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BioAssay: AID 1801

Summary of probe development efforts to identify agonists of Sphingosine 1-Phosphate Receptor 4 (S1P4)

Name: Summary of probe development efforts to identify agonists of Sphingosine 1-Phosphate Receptor 4 (S1P4) ..more
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Probe(2)
 
 
Active(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Probe(2)
 
 
Active(2)
 
 
AID: 1801
Data Source: The Scripps Research Institute Molecular Screening Center (S1P4_AG_LEADS_SUMMARY)
BioAssay Type: Panel, Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2009-06-03
Modify Date: 2012-03-02

Data Table ( Complete ):           View Probe Data    View Active Data    View All Data
Target
BioActive Compounds: Chemical Probe: 2    Active: 2
Related Experiments
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AIDNameTypeComment
1509Primary Cell-Based Assay to Identify Agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)Screeningdepositor-specified cross reference: Primary screen (S1P4 agonists in singlicate)
1523Confirmation cell-based high throughput assay for agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)Screeningdepositor-specified cross reference: Confirmation screen (S1P4 agonists in triplicate)
1563Counterscreen assay for S1P4 agonists: Cell-based high throughput screening assay to identify agonists of the Sphingosine 1-Phosphate Receptor 1 (S1P1)Screeningdepositor-specified cross reference: Counterscreen (S1P1 agonists in triplicate)
1686Fluorescence dose response cell-based high throughput screening assay for agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4)Confirmatorydepositor-specified cross reference: Dose response (S1P4 agonists in triplicate)
1701Fluorescence-based counterscreen assay for S1P4 agonists: Cell-based dose response high throughput screening assay to identify agonists of the Sphingosine 1-Phosphate Receptor 1 (S1P1)Confirmatorydepositor-specified cross reference: Dose response counterscreen (S1P1 agonists in triplicate)
463107Late-stage fluorescence dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Synthesized compoundsConfirmatorydepositor-specified cross reference: Late stage dose response (S1P4 agonists in triplicate)
463118Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 1 (S1P1) counterscreen assayConfirmatorydepositor-specified cross reference: Late stage dose response counterscreen (S1P1 agonists in triplicate)
463119Late-stage assay provider results from the probe development effort to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): luminescence-based cell-based dose response assay to determine cytotoxicity of agonist compoundsConfirmatorydepositor-specified cross reference: Late stage dose response counterscreen (Cytotoxicity in quadruplicate)
463122Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 2 (S1P2) counterscreen assayConfirmatorydepositor-specified cross reference: Late stage dose response counterscreen (S1P2 agonists in triplicate)
463123Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 3 (S1P3) counterscreen assayConfirmatorydepositor-specified cross reference: Late stage dose response counterscreen (S1P3 agonists in triplicate)
463129Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assayConfirmatorydepositor-specified cross reference: Late stage dose response counterscreen (S1P5 agonists in triplicate)
463225Late-stage fluorescence dose response cell-based counterscreening assay for agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonistConfirmatorydepositor-specified cross reference: Late stage dose response counterscreen (inhibition by S1P4-selective antagonist)
504400Late-stage counterscreen panel assay for S1P4 agonists: Ricerca HitProfilingScreen + CYP450Otherdepositor-specified cross reference: Late-stage counterscreen panel assay (Ricerca hit profiling CYP450)
504460Late-stage fluorescence dose response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): purchased compounds EC50Confirmatorydepositor-specified cross reference: Late-stage dose response(S1P4 agonists in triplicate)
504867Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) agonist assay Set 2Confirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (S1P5 agonists in triplicate)
504869Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) antagonist assay Set 2Confirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (S1P5 antagonists in triplicate)
504870Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 1 (S1P1) agonist assay Set 2Confirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (S1P1 agonists in triplicate)
504871Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist controlConfirmatorydepositor-specified cross reference
504872Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 3 (S1P3) antagonist assay Set 2Confirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (S1P3 antagonists in triplicate)
504873Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 2 (S1P2) agonist assay Set 2Confirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (S1P2 agonists in triplicate)
504875Late-stage assay provider results from the probe development effort to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): luminescence-based cell-based dose response assay to determine cytotoxicity of agonist compounds Set 2Confirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (cytotoxicity in six replicates)
504876Late-stage fluorescence dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 4 (S1P4) antagonist assay Set 2Confirmatorydepositor-specified cross reference
504877Late-stage fluorescence dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Synthesized compounds set 2Otherdepositor-specified cross reference: Late-stage dose response (S1P4 agonists in triplicate)
504879Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 3 (S1P3) agonist assay Set 2Confirmatorydepositor-specified cross reference: Late-stage dose response (S1P3 agonists in triplicate)
504880Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 1 (S1P1) antagonist assayConfirmatorydepositor-specified cross reference: Late-stage dose response (S1P1 antagonists in triplicate)
504881Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 2 (S1P2) antagonist assay Set 2Confirmatorydepositor-specified cross reference: Late-stage dose response (S1P2 antagonists in triplicate)
504917Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 1.2 nMConfirmatorydepositor-specified cross reference: Late-stage dose-response counterscreen (S1P4-selective antagonist 1.2 nM)
504918Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 0.4 nMConfirmatorydepositor-specified cross reference: Late-stage dose-response counterscreen (S1P4-selective antagonist 0.4 nM)
504919Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 11 nMConfirmatorydepositor-specified cross reference: Late-stage dose-response counterscreen (S1P4-selective antagonist 11 nM)
504921Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 33 nMConfirmatorydepositor-specified cross reference: Late-stage dose-response counterscreen (S1P4-selective antagonist 33 nM)
504923Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 100 nMConfirmatorydepositor-specified cross reference: Late-stage dose-response counterscreen (S1P4-selective antagonist 100 nM)
504924Late-stage fluorescence-based dose-response cell-based counterscreen assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): inhibition by S1P4-selective antagonist 3.7 nMConfirmatorydepositor-specified cross reference: Late-stage dose-response counterscreen (S1P4-selective antagonist 3.7 nM)
540332Late-stage counterscreen panel assay for S1P4 agonists: Ricerca HitProfilingScreen + CYP450: Set 2Otherdepositor-specified cross reference: Late-stage counterscreen panel assay (Ricerca hit profiling CYP450)
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC)
Center Affiliation: The Scripps Research Institute (TSRI)
Assay Provider: Michael Oldstone, TSRI
Network: Molecular Library Probe Production Center Network (MLPCN)
Grant Proposal Number: U01 AI074564 Fast Track
Grant Proposal PI: Michael Oldstone, TSRI
External Assay ID: S1P4_AG_LEADS_SUMMARY

Name: Summary of probe development efforts to identify agonists of Sphingosine 1-Phosphate Receptor 4 (S1P4)

Description:

Pandemic influenza represents a significant public health threat, due in part to immune cell-mediated lung tissue damage induced during viral infection. Sphingosine 1-phosphate (S1P) is a bioactive phospholipid released by activated blood platelets and serves to influence endothelial integrity, lung epithelial integrity (1), and lymphocyte recirculation (2-5) through five related high affinity G-protein coupled receptors. Recently, modulation of S1P receptors locally in the lungs was shown to alter dendritic cell activation and accumulation in the mediastinal lymph nodes, resulting in blunted T cell responses and control of immunopathological features of influenza virus infection (6). Reports showing that S1P5 expression is very low in dendritic cells but that S1P4 is highly expressed (7), suggest that chemical activation of the S1P4 receptor subtype in the airways could be efficient at controlling the immunopathological response to viral infection. S1P4 is coupled to Ga(i) and Ga(o) G-proteins and activates ERK MAPK and PLC downstream pathways (8). Thus, the identification of compounds that act as selective S1P4 agonists will provide insight into S1P4 biology and may serve as useful tools to limit lung tissue injury resulting from influenza infection.

Summary of Probe Development Effort:

This probe development effort is focused on the identification of S1P4 agonists. Following uHTS primary, confirmation, and dose response screening and counterscreening against the S1P1 receptor, a number of compounds of interest emerged. SAR analysis by purchase and synthesis was conducted on the lead hit. Titration assays were performed to determine potency and selectivity against the other S1P family member receptors S1P1, S1P2, S1P3, and S1P5, as well as cytotoxicity. Compound SID 87544119, with an EC50 for S1P4 of 46.3 nM and EC50s > 50 uM for the other S1P family of receptors, was selected as an exemplar of the potent set of S1P4 agonists. Compound SID 87544119 is also inhibited by an S1P4 receptor-selective antagonist with an IC50 of 0.83 uM.

All AIDs that contain results associated with this project can be found in the "Related Bioassays" section of this Summary AID. A probe report has been submitted. The results of our probe development efforts can be found at http://mlpcn.florida.scripps.edu/index.php/probes/probe-reports. A probe report for SID 87544119 can be found in the Molecular Libraries Bookshelf (PubMed Books) (http://www.ncbi.nlm.nih.gov/books) under ML178.


References:

1. Sanna, M.G., J. Liao, E. Jo, C. Alfonso, M.Y. Ahn, M.S. Peterson, B. Webb, S. Lefebvre, J. Chun, N. Gray, and H. Rosen, Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem, 2004. 279(14): p. 13839-48.
2. Forrest, M., S.Y. Sun, R. Hajdu, J. Bergstrom, D. Card, G. Doherty, J. Hale, C. Keohane, C. Meyers, J. Milligan, S. Mills, N. Nomura, H. Rosen, M. Rosenbach, G.J. Shei, Singer, II, M. Tian, S. West, V. White, J. Xie, R.L. Proia, and S. Mandala, Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes. J Pharmacol Exp Ther, 2004. 309(2): p. 758-68.
3. Gon, Y., M.R. Wood, W.B. Kiosses, E. Jo, M.G. Sanna, J. Chun, and H. Rosen, S1P3 receptor-induced reorganization of epithelial tight junctions compromises lung barrier integrity and is potentiated by TNF. Proc Natl Acad Sci U S A, 2005. 102(26): p. 9270-5.
4. Wei, S.H., H. Rosen, M.P. Matheu, M.G. Sanna, S.K. Wang, E. Jo, C.H. Wong, I. Parker, and M.D. Cahalan, Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses. Nat Immunol, 2005. 6(12): p. 1228-35.
5. Alfonso, C., M.G. McHeyzer-Williams, and H. Rosen, CD69 down-modulation and inhibition of thymic egress by short- and long-term selective chemical agonism of sphingosine 1-phosphate receptors. Eur J Immunol, 2006. 36(1): p. 149-59.
6. Jo, E., M.G. Sanna, P.J. Gonzalez-Cabrera, S. Thangada, G. Tigyi, D.A. Osborne, T. Hla, A.L. Parrill, and H. Rosen, S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate. Chem Biol, 2005. 12(6): p. 703-15.
7. Maeda, Y., Matsuyuki, H., Shimano, K., Kataoka, H., Sugahara, K., and Chiba, K., Migration of CD4 T cells and dendritic cells toward sphingosine 1-phosphate (S1P) is mediated by different receptor subtypes: S1P regulates the functions of murine mature dendritic cells via S1P receptor type 3. J Immunol, 2007. 178(6): p. 3437-46.
8. Toman, R.E. and S. Spiegel, Lysophospholipid receptors in the nervous system. Neurochem Res, 2002. 27(7-8): p. 619-27.

Keywords:

Summary AID, Sphingosine Receptor, Sphingosine-1-phosphate receptor 4, S1P4, S1PR4, EDG6, LPC1, agonist, activator, HTS, GPCR, 1536, Tango, FRET, GAL4-VP16, beta-arrestin, beta-lactamase, BLA, reporter gene, fluorescence, dose response, counterscreen, S1P1, EDG1, EDG-1, Scripps, Scripps Florida, Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Library Probe Production Center Network, MLPCN.
Panel Information
Related BioAssays
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1AID 463107Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
2AID 463225Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
3AID 463119
4AID 463118sphingosine 1-phosphate receptor 1 [Homo sapiens] [gi:13027636]
Taxonomy id: 9606
Gene id: 1901
5AID 463122sphingosine 1-phosphate receptor 2 [Homo sapiens] [gi:134244587]
Taxonomy id: 9606
Gene id: 9294
6AID 463123sphingosine 1-phosphate receptor 3 [Homo sapiens] [gi:38788193]
Taxonomy id: 9606
Gene id: 1903
7AID 463129Sphingosine-1-phosphate receptor 5 [Homo sapiens] [gi:21961528]
Taxonomy id: 9606
Gene id: 53637
8AID 504871Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
9AID 504877_1Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
10AID 504918Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
11AID 504917Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
12AID 504867Sphingosine-1-phosphate receptor 5 [Homo sapiens] [gi:21961528]
Taxonomy id: 9606
Gene id: 53637
13AID 504881sphingosine 1-phosphate receptor 2 [Homo sapiens] [gi:134244587]
Taxonomy id: 9606
Gene id: 9294
14AID 504872sphingosine 1-phosphate receptor 3 [Homo sapiens] [gi:38788193]
Taxonomy id: 9606
Gene id: 1903
15AID 504919Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
16AID 504921Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
17AID 504923Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
18AID 504924Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
19AID 504875
20AID 504869Sphingosine-1-phosphate receptor 5 [Homo sapiens] [gi:21961528]
Taxonomy id: 9606
Gene id: 53637
21AID 504870sphingosine 1-phosphate receptor 1 [Homo sapiens] [gi:13027636]
Taxonomy id: 9606
Gene id: 1901
22AID 504873sphingosine 1-phosphate receptor 2 [Homo sapiens] [gi:134244587]
Taxonomy id: 9606
Gene id: 9294
23AID 504876Sphingosine-1-phosphate receptor 4 [Homo sapiens] [gi:15929025]
Taxonomy id: 9606
Gene id: 8698
24AID 504879sphingosine 1-phosphate receptor 3 [Homo sapiens] [gi:38788193]
Taxonomy id: 9606
Gene id: 1903
25AID 504880sphingosine 1-phosphate receptor 1 [Homo sapiens] [gi:13027636]
Taxonomy id: 9606
Gene id: 1901

§ Panel component ID.
Protocol
Please see AIDs 1509, 1523, 1563 1686, 1701 for protocols performed in this probe development effort.
Comment
This probe development project is still underway at the SRIMSC.
Categorized Comment - additional comments and annotations
From MLP Probe Report:
Probe count: 2
MLP Probe ML# for probe 1: ML178
PubChem Substance ID (SID) for probe 1: 87544119
PubChem Compound ID (CID) for probe 1: 44620892
Probe type for probe 1: Agonist
IC50/EC50 (nM) for probe 1: 46.3
Target for probe 1: S1P4 (gi: 15929025)
Disease relevance for probe 1: influenza
Anti-target for probe 1: S1P1
Fold selectivity for probe 1: >1000
NCBI Book chapter link for probe 1: http://www.ncbi.nlm.nih.gov/books/NBK98915/ (ID: 2961648)
Grant number for probe 1: AI074564
MLP Probe ML# for probe 2: ML248
PubChem Substance ID (SID) for probe 2: 103911214
PubChem Compound ID (CID) for probe 2: 49835928
Probe type for probe 2: Agonist
IC50/EC50 (nM) for probe 2: <80
Target for probe 2: S1P4 (gi: 15929025)
Anti-target for probe 2: S1P1
Fold selectivity for probe 2: >316
NCBI Book chapter link for probe 2: http://www.ncbi.nlm.nih.gov/books/NBK143556/ (ID: 3036516)
Grant number for probe 2: AI074564
NCBI Book chapter title for probe 1: Probe Development Efforts to Identify Novel Agonists of the Sphingosine 1-phosphate Receptor 4 (S1P4)
NCBI Book chapter title for probe 2: Identification of a Novel Agonist of the Sphingosine 1-phosphate Receptor 4 (S1P4)
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1ML #Unique alphanumeric identifier assigned to a chemical probe molecule within the Molecular Libraries Probe Production Centers Network (MLPCN).String
2EC50 [AID 463107]*Data from AID 463107. The value for concentration at which 50% activation is observed; EC50 shown in uM.1Sphingosine-1-phosphate receptor 4 [Homo sapiens]FloatμM
3IC50 [AID 463225]*Data from AID 463225. The value for concentration at which 50% inhibition is observed; IC50 shown in uM.2Sphingosine-1-phosphate receptor 4 [Homo sapiens]FloatμM
4Qualifier [AID 463119]Data from AID 463119. Activity Qualifier identifies if the resultant data CC50 came from a fitted curve or was determined manually to be less than or greater than its listed CC50 concentration.3String
5CC50 [AID 463119]*Data from AID 463119. The value for concentration at which 50% inhibition is observed; CC50 shown in uM.3FloatμM
6Qualifier [AID 463118]Data from AID 463118. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.4sphingosine 1-phosphate receptor 1 [Homo sapiens]String
7EC50 [AID 463118]*Data from AID 463118. The value for concentration at which 50% activation is observed; EC50 shown in uM.4FloatμM
8Qualifier [AID 463122]Data from AID 463122. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.5sphingosine 1-phosphate receptor 2 [Homo sapiens]String
9EC50 [AID 463122]*Data from AID 463122. The value for concentration at which 50% activation is observed; EC50 shown in uM.5FloatμM
10Qualifier [AID 463123]Data from AID 463123. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.6sphingosine 1-phosphate receptor 3 [Homo sapiens]String
11EC50 [AID 463123]*Data from AID 463123. The value for concentration at which 50% activation is observed; EC50 shown in uM.6FloatμM
12Qualifier [AID 463129]Data from AID 463129. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.7Sphingosine-1-phosphate receptor 5 [Homo sapiens]String
13EC50 [AID 463129]*Data from AID 463129. The value for concentration at which 50% activation is observed; EC50 shown in uM.7FloatμM
14EC50 [AID 504871]*Data from AID 504871. The value for concentration at which 50% activation is observed; EC50 shown in uM.8Sphingosine-1-phosphate receptor 4 [Homo sapiens]FloatμM
15EC50 [AID 504877_1]*Data from AID 504877_1. The value for concentration at which 50% activation is observed; EC50 shown in uM.9Sphingosine-1-phosphate receptor 4 [Homo sapiens]FloatμM
16EC50 [AID 504918]*Data from AID 504918. The value for concentration at which 50% activation is observed; EC50 shown in uM.10Sphingosine-1-phosphate receptor 4 [Homo sapiens]FloatμM
17EC50 [AID 504917]*Data from AID 504917. The value for concentration at which 50% activation is observed; EC50 shown in uM.11Sphingosine-1-phosphate receptor 4 [Homo sapiens]FloatμM
18EC50 [AID 504867]*Data from AID 504867. The value for concentration at which 50% activation is observed; EC50 shown in uM.12Sphingosine-1-phosphate receptor 5 [Homo sapiens]FloatμM
19IC50 [AID 504881]*Data from AID 504881. The value for concentration at which 50% inhibition is observed; IC50 shown in uM.13sphingosine 1-phosphate receptor 2 [Homo sapiens]FloatμM
20IC50 [AID 504872]*Data from AID 504872. The value for concentration at which 50% inhibition is observed; IC50 shown in uM.14sphingosine 1-phosphate receptor 3 [Homo sapiens]FloatμM
21Qualifier [AID 504919]Data from AID 504919. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.15Sphingosine-1-phosphate receptor 4 [Homo sapiens]String
22EC50 [AID 504919]*Data from AID 504919. The value for concentration at which 50% activation is observed; EC50 shown in uM.15FloatμM
23Qualifier [AID 504921]Data from AID 504921. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.16Sphingosine-1-phosphate receptor 4 [Homo sapiens]String
24EC50 [AID 504921]*Data from AID 504921. The value for concentration at which 50% activation is observed; EC50 shown in uM.16FloatμM
25Qualifier [AID 504923]Data from AID 504923. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.17Sphingosine-1-phosphate receptor 4 [Homo sapiens]String
26EC50 [AID 504923]*Data from AID 504923. The value for concentration at which 50% activation is observed; EC50 shown in uM.17FloatμM
27Qualifier [AID 504924]Data from AID 504924. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.18Sphingosine-1-phosphate receptor 4 [Homo sapiens]String
28EC50 [AID 504924]*Data from AID 504924. The value for concentration at which 50% activation is observed; EC50 shown in uM.18FloatμM
29Qualifier [AID 504875]Data from AID 504875. Activity Qualifier identifies if the resultant data CC50 came from a fitted curve or was determined manually to be less than or greater than its listed CC50 concentration.19String
30CC50 [AID 504875]*Data from AID 504875. The value for concentration at which 50% inhibition is observed; CC50 shown in uM.19FloatμM
31Qualifier [AID 504869]Data from AID 504869. Activity Qualifier identifies if the resultant data IC50 came from a fitted curve or was determined manually to be less than or greater than its listed IC50 concentration.20Sphingosine-1-phosphate receptor 5 [Homo sapiens]String
32IC50 [AID 504869]*Data from AID 504869. The value for concentration at which 50% inhibition is observed; IC50 shown in uM.20FloatμM
33Qualifier [AID 504870]Data from AID 504870. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.21sphingosine 1-phosphate receptor 1 [Homo sapiens]String
34EC50 [AID 504870]*Data from AID 504870. The value for concentration at which 50% activation is observed; EC50 shown in uM.21FloatμM
35Qualifier [AID 504873]Data from AID 504873. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.22sphingosine 1-phosphate receptor 2 [Homo sapiens]String
36EC50 [AID 504873]*Data from AID 504873. The value for concentration at which 50% activation is observed; EC50 shown in uM.22FloatμM
37Qualifier [AID 504876]Data from AID 504876. Activity Qualifier identifies if the resultant data IC50 came from a fitted curve or was determined manually to be less than or greater than its listed IC50 concentration.23Sphingosine-1-phosphate receptor 4 [Homo sapiens]String
38IC50 [AID 504876]*Data from AID 504876. The value for concentration at which 50% inhibition is observed; IC50 shown in uM.23FloatμM
39Qualifier [AID 504879]Data from AID 504879. Activity Qualifier identifies if the resultant data EC50 came from a fitted curve or was determined manually to be less than or greater than its listed EC50 concentration.24sphingosine 1-phosphate receptor 3 [Homo sapiens]String
40EC50 [AID 504879]*Data from AID 504879. The value for concentration at which 50% activation is observed; EC50 shown in uM.24FloatμM
41Qualifier [AID 504880]Data from AID 504880. Activity Qualifier identifies if the resultant data IC50 came from a fitted curve or was determined manually to be less than or greater than its listed IC50 concentration.25sphingosine 1-phosphate receptor 1 [Homo sapiens]String
42IC50 [AID 504880]*Data from AID 504880. The value for concentration at which 50% inhibition is observed; IC50 shown in uM.25FloatμM

* Activity Concentration. § Panel component ID.
Additional Information
Grant Number: U01 AI074564

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