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Assay Detail

CHEMBL4719884

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

Binding
Agonist activity at human S1P1 in HLE cell membranes incubated for 45 mins by scintillation counting based [35S]GTP-gamma-S binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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

Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P Receptor Modulator.
Yang MG,Xiao Z,Dhar TG,Xiao HY,Gilmore JL,Marcoux D,Xie JH,McIntyre KW,Taylor TL,Borowski V,Heimrich E,Li YW,Feng J,Fernandes A,Yang Z,Balimane P,Marino AM,Cornelius G,Warrack BM,Mathur A,Wu DR,Li P,Gupta A,Pragalathan B,Shen DR,Cvijic ME,Lehman-McKeeman LD,Salter-Cid L,Barrish JC,Carter PH,Dyckman AJ
J Med Chem (2016) 59 : 11138 -11147
PubMed 28002964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.71 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3806205 1 8.19
CHEMBL4762613 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3806205 EC50 = 6.4 nM 8.19
CHEMBL4762613 EC50 = 60.0 nM 7.22