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Assay Detail

CHEMBL833010

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

Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 2 expressed on CHO cell membranes
22
Total Activities
19
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 Expert

Target

Sphingosine 1-phosphate receptor 2 (CHEMBL2955)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Yan L, Hale JJ, Lynch CL, Budhu R, Gentry A, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Rosen H, Mandala SM.
Bioorg Med Chem Lett (2004) 14 : 4861 -4866
PubMed 15341940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.23 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL187692 2 6.60
CHEMBL118860 1 6.50
CHEMBL187588 1 6.48
CHEMBL184879 2 6.38
CHEMBL334213 1 6.24
CHEMBL1161691 1 5.96
CHEMBL185100 1 5.66
CHEMBL363008 1 -
CHEMBL184237 1 -
CHEMBL187645 1 -
CHEMBL359762 1 -
CHEMBL184591 1 -
CHEMBL186921 2 -
CHEMBL181597 1 -
CHEMBL184349 1 -
CHEMBL183688 1 -
CHEMBL185066 1 -
CHEMBL185447 1 -
CHEMBL187061 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL187692 IC50 = 250.0 nM 6.60
CHEMBL118860 IC50 = 320.0 nM 6.50
CHEMBL187588 IC50 = 330.0 nM 6.48
CHEMBL184879 IC50 = 422.0 nM 6.38
CHEMBL334213 IC50 = 580.0 nM 6.24
CHEMBL187692 IC50 = 760.0 nM 6.12
CHEMBL184879 IC50 = 750.0 nM 6.12
CHEMBL1161691 IC50 = 1100.0 nM 5.96
CHEMBL185100 IC50 = 2200.0 nM 5.66
CHEMBL363008 IC50 > 1000.0 nM -
CHEMBL184237 IC50 > 1000.0 nM -
CHEMBL187645 IC50 > 1000.0 nM -
CHEMBL359762 IC50 > 1000.0 nM -
CHEMBL184591 IC50 > 1000.0 nM -
CHEMBL186921 IC50 > 1000.0 nM -
CHEMBL186921 IC50 > 1000.0 nM -
CHEMBL181597 IC50 > 1000.0 nM -
CHEMBL184349 IC50 > 1000.0 nM -
CHEMBL183688 IC50 > 1000.0 nM -
CHEMBL185066 IC50 > 1000.0 nM -
CHEMBL185447 IC50 > 1000.0 nM -
CHEMBL187061 IC50 > 1000.0 nM -