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Assay Detail

CHEMBL4426201

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

ADMET
Agonist activity at human S1P3 receptor expressed in HEK293T cell co-expressing G-alpha15-BLA measured after 45 mins by [35S]GTP-gammaS binding assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 3 (CHEMBL3892)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).
Gilmore JL, Sheppeck JE, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ.
J Med Chem (2016) 59 : 6248 -6264
PubMed 27309907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 5.35 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553789 1 6.05
CHEMBL4469843 1 5.96
CHEMBL4457691 1 5.92
CHEMBL4553546 1 5.89
CHEMBL4529165 1 5.75
CHEMBL4587424 1 5.70
CHEMBL4473672 1 5.68
CHEMBL4452807 1 5.68
CHEMBL4569675 1 5.60
CHEMBL4474984 1 5.46
CHEMBL4458762 1 5.42
CHEMBL4541678 1 5.35
CHEMBL4522539 1 5.32
CHEMBL4458575 1 5.28
CHEMBL4574665 1 5.25
CHEMBL4520384 1 5.13
CHEMBL4448752 1 5.03
CHEMBL4474880 1 5.00
CHEMBL4545842 1 4.92
CHEMBL4521128 1 4.92
CHEMBL4461520 1 4.85
CHEMBL4476492 1 4.85
CHEMBL4553920 1 4.69
CHEMBL4473311 1 4.68
CHEMBL4437944 1 -
CHEMBL4464631 1 -
CHEMBL4440968 1 -
CHEMBL4475594 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4553789 EC50 = 900.0 nM 6.05
CHEMBL4469843 EC50 = 1100.0 nM 5.96
CHEMBL4457691 EC50 = 1200.0 nM 5.92
CHEMBL4553546 EC50 = 1300.0 nM 5.89
CHEMBL4529165 EC50 = 1800.0 nM 5.75
CHEMBL4587424 EC50 = 2000.0 nM 5.70
CHEMBL4473672 EC50 = 2100.0 nM 5.68
CHEMBL4452807 EC50 = 2100.0 nM 5.68
CHEMBL4569675 EC50 = 2500.0 nM 5.60
CHEMBL4474984 EC50 = 3500.0 nM 5.46
CHEMBL4458762 EC50 = 3800.0 nM 5.42
CHEMBL4541678 EC50 = 4500.0 nM 5.35
CHEMBL4522539 EC50 = 4800.0 nM 5.32
CHEMBL4458575 EC50 = 5300.0 nM 5.28
CHEMBL4574665 EC50 = 5600.0 nM 5.25
CHEMBL4520384 EC50 = 7400.0 nM 5.13
CHEMBL4448752 EC50 = 9400.0 nM 5.03
CHEMBL4474880 EC50 = 10000.0 nM 5.00
CHEMBL4545842 EC50 = 12000.0 nM 4.92
CHEMBL4521128 EC50 = 12000.0 nM 4.92
CHEMBL4461520 EC50 = 14000.0 nM 4.85
CHEMBL4476492 EC50 = 14000.0 nM 4.85
CHEMBL4553920 EC50 = 20300.0 nM 4.69
CHEMBL4473311 EC50 = 21000.0 nM 4.68
CHEMBL4437944 EC50 > 31000.0 nM -
CHEMBL4464631 EC50 > 31300.0 nM -
CHEMBL4440968 EC50 - -
CHEMBL4475594 EC50 - -