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Assay Detail

CHEMBL4681122

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Binding
Agonist activity at human S1P3 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
ChEMBL ↗
37
Total Activities
34
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 3 (CHEMBL3892) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P) Employing Ligand-Based Drug Design.
Xiao HY,Watterson SH,Langevine CM,Srivastava AS,Ko SS,Zhang Y,Cherney RJ,Guo WW,Gilmore JL,Sheppeck JE,Wu DR,Li P,Ramasamy D,Arunachalam P,Mathur A,Taylor TL,Shuster DJ,McIntyre KW,Shen DR,Yarde M,Cvijic ME,Marino AM,Balimane PV,Yang Z,Banas DM,Cornelius G,D'Arienzo CJ,Warrack BM,Lehman-McKeeman L,Salter-Cid LM,Xie J,Barrish JC,Carter PH,Dyckman AJ,Dhar TG
J Med Chem (2016) 59 : 9837 -9854
PubMed 27726358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 5.32 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4760972 — — 1 6.04
CHEMBL4758827 — — 1 5.92
CHEMBL4757149 — — 1 5.92
CHEMBL4776597 — — 1 5.89
CHEMBL4757437 — — 1 5.89
CHEMBL4784344 — — 1 5.85
CHEMBL4798447 — — 1 5.80
CHEMBL3794064 — — 1 5.80
CHEMBL4792990 — — 2 5.77
CHEMBL3930827 — — 1 5.72
CHEMBL4750972 — — 1 5.68
CHEMBL3942289 — — 1 5.55
CHEMBL4747682 — — 1 5.36
CHEMBL3959509 — — 1 5.36
CHEMBL4782854 — — 1 5.34
CHEMBL4758481 — — 2 5.21
CHEMBL4784466 — — 1 4.96
CHEMBL4795734 — — 1 4.92
CHEMBL4755286 — — 1 4.92
CHEMBL4761456 — — 2 4.89
CHEMBL4793933 — — 1 4.85
CHEMBL4764300 — — 1 4.82
CHEMBL4759408 — — 1 4.64
CHEMBL3970572 — — 1 4.58
CHEMBL4797042 — — 1 4.50
CHEMBL3908750 — — 1 -
CHEMBL4763970 — — 1 -
CHEMBL3964923 — — 1 -
CHEMBL4741076 — — 1 -
CHEMBL4785652 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4760972 — EC50 = 920.0 nM 6.04
CHEMBL4758827 — EC50 = 1200.0 nM 5.92
CHEMBL4757149 — EC50 = 1200.0 nM 5.92
CHEMBL4776597 — EC50 = 1300.0 nM 5.89
CHEMBL4757437 — EC50 = 1300.0 nM 5.89
CHEMBL4784344 — EC50 = 1400.0 nM 5.85
CHEMBL3794064 — EC50 = 1600.0 nM 5.80
CHEMBL4798447 — EC50 = 1600.0 nM 5.80
CHEMBL4792990 — EC50 = 1700.0 nM 5.77
CHEMBL3930827 — EC50 = 1900.0 nM 5.72
CHEMBL4750972 — EC50 = 2100.0 nM 5.68
CHEMBL3942289 — EC50 = 2800.0 nM 5.55
CHEMBL3959509 — EC50 = 4400.0 nM 5.36
CHEMBL4747682 — EC50 = 4400.0 nM 5.36
CHEMBL4782854 — EC50 = 4600.0 nM 5.34
CHEMBL4758481 — EC50 = 6200.0 nM 5.21
CHEMBL4792990 — EC50 = 7400.0 nM 5.13
CHEMBL4784466 — EC50 = 11000.0 nM 4.96
CHEMBL4795734 — EC50 = 12000.0 nM 4.92
CHEMBL4755286 — EC50 = 12000.0 nM 4.92
CHEMBL4761456 — EC50 = 13000.0 nM 4.89
CHEMBL4793933 — EC50 = 14000.0 nM 4.85
CHEMBL4764300 — EC50 = 15000.0 nM 4.82
CHEMBL4761456 — EC50 = 16000.0 nM 4.80
CHEMBL4758481 — EC50 = 18000.0 nM 4.75
CHEMBL4759408 — EC50 = 23000.0 nM 4.64
CHEMBL3970572 — EC50 = 26000.0 nM 4.58
CHEMBL4797042 — EC50 = 32000.0 nM 4.50
CHEMBL3954922 — EC50 > 3100.0 nM -
CHEMBL4744056 — EC50 > 63000.0 nM -
CHEMBL3964377 — EC50 > 63000.0 nM -
CHEMBL3908750 — EC50 > 31000.0 nM -
CHEMBL4763970 — EC50 > 63000.0 nM -
CHEMBL4799712 — EC50 > 63000.0 nM -
CHEMBL3964923 — EC50 > 63000.0 nM -
CHEMBL4741076 — EC50 > 63000.0 nM -
CHEMBL4785652 — EC50 > 63000.0 nM -