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Assay Detail

CHEMBL3404799

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

Functional
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
37
Total Activities
32
Compounds Tested
2
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 1 (CHEMBL4333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor.
Buzard DJ, Schrader TO, Zhu X, Lehmann J, Johnson B, Kasem M, Kim SH, Kawasaki A, Lopez L, Moody J, Han S, Gao Y, Edwards J, Barden J, Thatte J, Gatlin J, Jones RM.
Bioorg Med Chem Lett (2015) 25 : 659 -663
PubMed 25532755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 35 8.50 10.52
IC50 2 10.32 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3403631 3 11.00
CHEMBL3403619 2 10.52
CHEMBL3403632 1 10.40
CHEMBL3403630 1 10.40
CHEMBL3400909 1 10.40
CHEMBL3400910 1 10.40
CHEMBL3403626 1 9.85
CHEMBL3403636 1 9.82
CHEMBL3400916 1 9.52
CHEMBL3403622 1 9.39
CHEMBL3403629 1 9.32
CHEMBL3403634 1 9.17
CHEMBL3403620 2 8.92
CHEMBL3403621 2 8.85
CHEMBL3403628 1 8.77
CHEMBL3403635 1 8.77
CHEMBL3403633 1 8.68
CHEMBL3400906 1 8.64
CHEMBL3403623 1 8.48
CHEMBL3403625 1 8.17
CHEMBL3403627 1 7.96
CHEMBL3400911 1 7.72
CHEMBL3400908 1 7.66
CHEMBL3400907 1 7.60
CHEMBL3403617 1 6.82
CHEMBL3403624 1 6.77
CHEMBL3403618 1 6.77
CHEMBL3400913 1 6.66
CHEMBL3400914 1 6.54
CHEMBL3400917 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3403631 IC50 = 0.01 nM 11.00
CHEMBL3403619 EC50 = 0.03 nM 10.52
CHEMBL3400910 EC50 = 0.04 nM 10.40
CHEMBL3400909 EC50 = 0.04 nM 10.40
CHEMBL3403630 EC50 = 0.04 nM 10.40
CHEMBL3403631 EC50 = 0.04 nM 10.40
CHEMBL3403632 EC50 = 0.04 nM 10.40
CHEMBL3403619 EC50 = 0.06 nM 10.22
CHEMBL3403626 EC50 = 0.14 nM 9.85
CHEMBL3403636 EC50 = 0.15 nM 9.82
CHEMBL3403631 IC50 = 0.23 nM 9.64
CHEMBL3400916 EC50 = 0.3 nM 9.52
CHEMBL3403622 EC50 = 0.41 nM 9.39
CHEMBL3403629 EC50 = 0.48 nM 9.32
CHEMBL3403634 EC50 = 0.67 nM 9.17
CHEMBL3403620 EC50 = 1.2 nM 8.92
CHEMBL3403621 EC50 = 1.4 nM 8.85
CHEMBL3403628 EC50 = 1.7 nM 8.77
CHEMBL3403635 EC50 = 1.7 nM 8.77
CHEMBL3403621 EC50 = 2.0 nM 8.70
CHEMBL3403633 EC50 = 2.1 nM 8.68
CHEMBL3403620 EC50 = 2.2 nM 8.66
CHEMBL3400906 EC50 = 2.3 nM 8.64
CHEMBL3403623 EC50 = 3.3 nM 8.48
CHEMBL3403625 EC50 = 6.8 nM 8.17
CHEMBL3403627 EC50 = 11.0 nM 7.96
CHEMBL3400911 EC50 = 19.0 nM 7.72
CHEMBL3400908 EC50 = 22.0 nM 7.66
CHEMBL3400907 EC50 = 25.0 nM 7.60
CHEMBL3403617 EC50 = 150.0 nM 6.82
CHEMBL3403618 EC50 = 170.0 nM 6.77
CHEMBL3403624 EC50 = 170.0 nM 6.77
CHEMBL3400913 EC50 = 220.0 nM 6.66
CHEMBL3400914 EC50 = 290.0 nM 6.54
CHEMBL3400917 EC50 = 400.0 nM 6.40
CHEMBL3400915 EC50 = 10000.0 nM 5.00
CHEMBL3400912 EC50 = 10000.0 nM 5.00