11.00
CHEMBL4752394 1 10.80
CHEMBL4786296 1 10.40
CHEMBL114606 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3806205 IC50 = 0.01 nM 11.00
CHEMBL4752394 IC50 = 0.016 nM 10.80
CHEMBL4786296 IC50 = 0.04 nM 10.40
CHEMBL114606 IC50 = 0.008 nM -