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Assay Detail

CHEMBL5734827

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

Binding
S1P1 assay: The method involves contacting the receptor with a suitable concentration of an inventive compound to bring about activation of the receptor. The contacting can take place in vitro, for example in carrying out an assay to determine the S1P receptor activation activity of an inventive compound undergoing experimentation related to a submission for regulatory approval.
ChEMBL ↗
501
Total Activities
162
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Modulators of sphingosine phosphate receptors
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 167 7.04 10.00
kon 167 - -
k_off 167 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5889151 — — 6 10.00
CHEMBL6032090 — — 3 9.85
CHEMBL5810275 — — 3 9.82
CHEMBL5975353 — — 3 9.70
CHEMBL5927389 — — 3 9.30
CHEMBL6056220 — — 3 9.28
CHEMBL6017446 — — 3 9.15
CHEMBL5873453 — — 3 9.11
CHEMBL6004182 — — 3 9.10
CHEMBL5859650 — — 3 9.00
CHEMBL5820239 — — 3 9.00
CHEMBL5973208 — — 3 8.96
CHEMBL3922179 — — 3 8.96
CHEMBL5814448 — — 9 8.82
CHEMBL5997688 — — 3 8.77
CHEMBL5816974 — — 3 8.77
CHEMBL5901284 — — 3 8.66
CHEMBL5892144 — — 3 8.60
CHEMBL5870305 — — 3 8.57
CHEMBL5806118 — — 3 8.52
CHEMBL5986504 — — 3 8.51
CHEMBL5954930 — — 3 8.48
CHEMBL5948151 — — 3 8.47
CHEMBL1452805 — — 3 8.43
CHEMBL5805558 — — 3 8.39
CHEMBL5825797 — — 3 8.38
CHEMBL5956241 — — 3 8.38
CHEMBL5806759 — — 3 8.30
CHEMBL5858468 — — 3 8.30
CHEMBL5873753 — — 3 8.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5889151 — EC50 = 0.1 nM 10.00
CHEMBL6032090 — EC50 = 0.14 nM 9.85
CHEMBL5810275 — EC50 = 0.15 nM 9.82
CHEMBL5975353 — EC50 = 0.2 nM 9.70
CHEMBL5927389 — EC50 = 0.5 nM 9.30
CHEMBL6056220 — EC50 = 0.52 nM 9.28
CHEMBL6017446 — EC50 = 0.7 nM 9.15
CHEMBL5873453 — EC50 = 0.78 nM 9.11
CHEMBL6004182 — EC50 = 0.8 nM 9.10
CHEMBL5859650 — EC50 = 1.0 nM 9.00
CHEMBL5820239 — EC50 = 1.0 nM 9.00
CHEMBL5973208 — EC50 = 1.1 nM 8.96
CHEMBL3922179 — EC50 = 1.1 nM 8.96
CHEMBL5814448 — EC50 = 1.5 nM 8.82
CHEMBL5997688 — EC50 = 1.7 nM 8.77
CHEMBL5816974 — EC50 = 1.7 nM 8.77
CHEMBL5901284 — EC50 = 2.2 nM 8.66
CHEMBL5892144 — EC50 = 2.5 nM 8.60
CHEMBL5870305 — EC50 = 2.7 nM 8.57
CHEMBL5806118 — EC50 = 3.0 nM 8.52
CHEMBL5986504 — EC50 = 3.1 nM 8.51
CHEMBL5954930 — EC50 = 3.3 nM 8.48
CHEMBL5948151 — EC50 = 3.4 nM 8.47
CHEMBL1452805 — EC50 = 3.7 nM 8.43
CHEMBL5805558 — EC50 = 4.1 nM 8.39
CHEMBL5956241 — EC50 = 4.2 nM 8.38
CHEMBL5825797 — EC50 = 4.2 nM 8.38
CHEMBL5858468 — EC50 = 5.0 nM 8.30
CHEMBL5806759 — EC50 = 5.0 nM 8.30
CHEMBL5873753 — EC50 = 5.9 nM 8.23
CHEMBL5807356 — EC50 = 6.0 nM 8.22
CHEMBL5814448 — EC50 = 6.1 nM 8.21
CHEMBL5903888 — EC50 = 6.9 nM 8.16
CHEMBL5756135 — EC50 = 7.0 nM 8.15
CHEMBL588026 — EC50 = 7.3 nM 8.14
CHEMBL5749091 — EC50 = 8.0 nM 8.10
CHEMBL5996016 — EC50 = 8.8 nM 8.06
CHEMBL6042234 — EC50 = 10.0 nM 8.00
CHEMBL5741678 — EC50 = 10.1 nM 8.00
CHEMBL5978097 — EC50 = 10.7 nM 7.97
CHEMBL6012438 — EC50 = 10.8 nM 7.97
CHEMBL6015803 — EC50 = 11.7 nM 7.93
CHEMBL5874736 — EC50 = 11.7 nM 7.93
CHEMBL5749587 — EC50 = 12.2 nM 7.91
CHEMBL5759499 — EC50 = 12.5 nM 7.90
CHEMBL5778705 — EC50 = 13.0 nM 7.89
CHEMBL6026958 — EC50 = 14.9 nM 7.83
CHEMBL5992375 — EC50 = 15.4 nM 7.81
CHEMBL6026244 — EC50 = 15.9 nM 7.80
CHEMBL5814448 — EC50 = 17.8 nM 7.75