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Assay Detail

CHEMBL1920392

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Functional
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P₁ agonists.
Buzard D, Han S, Thoresen L, Moody J, Lopez L, Kawasaki A, Schrader T, Sage C, Gao Y, Edwards J, Barden J, Thatte J, Fu L, Solomon M, Liu L, Al-Shamma H, Gatlin J, Le M, Xing C, Espinola S, Jones RM.
Bioorg Med Chem Lett (2011) 21 : 6013 -6018
PubMed 21852130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 39 8.01 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1916564 1 9.09
CHEMBL1916570 1 9.00
CHEMBL1916409 1 9.00
CHEMBL1916569 1 8.96
CHEMBL1916399 1 8.92
CHEMBL1916558 1 8.92
CHEMBL1916565 1 8.89
CHEMBL1916568 1 8.82
CHEMBL1916563 1 8.79
CHEMBL1916572 1 8.57
CHEMBL1916571 1 8.40
CHEMBL1916405 1 8.38
CHEMBL1916553 1 8.37
CHEMBL1916559 1 8.34
CHEMBL1916404 1 8.31
CHEMBL1916573 1 8.28
CHEMBL1916560 1 8.21
CHEMBL1916574 1 8.20
CHEMBL1916561 1 8.18
CHEMBL1916402 1 8.14
CHEMBL1916403 1 8.01
CHEMBL1916580 1 7.99
CHEMBL1916577 1 7.96
CHEMBL1916575 1 7.96
CHEMBL1916576 1 7.75
CHEMBL1916566 1 7.75
CHEMBL1916410 1 7.62
CHEMBL1916554 1 7.43
CHEMBL1916578 1 7.42
CHEMBL1916557 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1916564 EC50 = 0.82 nM 9.09
CHEMBL1916570 EC50 = 1.0 nM 9.00
CHEMBL1916409 EC50 = 1.0 nM 9.00
CHEMBL1916569 EC50 = 1.1 nM 8.96
CHEMBL1916399 EC50 = 1.2 nM 8.92
CHEMBL1916558 EC50 = 1.2 nM 8.92
CHEMBL1916565 EC50 = 1.3 nM 8.89
CHEMBL1916568 EC50 = 1.5 nM 8.82
CHEMBL1916563 EC50 = 1.63 nM 8.79
CHEMBL1916572 EC50 = 2.7 nM 8.57
CHEMBL1916571 EC50 = 4.0 nM 8.40
CHEMBL1916405 EC50 = 4.2 nM 8.38
CHEMBL1916553 EC50 = 4.3 nM 8.37
CHEMBL1916559 EC50 = 4.6 nM 8.34
CHEMBL1916404 EC50 = 4.9 nM 8.31
CHEMBL1916573 EC50 = 5.3 nM 8.28
CHEMBL1916560 EC50 = 6.1 nM 8.21
CHEMBL1916574 EC50 = 6.3 nM 8.20
CHEMBL1916561 EC50 = 6.6 nM 8.18
CHEMBL1916402 EC50 = 7.2 nM 8.14
CHEMBL1916403 EC50 = 9.8 nM 8.01
CHEMBL1916580 EC50 = 10.3 nM 7.99
CHEMBL1916577 EC50 = 11.0 nM 7.96
CHEMBL1916575 EC50 = 11.0 nM 7.96
CHEMBL1916576 EC50 = 18.0 nM 7.75
CHEMBL1916566 EC50 = 18.0 nM 7.75
CHEMBL1916410 EC50 = 24.0 nM 7.62
CHEMBL1916554 EC50 = 37.0 nM 7.43
CHEMBL1916578 EC50 = 38.0 nM 7.42
CHEMBL1916557 EC50 = 41.0 nM 7.39
CHEMBL1916567 EC50 = 45.0 nM 7.35
CHEMBL1916555 EC50 = 54.0 nM 7.27
CHEMBL1916579 EC50 = 68.0 nM 7.17
CHEMBL1916411 EC50 = 75.0 nM 7.12
CHEMBL1916562 EC50 = 102.0 nM 6.99
CHEMBL1916407 EC50 = 297.0 nM 6.53
CHEMBL1916556 EC50 = 369.0 nM 6.43
CHEMBL1916408 EC50 = 406.0 nM 6.39
CHEMBL1916406 EC50 > 100.0 nM -