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Assay Detail

CHEMBL3807065

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

Binding
Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
Dhar TG, Xiao HY, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Warrack B, Shi H, Levesque PC, Zhu JL, Hennan J, Balimane P, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.
ACS Med Chem Lett (2016) 7 : 283 -288
PubMed 26985316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 10.05 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114606 1 10.15
CHEMBL3806205 1 9.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114606 EC50 = 0.07 nM 10.15
CHEMBL3806205 EC50 = 0.114 nM 9.94