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Assay Detail

CHEMBL3801746

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Functional
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.
J Med Chem (2016) 59 : 2820 -2840
PubMed 26924461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 8.87 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3799701 1 9.57
CHEMBL3797951 1 9.52
CHEMBL3800091 1 9.41
CHEMBL3799693 1 9.36
CHEMBL3800257 1 9.36
CHEMBL3794064 1 9.33
CHEMBL3798735 1 9.27
CHEMBL3797415 1 9.25
CHEMBL3800349 1 9.01
CHEMBL3798784 1 9.00
CHEMBL3800513 1 8.89
CHEMBL3800595 1 8.80
CHEMBL3799276 1 8.77
CHEMBL3798775 1 8.49
CHEMBL3800122 1 8.30
CHEMBL3798531 1 8.28
CHEMBL3798560 1 7.60
CHEMBL3799501 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3799701 EC50 = 0.27 nM 9.57
CHEMBL3797951 EC50 = 0.3 nM 9.52
CHEMBL3800091 EC50 = 0.39 nM 9.41
CHEMBL3799693 EC50 = 0.44 nM 9.36
CHEMBL3800257 EC50 = 0.44 nM 9.36
CHEMBL3794064 EC50 = 0.47 nM 9.33
CHEMBL3798735 EC50 = 0.54 nM 9.27
CHEMBL3797415 EC50 = 0.56 nM 9.25
CHEMBL3800349 EC50 = 0.98 nM 9.01
CHEMBL3798784 EC50 = 0.99 nM 9.00
CHEMBL3800513 EC50 = 1.3 nM 8.89
CHEMBL3800595 EC50 = 1.6 nM 8.80
CHEMBL3799276 EC50 = 1.7 nM 8.77
CHEMBL3798775 EC50 = 3.2 nM 8.49
CHEMBL3800122 EC50 = 5.0 nM 8.30
CHEMBL3798531 EC50 = 5.3 nM 8.28
CHEMBL3798560 EC50 = 25.0 nM 7.60
CHEMBL3799501 EC50 = 44.0 nM 7.36