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Assay Detail

CHEMBL1953077

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

Functional
Agonist activity at human S1P3 receptor assessed as stimulation of [35S]GTPgamma binding
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.
Nakamura T, Asano M, Sekiguchi Y, Mizuno Y, Tamaki K, Kimura T, Nara F, Kawase Y, Shimozato T, Doi H, Kagari T, Tomisato W, Inoue R, Nagasaki M, Yuita H, Oguchi-Oshima K, Kaneko R, Watanabe N, Abe Y, Nishi T.
Bioorg Med Chem Lett (2012) 22 : 1788 -1792
PubMed 22264485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 5.32 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1951147 1 6.10
CHEMBL1951154 1 6.05
CHEMBL225575 1 5.80
CHEMBL1951157 1 5.70
CHEMBL1951158 1 5.52
CHEMBL1951312 1 5.35
CHEMBL1951152 1 5.34
CHEMBL1951319 1 5.22
CHEMBL1951313 1 5.00
CHEMBL1951315 1 4.96
CHEMBL1951155 1 4.92
CHEMBL1951305 1 4.89
CHEMBL1951306 1 4.82
CHEMBL1951311 1 4.82
CHEMBL1951150 1 -
CHEMBL1951159 1 -
CHEMBL1951303 1 -
CHEMBL1951304 1 -
CHEMBL1951307 1 -
CHEMBL1951308 1 -
CHEMBL1951309 1 -
CHEMBL1951310 1 -
CHEMBL1951149 1 -
CHEMBL1951314 1 -
CHEMBL1949690 1 -
CHEMBL1951316 1 -
CHEMBL1951317 1 -
CHEMBL1951318 1 -
CHEMBL1951153 1 -
CHEMBL1951148 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1951147 EC50 = 800.0 nM 6.10
CHEMBL1951154 EC50 = 900.0 nM 6.05
CHEMBL225575 EC50 = 1600.0 nM 5.80
CHEMBL1951157 EC50 = 2000.0 nM 5.70
CHEMBL1951158 EC50 = 3000.0 nM 5.52
CHEMBL1951312 EC50 = 4500.0 nM 5.35
CHEMBL1951152 EC50 = 4600.0 nM 5.34
CHEMBL1951319 EC50 = 6000.0 nM 5.22
CHEMBL1951313 EC50 = 10000.0 nM 5.00
CHEMBL1951315 EC50 = 11000.0 nM 4.96
CHEMBL1951155 EC50 = 12000.0 nM 4.92
CHEMBL1951305 EC50 = 13000.0 nM 4.89
CHEMBL1951306 EC50 = 15000.0 nM 4.82
CHEMBL1951311 EC50 = 15000.0 nM 4.82
CHEMBL1951156 EC50 > 20000.0 nM -
CHEMBL1951151 EC50 > 20000.0 nM -
CHEMBL1951150 EC50 > 20000.0 nM -
CHEMBL1951159 EC50 > 20000.0 nM -
CHEMBL1951303 EC50 > 20000.0 nM -
CHEMBL1951304 EC50 > 20000.0 nM -
CHEMBL1951307 EC50 > 20000.0 nM -
CHEMBL1951308 EC50 > 20000.0 nM -
CHEMBL1951309 EC50 > 20000.0 nM -
CHEMBL1951310 EC50 > 20000.0 nM -
CHEMBL1951149 EC50 > 20000.0 nM -
CHEMBL1951314 EC50 > 20000.0 nM -
CHEMBL1949690 EC50 > 20000.0 nM -
CHEMBL1951316 EC50 > 20000.0 nM -
CHEMBL1951317 EC50 > 20000.0 nM -
CHEMBL1951318 EC50 > 20000.0 nM -
CHEMBL1951153 EC50 > 20000.0 nM -
CHEMBL1951148 EC50 > 20000.0 nM -