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Assay Detail

CHEMBL3089538

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

Binding
Agonist activity at human S1P3 receptor expressed in CHO cells after 4 hrs by fluorescence assay
28
Total Activities
28
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 3 (CHEMBL3892)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.
Guerrero M, Poddutoori R, Urbano M, Peng X, Spicer TP, Chase PS, Hodder PS, Schaeffer MT, Brown S, Rosen H, Roberts E.
Bioorg Med Chem Lett (2013) 23 : 6346 -6349
PubMed 24135724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 5.91 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1973788 1 6.99
CHEMBL1970071 1 6.98
CHEMBL1969371 1 6.70
CHEMBL1984536 1 6.49
CHEMBL3088204 1 6.47
CHEMBL2004782 1 6.47
CHEMBL1455786 1 6.36
CHEMBL1965004 1 6.27
CHEMBL3088203 1 6.25
CHEMBL1968913 1 6.02
CHEMBL1999116 1 5.86
CHEMBL1972130 1 5.77
CHEMBL1995815 1 5.76
CHEMBL1976353 1 5.56
CHEMBL1979798 1 5.55
CHEMBL1975200 1 5.46
CHEMBL1967913 1 5.45
CHEMBL1369793 1 5.18
CHEMBL3088201 1 5.18
CHEMBL3087666 1 5.16
CHEMBL1975908 1 5.10
CHEMBL3088205 1 5.09
CHEMBL1989169 1 -
CHEMBL1979472 1 -
CHEMBL1976643 1 -
CHEMBL3088202 1 -
CHEMBL1478485 1 -
CHEMBL1392307 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1973788 EC50 = 103.0 nM 6.99
CHEMBL1970071 EC50 = 105.0 nM 6.98
CHEMBL1969371 EC50 = 202.0 nM 6.70
CHEMBL1984536 EC50 = 323.0 nM 6.49
CHEMBL3088204 EC50 = 339.0 nM 6.47
CHEMBL2004782 EC50 = 337.0 nM 6.47
CHEMBL1455786 EC50 = 434.0 nM 6.36
CHEMBL1965004 EC50 = 535.0 nM 6.27
CHEMBL3088203 EC50 = 559.0 nM 6.25
CHEMBL1968913 EC50 = 959.0 nM 6.02
CHEMBL1999116 EC50 = 1375.0 nM 5.86
CHEMBL1972130 EC50 = 1683.0 nM 5.77
CHEMBL1995815 EC50 = 1740.0 nM 5.76
CHEMBL1976353 EC50 = 2753.0 nM 5.56
CHEMBL1979798 EC50 = 2820.0 nM 5.55
CHEMBL1975200 EC50 = 3430.0 nM 5.46
CHEMBL1967913 EC50 = 3536.0 nM 5.45
CHEMBL1369793 EC50 = 6595.0 nM 5.18
CHEMBL3088201 EC50 = 6563.0 nM 5.18
CHEMBL3087666 EC50 = 7000.0 nM 5.16
CHEMBL1975908 EC50 = 7985.0 nM 5.10
CHEMBL3088205 EC50 = 8070.0 nM 5.09
CHEMBL1989169 EC50 > 50000.0 nM -
CHEMBL1979472 EC50 > 50000.0 nM -
CHEMBL1976643 EC50 > 50000.0 nM -
CHEMBL3088202 EC50 > 50000.0 nM -
CHEMBL1478485 EC50 > 50000.0 nM -
CHEMBL1392307 EC50 > 50000.0 nM -