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Assay Detail

CHEMBL4032272

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Functional
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as increase in S1P-stimulated calcium influx preincubated for 5 mins followed by S1P stimulation measured every 3 secs by fluorescence method
22
Total Activities
22
Compounds Tested
1
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

Discovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P1 and S1P5 Selective Agonist for the Treatment of Autoimmune Diseases.
Kurata H, Kusumi K, Otsuki K, Suzuki R, Kurono M, Komiya T, Hagiya H, Mizuno H, Shioya H, Ono T, Takada Y, Maeda T, Matsunaga N, Kondo T, Tominaga S, Nunoya KI, Kiyoshi H, Komeno M, Nakade S, Habashita H.
J Med Chem (2017) 60 : 9508 -9530
PubMed 29120624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 8.29 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4092538 1 9.24
CHEMBL4074505 1 9.24
CHEMBL4085321 1 9.00
CHEMBL4093489 1 9.00
CHEMBL4095920 1 8.92
CHEMBL4087932 1 8.92
CHEMBL4071753 1 8.85
CHEMBL4093077 1 8.77
CHEMBL4084786 1 8.59
CHEMBL4095501 1 8.52
CHEMBL1962532 1 8.52
CHEMBL4065871 1 8.46
CHEMBL4075067 1 8.35
CHEMBL4103252 1 8.30
CHEMBL4101237 1 8.18
CHEMBL4100785 1 8.10
CHEMBL4063139 1 7.89
CHEMBL4074023 1 7.72
CHEMBL4062652 1 7.27
CHEMBL4077888 1 7.24
CHEMBL4065407 1 7.01
CHEMBL4059628 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4092538 EC50 = 0.58 nM 9.24
CHEMBL4074505 EC50 = 0.58 nM 9.24
CHEMBL4085321 EC50 = 1.0 nM 9.00
CHEMBL4093489 EC50 = 1.0 nM 9.00
CHEMBL4095920 EC50 = 1.2 nM 8.92
CHEMBL4087932 EC50 = 1.2 nM 8.92
CHEMBL4071753 EC50 = 1.4 nM 8.85
CHEMBL4093077 EC50 = 1.7 nM 8.77
CHEMBL4084786 EC50 = 2.6 nM 8.59
CHEMBL4095501 EC50 = 3.0 nM 8.52
CHEMBL1962532 EC50 = 3.0 nM 8.52
CHEMBL4065871 EC50 = 3.5 nM 8.46
CHEMBL4075067 EC50 = 4.5 nM 8.35
CHEMBL4103252 EC50 = 5.0 nM 8.30
CHEMBL4101237 EC50 = 6.6 nM 8.18
CHEMBL4100785 EC50 = 7.9 nM 8.10
CHEMBL4063139 EC50 = 13.0 nM 7.89
CHEMBL4074023 EC50 = 19.0 nM 7.72
CHEMBL4062652 EC50 = 54.0 nM 7.27
CHEMBL4077888 EC50 = 57.0 nM 7.24
CHEMBL4065407 EC50 = 97.0 nM 7.01
CHEMBL4059628 EC50 = 540.0 nM 6.27