Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL3806205 s1pr1_human Human No 11.2 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by HTRF analysisAgonist activity at human S1P1 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by HTRF analysis
409 9 3 3 4.8 CCCCCC[C@@H]1CCC2=C(C1)C=CC(=C2)[C@H]3CC[C@@](C3)(COP(=O)(O)O)N
CHEMBL2032300 s1pr1_human Human No 11.0 EC50 = 0.0 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
425 7 1 6 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3ccn4CCC(=O)O)no2)cc1Cl
CHEMBL366208 s1pr1_human Human Yes 10.9 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assayAgonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL2018176 s1pr1_human Human No 10.9 EC50 = 0.0 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCC(=O)O)c[nH]c34)no2)cc1Cl
CHEMBL2059683 s1pr1_human Human No 10.8 EC50 = 0.0 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
493 10 2 6 5.5 CCc1c(CCNCC(=O)O)cccc1-c1nsc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL1093686 s1pr1_human Human No 10.7 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assayAgonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay
397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@H]([C@@](C)(N)COP(=O)(O)O)C2
CHEMBL2059684 s1pr1_human Human No 10.7 EC50 = 0.0 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
507 10 1 6 5.8 CCc1c(CCN(C)CC(=O)O)cccc1-c1nsc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL114606 s1pr1_human Human Yes 10.7 EC50 = 0.0 nM Bind
Agonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysisAgonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysis
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL366208 s1pr1_human Human Yes 10.7 EC50 = 0.0 nM Bind
Agonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysisAgonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysis
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL3359523 s1pr1_human Human No 10.7 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F
CHEMBL3359522 s1pr1_human Human No 10.6 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N
CHEMBL2032301 s1pr1_human Human No 10.6 EC50 = 0.0 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
459 7 1 6 5.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3c(Cl)cn4CCC(=O)O)no2)cc1Cl
CHEMBL225155 s1pr1_human Human Yes 10.6 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assayAgonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay
379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O
CHEMBL4093489 s1pr1_human Human Yes 10.6 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1
CHEMBL4093489 s1pr1_rat Rat Yes 10.5 EC50 = 0.0 nM Funct
Agonist activity at rat S1P1 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at rat S1P1 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1
CHEMBL378436 s1pr1_human Human No 10.5 EC50 = 0.0 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
445 7 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C(F)(F)F)c(C#N)c2)n1
CHEMBL3403619 s1pr1_human Human Yes 10.5 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL2018320 s1pr1_human Human No 10.5 EC50 = 0.0 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
424 7 2 5 4.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCC(N)=O)c[nH]c34)no2)cc1Cl
CHEMBL2032428 s1pr1_human Human No 10.5 EC50 = 0.0 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
454 8 2 4 5.8 O=C(O)CNCCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1
CHEMBL2032430 s1pr1_human Human No 10.5 EC50 = 0.0 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
454 8 2 4 5.8 O=C(O)CCNCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1
CHEMBL3959509 s1pr1_human Human No 10.5 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 assessed as stimulation of cAMP accumulationAgonist activity at human S1P1 assessed as stimulation of cAMP accumulation
495 5 1 6 5.3 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2onc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL3359522 h9euw9_macmu Rhesus macaque No 10.4 EC50 = 0.0 nM Funct
Agonist activity at monkey S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at monkey S1P1 receptor assessed as cAMP accumulation by HTRF assay
438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N
CHEMBL2018321 s1pr1_human Human No 10.4 EC50 = 0.0 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
438 7 2 5 5.0 CNC(=O)CCc1c[nH]c2c(-c3noc(-c4ccc(OC(C)C)c(Cl)c4)n3)cccc12
CHEMBL2011746 s1pr1_human Human No 10.4 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assayAgonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assay
516 9 1 6 6.1 CCCCN(C(=O)c1ccc(C(F)(F)F)cc1)c1nnc(-c2cccc3c2ccn3CCC(=O)O)s1
CHEMBL3403619 w5vnf7_canlf Dog Yes 10.4 EC50 = 0.0 nM Funct
Agonist activity at dog S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at dog S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL3358920 s1pr1_human Human Yes 10.4 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1
CHEMBL3400909 s1pr1_human Human No 10.4 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
419 7 3 5 4.1 CC(C)Oc1ccc(COc2ccc3[nH]c4c(c3c2)CCNC4CC(=O)O)cc1C#N
CHEMBL3400910 s1pr1_human Human No 10.4 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
460 7 3 3 5.6 CC(C)Cc1ccc(COc2ccc3[nH]c4c(c3c2)CCNC4CC(=O)O)cc1C(F)(F)F
CHEMBL3403630 s1pr1_human Human No 10.4 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
497 7 1 5 6.2 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CCOC2CC(=O)O)cc1C(F)(F)F
CHEMBL3403631 s1pr1_human Human No 10.4 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
454 7 1 6 5.1 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CCOC2CC(=O)O)cc1C#N
CHEMBL3403632 s1pr1_human Human No 10.4 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
507 6 1 4 7.1 O=C(O)CC1OCCn2c1c(Cl)c1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12
CHEMBL3403619 s1pr1_rat Rat Yes 10.4 EC50 = 0.0 nM Funct
Agonist activity at rat S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at rat S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL3358955 s1pr1_human Human No 10.4 EC50 = 0.0 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12
CHEMBL3359522 w5vnf7_canlf Dog No 10.3 EC50 = 0.0 nM Funct
Agonist activity at dog S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at dog S1P1 receptor assessed as cAMP accumulation by HTRF assay
438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N
CHEMBL3359523 w5vnf7_canlf Dog No 10.3 EC50 = 0.0 nM Funct
Agonist activity at dog S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at dog S1P1 receptor assessed as cAMP accumulation by HTRF assay
481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F
CHEMBL3891354 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
406 7 1 6 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCF)no2)cc1C#N
CHEMBL3893180 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCOCC3)no2)cc1C#N
CHEMBL3894084 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
417 6 2 7 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)CN)no2)cc1C#N
CHEMBL3894716 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCO)no2)cc1C#N
CHEMBL3895822 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
431 7 2 7 3.4 CNC(=O)CN[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3895901 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
448 9 2 8 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N(CCO)CCO)no2)cc1C#N
CHEMBL3896496 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
446 8 1 8 4.2 COC(=O)CCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3897106 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
374 5 1 6 4.3 CN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3899152 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
501 6 2 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(CO)CC3)no2)cc1C#N
CHEMBL3899733 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
416 5 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(O)C3)no2)cc1C#N
CHEMBL3899952 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
529 6 1 8 4.6 COC(=O)C1CCN(C(=O)N[C@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)CC1
CHEMBL3902406 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
402 7 1 6 5.0 CCCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3902939 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCOCC3)no2)cc1C#N
CHEMBL3905058 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
471 6 0 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(C(=O)N(C)C)C3)no2)cc1C#N
CHEMBL3905765 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
431 5 1 6 4.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N(C)C)no2)cc1C#N
CHEMBL3906427 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
457 7 1 7 3.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCC3)no2)cc1C#N
CHEMBL3907353 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
444 5 1 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCC(O)CC3)no2)cc1C#N
CHEMBL3907543 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 7 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCN(CCO)CC3)no2)cc1C#N
CHEMBL3910977 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
472 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@@H](N)C3)no2)cc1C#N
CHEMBL3912931 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
551 8 1 9 2.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CCOCC3)no2)cc1C#N
CHEMBL3915065 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
404 4 1 5 5.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C(F)(F)F
CHEMBL3916821 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
434 8 3 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@H](O)CO)no2)cc1C#N
CHEMBL3918031 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N[C@@H](C)CO)no2)cc1C#N
CHEMBL3918159 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 5 1 7 4.4 COC(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3918328 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
511 11 3 9 2.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCNCCO)no2)cc1C#N
CHEMBL3918503 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 8 1 7 4.3 COCCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3919810 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
430 5 0 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CCOC3=O)no2)cc1C#N
CHEMBL3919920 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
347 4 1 6 3.7 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1C#N
CHEMBL3919959 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@H](O)C3)no2)cc1C#N
CHEMBL3920863 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)CN(C)C)no2)cc1C#N
CHEMBL3920889 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 5 1 7 4.4 COC(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3922629 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
347 4 1 6 3.7 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C#N
CHEMBL3924073 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
434 8 3 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@@H](O)CO)no2)cc1C#N
CHEMBL3924318 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
420 7 2 8 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N(CO)CO)no2)cc1C#N
CHEMBL3924832 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
448 7 2 8 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)OCCO)no2)cc1C#N
CHEMBL3926299 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
432 7 1 7 3.8 COCC(=O)NC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3926586 s1pr1_human Human Yes 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
402 5 1 6 4.2 CC(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3926787 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
403 7 2 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NCCN)no2)cc1C#N
CHEMBL3927322 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 7 2 8 3.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CC[C@@H](O)C3)no2)cc1C#N
CHEMBL3930042 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 7 2 8 3.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CC[C@H](O)C3)no2)cc1C#N
CHEMBL3930528 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 7 1 8 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCOCC3)no2)cc1C#N
CHEMBL3931604 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@@H](O)C3)no2)cc1C#N
CHEMBL3931785 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCCS(C)(=O)=O)no2)cc1C#N
CHEMBL3934309 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
529 7 2 7 4.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(CC(=O)O)CC3)no2)cc1C#N
CHEMBL3934482 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCS(C)(=O)=O)no2)cc1C#N
CHEMBL3934530 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
430 5 0 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CCOC3=O)no2)cc1C#N
CHEMBL3935065 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
543 7 1 8 5.0 COC(=O)CC1CCN(C(=O)N[C@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)CC1
CHEMBL3936105 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
529 6 1 8 4.6 COC(=O)C1CCN(C(=O)N[C@@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)CC1
CHEMBL3937763 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
444 6 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(C(=O)O)C3)no2)cc1C#N
CHEMBL3938039 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
515 6 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(C(=O)O)CC3)no2)cc1C#N
CHEMBL3938278 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
472 5 2 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCNCC3)no2)cc1C#N
CHEMBL3939008 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
481 9 2 8 3.2 CNS(=O)(=O)CCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3940245 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
429 5 1 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCNCC3)no2)cc1C#N
CHEMBL3940511 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
471 6 0 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CC(C(=O)N(C)C)C3)no2)cc1C#N
CHEMBL3941756 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
471 7 1 7 4.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCCC3)no2)cc1C#N
CHEMBL3942853 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
432 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)CC(=O)O)no2)cc1C#N
CHEMBL3943755 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
432 6 1 7 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)C(=O)CO)no2)cc1C#N
CHEMBL3944842 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
446 8 1 8 4.2 CC(=O)OCCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3945226 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
482 8 2 8 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)O)no2)cc1C#N
CHEMBL3947288 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
406 7 1 6 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCCF)no2)cc1C#N
CHEMBL3947411 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
495 9 1 8 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN(C)C)no2)cc1C#N
CHEMBL3947465 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
457 6 1 7 3.7 CNC(=O)C1CN([C@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)C1
CHEMBL3949785 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
537 9 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CC[C@@H](O)C3)no2)cc1C#N
CHEMBL3952253 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
438 6 1 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(C)(=O)=O)no2)cc1C#N
CHEMBL3954097 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
446 8 1 7 4.2 CCOCC(=O)NC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3954350 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
537 8 2 9 2.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CC(O)C3)no2)cc1C#N
CHEMBL3954873 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@@H](O)C3)no2)cc1C#N
CHEMBL3955035 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 7 1 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)CCO)no2)cc1C#N
CHEMBL3957449 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1OCC
CHEMBL3957491 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@H](O)C3)no2)cc1C#N
CHEMBL3957713 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
432 8 1 7 4.4 CCN(CCO)[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3958210 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC[C@@H](O)C3)no2)cc1C#N
CHEMBL3960138 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1OCC
CHEMBL3960551 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
424 7 1 6 4.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCC(F)F)no2)cc1C#N
CHEMBL3963066 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
464 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)C3CC3)no2)cc1C#N
CHEMBL3964002 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
416 5 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CC(O)C3)no2)cc1C#N
CHEMBL3964055 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
515 6 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCC(C(=O)O)CC3)no2)cc1C#N
CHEMBL3964817 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
507 9 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CCC3)no2)cc1C#N
CHEMBL3965400 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
402 5 3 6 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=N)N)no2)cc1C#N
CHEMBL3965441 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
374 5 1 6 4.3 CN[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3967098 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
461 9 3 8 2.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)NCCO)no2)cc1C#N
CHEMBL3967100 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
457 7 1 8 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCc3cncs3)no2)cc1C#N
CHEMBL3968024 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
523 9 2 9 2.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CC(O)C3)no2)cc1C#N
CHEMBL3969165 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
390 4 1 5 4.8 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C(F)(F)F
CHEMBL3969712 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)CN(C)C)no2)cc1C#N
CHEMBL3970705 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
565 8 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CCC(O)CC3)no2)cc1C#N
CHEMBL3970830 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@H](C)O)no2)cc1C#N
CHEMBL3971646 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
510 9 1 9 3.5 COC(=O)CCS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3972549 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N[C@H](C)CO)no2)cc1C#N
CHEMBL3973804 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
448 7 2 8 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)OCCO)no2)cc1C#N
CHEMBL3975029 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N[C@H](C)CO)no2)cc1C#N
CHEMBL3976048 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
509 8 1 8 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N(C)C)no2)cc1C#N
CHEMBL3977164 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(O)CC3)no2)cc1C#N
CHEMBL3977376 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC[C@H](O)C3)no2)cc1C#N
CHEMBL3978076 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
464 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)C3CC3)no2)cc1C#N
CHEMBL3979740 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NCCS(C)(=O)=O)no2)cc1C#N
CHEMBL3979815 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
388 6 1 6 4.7 CCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3984513 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
458 6 0 8 4.2 COC(=O)C1CN(C2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)C1
CHEMBL3985742 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
495 8 2 8 2.7 CNC(=O)CS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3987033 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
496 10 1 8 4.0 CCOCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3987097 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
481 9 2 8 3.2 CNCCS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3359522 s1pr1_mouse Mouse No 10.3 EC50 = 0.1 nM Funct
Agonist activity at mouse S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at mouse S1P1 receptor assessed as cAMP accumulation by HTRF assay
438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N
CHEMBL3403619 s1pr1_mouse Mouse Yes 10.3 EC50 = 0.1 nM Funct
Agonist activity at mouse S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at mouse S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL3359523 s1pr1_rat Rat No 10.3 EC50 = 0.1 nM Funct
Agonist activity at rat S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at rat S1P1 receptor assessed as cAMP accumulation by HTRF assay
481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F
CHEMBL2018319 s1pr1_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
453 9 2 5 6.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCCCC(=O)O)c[nH]c34)no2)cc1Cl
CHEMBL3359523 h9euw9_macmu Rhesus macaque No 10.2 EC50 = 0.1 nM Funct
Agonist activity at monkey S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at monkey S1P1 receptor assessed as cAMP accumulation by HTRF assay
481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F
CHEMBL3403619 s1pr1_human Human Yes 10.2 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL225155 s1pr1_human Human Yes 10.2 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O
CHEMBL3359523 s1pr1_mouse Mouse No 10.2 EC50 = 0.1 nM Funct
Agonist activity at mouse S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at mouse S1P1 receptor assessed as cAMP accumulation by HTRF assay
481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F
CHEMBL3359519 s1pr1_human Human No 10.2 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
447 7 1 4 6.0 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C(F)(F)F
CHEMBL378054 s1pr1_human Human No 10.2 EC50 = 0.1 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
405 8 1 6 4.8 CC[C@H](C)Oc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C#N
CHEMBL114606 s1pr1_human Human Yes 10.2 EC50 = 0.1 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assayAgonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL114606 s1pr1_human Human Yes 10.2 EC50 = 0.1 nM Bind
Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysisAgonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL366208 s1pr1_human Human Yes 10.2 EC50 = 0.1 nM Bind
Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysisAgonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL4095920 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
449 9 1 4 5.3 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1
CHEMBL3359522 s1pr1_rat Rat No 10.1 EC50 = 0.1 nM Funct
Agonist activity at rat S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at rat S1P1 receptor assessed as cAMP accumulation by HTRF assay
438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N
CHEMBL3358912 s1pr1_human Human Yes 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 2 2 6.9 O=C(O)CC1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL3358911 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
471 6 2 2 7.3 O=C(O)CC1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCCC4)c(C(F)(F)F)c3)cc21
CHEMBL1091103 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assayAgonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay
413 12 4 4 3.5 CCCCCCCCc1ccc2c(c1)CC[C@@H](C(N)(CO)COP(=O)(O)O)C2
CHEMBL2018322 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
449 7 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCc5nnn[nH]5)c[nH]c34)no2)cc1Cl
CHEMBL2032434 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
494 6 1 4 6.8 O=C(O)CCN1CCC(c2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1
CHEMBL2048293 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1
CHEMBL208924 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL211505 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL3358910 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
428 6 2 3 6.2 N#Cc1cc(COc2ccc3[nH]c4c(c3c2)CCC4CC(=O)O)ccc1C1CCCCC1
CHEMBL1089004 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assayAgonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay
397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@@H]([C@@](C)(N)COP(=O)(O)O)C2
CHEMBL208924 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL3922998 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCC(=O)N(C)C)no2)cc1C#N
CHEMBL3933952 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
482 9 1 8 3.6 COCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3358919 s1pr1_human Human No 10.1 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 2 2 6.9 O=C(O)C[C@@H]1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL3358955 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12
CHEMBL2059687 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
547 9 1 6 6.6 CCc1c(CCN2CCC(C(=O)O)CC2)cccc1-c1nsc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL2048293 s1pr1_rat Rat No 10.0 EC50 = 0.1 nM Funct
Agonist activity against rat S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against rat S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1
CHEMBL211505 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL209484 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
455 7 1 6 5.1 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C(F)(F)F)c(Cl)c2)n1
CHEMBL210942 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
499 7 1 6 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C(F)(F)F)C(F)(F)F)c(C#N)c2)n1
CHEMBL2032441 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
480 7 1 4 6.1 O=C(O)C1CN(CCCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)C1
CHEMBL3893172 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC(O)C3)no2)cc1C#N
CHEMBL3895230 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCO)no2)cc1C#N
CHEMBL3910269 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC(O)C3)no2)cc1C#N
CHEMBL3753584 s1pr1_human Human No 10.0 EC50 = 0.1 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
446 8 2 8 3.6 CC(C)Oc1ccc(-c2nc(-c3cc(F)c(OC[C@H](N)CO)cc3Cl)no2)cc1C#N
CHEMBL3126433 s1pr1_human Human No 10.0 EC50 = 0.1 nM Bind
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assayAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assay
480 10 3 8 3.2 CCc1cc(-c2noc(-c3ccnc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126607 s1pr1_human Human No 10.0 EC50 = 0.1 nM Bind
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assayAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assay
482 12 3 8 3.4 CCc1cc(-c2noc(-c3ccnc(C(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126433 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
480 10 3 8 3.2 CCc1cc(-c2noc(-c3ccnc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126436 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
482 11 3 8 3.0 CCc1cc(-c2noc(-c3cc(C)nc(CC(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126584 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
480 10 3 8 3.1 CCc1cc(-c2noc(-c3cc(C)nc(C4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126588 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
494 11 3 8 3.3 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc(C2CCC2)n1
CHEMBL3126607 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
482 12 3 8 3.4 CCc1cc(-c2noc(-c3ccnc(C(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126620 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
468 10 3 8 2.9 CCc1cc(-c2noc(-c3cnc(C(C)C)c(C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126622 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
494 10 3 8 3.5 CCc1cc(-c2noc(-c3cnc(C4CCCC4)c(C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126623 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
496 12 3 8 3.3 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cnc1CC(C)C
CHEMBL225155 s1pr1_human Human Yes 10.0 EC50 = 0.1 nM Bind
Displacement of [33P]S1P from human recombinant S1P1 receptor expressed in HEK cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P1 receptor expressed in HEK cells by scintillation counting
379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O
CHEMBL3953201 s1pr1_human Human No 10.0 EC50 = 0.1 nM Bind
Homogeneous Time-Resolved Fluorescence (HTRF) Assay: The compound (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid was shown to be an agonist of the S1P1 receptor (e.g., human S1P1 receptor) using the HTRF assay for direct cAMP measurement (Gabriel et al., Assay and Drug Development Technologies, 1:291-303, 2003) and recombinant CHO-K1 cells stably transfected with S1P1. CHO-K1 cells were obtained from ATCC (Manassas, Va.; Catalog #CCL-61). The compound was determined to be an agonist of the S1P1 receptor and was detected in the HTRF assay for direct cAMP measurement as a compound which decreased cAMP concentration. The HTRF assay has been used to determine EC50 values for S1P1 receptor agonists.Principle of the assay: HTRF assay kit was purchased from Cisbio-US, Inc. (Bedford, Mass.; Catalog #62AM4PEC). The HTRF assay supported by the kit is a competitive immunoassay between endogenous cAMP produced by the CHO-K1 cells and tracer cAMP labeled with the dye d2.Homogeneous Time-Resolved Fluorescence (HTRF) Assay: The compound (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid was shown to be an agonist of the S1P1 receptor (e.g., human S1P1 receptor) using the HTRF assay for direct cAMP measurement (Gabriel et al., Assay and Drug Development Technologies, 1:291-303, 2003) and recombinant CHO-K1 cells stably transfected with S1P1. CHO-K1 cells were obtained from ATCC (Manassas, Va.; Catalog #CCL-61). The compound was determined to be an agonist of the S1P1 receptor and was detected in the HTRF assay for direct cAMP measurement as a compound which decreased cAMP concentration. The HTRF assay has been used to determine EC50 values for S1P1 receptor agonists.Principle of the assay: HTRF assay kit was purchased from Cisbio-US, Inc. (Bedford, Mass.; Catalog #62AM4PEC). The HTRF assay supported by the kit is a competitive immunoassay between endogenous cAMP produced by the CHO-K1 cells and tracer cAMP labeled with the dye d2.
471 6 1 3 7.0 COC(=O)CC1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL379380 s1pr1_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
431 7 1 6 4.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OCC(F)(F)F)c(C#N)c2)n1
CHEMBL3806205 s1pr1_human Human No 10.0 EC50 = 0.1 nM Bind
Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysisAgonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis
409 9 3 3 4.8 CCCCCC[C@@H]1CCC2=C(C1)C=CC(=C2)[C@H]3CC[C@@](C3)(COP(=O)(O)O)N
CHEMBL4637401 s1pr1_human Human No 10.0 EC50 = 0.1 nM Bind
Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysisAgonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis
459 8 3 4 4.5 COc1ccccc1CC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1
CHEMBL3806205 s1pr1_human Human No 9.9 EC50 = 0.1 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assayAgonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay
409 9 3 3 4.8 CCCCCC[C@@H]1CCC2=C(C1)C=CC(=C2)[C@H]3CC[C@@](C3)(COP(=O)(O)O)N
CHEMBL391869 s1pr1_human Human No 9.9 EC50 = 0.1 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
448 7 1 5 6.1 Cc1cc(C(C)CC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL3921214 s1pr1_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N(C)C)no2)cc1C#N
CHEMBL3991184 s1pr1_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N(C)C)no2)cc1C#N
CHEMBL3359520 s1pr1_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N
CHEMBL3403626 s1pr1_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
473 6 1 4 6.4 O=C(O)CC1OCCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12
CHEMBL190006 s1pr1_human Human Yes 9.9 EC50 = 0.1 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1
CHEMBL206940 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1
CHEMBL3359519 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
447 7 1 4 6.0 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C(F)(F)F
CHEMBL3359520 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N
CHEMBL3403636 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
520 6 1 4 7.0 CN1CCn2c(c(Cl)c3cc(OCc4ccc(C5CCCC5)c(C(F)(F)F)c4)ccc32)C1CC(=O)O
CHEMBL2057282 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
513 9 1 6 6.2 CCc1c(CCN2CCC(C(=O)O)CC2)cccc1-c1nsc(-c2ccc(OC(C)C)c(Cl)c2)n1
CHEMBL2032436 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
494 6 1 4 6.5 O=C(O)C1CCN(CCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1
CHEMBL3707247 s1pr1_human Human Yes 9.8 EC50 = 0.2 nM Funct
Agonist activity at S1P1 (unknown origin) expressed in CHO-K1 cells using CC4-AM as substrate assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 4 hrs followed by substrate addition and measured after 2 hrs by FRET assayAgonist activity at S1P1 (unknown origin) expressed in CHO-K1 cells using CC4-AM as substrate assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 4 hrs followed by substrate addition and measured after 2 hrs by FRET assay
404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C
CHEMBL3707247 s1pr1_human Human Yes 9.8 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor (unknown origin) assessed as reduction in forskolin-induced cAMP accumulation after 4 hrs by fluorescence assayAgonist activity at S1P1 receptor (unknown origin) assessed as reduction in forskolin-induced cAMP accumulation after 4 hrs by fluorescence assay
404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C
CHEMBL208718 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
405 7 1 5 5.3 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(CC(C)C)c(C#N)c2)s1
CHEMBL3707247 s1pr1_human Human Yes 9.8 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C
CHEMBL3919445 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CCC4O)no2)cc1OCC
CHEMBL3951270 s1pr1_human Human Yes 9.8 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
404 7 2 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCO)no2)cc1C#N
CHEMBL3902160 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
360 4 1 6 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N
CHEMBL3990889 s1pr1_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
360 4 1 6 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N
CHEMBL211046 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1ncc(-c2ccc(OC(C)C)c(C#N)c2)s1
CHEMBL3899384 s1pr1_human Human Yes 9.7 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N
CHEMBL4087932 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
450 9 1 5 4.7 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)n1
CHEMBL2059515 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
419 9 1 6 5.0 CCc1c(CCCC(=O)O)cccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL2018178 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3ccc4[nH]c(CCC(=O)O)cc4c3)no2)cc1Cl
CHEMBL225575 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
485 6 1 6 5.7 O=C(O)C1CN(Cc2ccc(-c3noc(-c4cc(-c5ccccc5)c(C(F)(F)F)s4)n3)cc2)C1
CHEMBL377767 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
407 7 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)s1
CHEMBL206940 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1
CHEMBL208898 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
380 7 1 5 4.8 Cc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C
CHEMBL1950574 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysisAgonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysis
461 7 2 5 5.3 C[C@@](N)(CCc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1)C(=O)O
CHEMBL225575 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
485 6 1 6 5.7 O=C(O)C1CN(Cc2ccc(-c3noc(-c4cc(-c5ccccc5)c(C(F)(F)F)s4)n3)cc2)C1
CHEMBL3753943 s1pr1_human Human No 9.7 EC50 = 0.2 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
459 6 2 7 4.4 Cc1cc(-c2nc(-c3cc(F)c(O[C@H]4CCC(=O)NC4)cc3Cl)no2)cc(NC(C)C)n1
CHEMBL3126605 s1pr1_human Human No 9.7 EC50 = 0.2 nM Bind
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assayAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assay
468 11 3 8 2.7 CCc1cc(-c2noc(-c3ccnc(CC(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3124957 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
496 12 3 8 3.7 CCc1cc(-c2noc(-c3cc(C)nc(C(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126585 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)nc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126587 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
510 13 3 8 4.0 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc(C(CC)CC)n1
CHEMBL3126605 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
468 11 3 8 2.7 CCc1cc(-c2noc(-c3ccnc(CC(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126611 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
482 11 3 8 3.0 CCc1cc(-c2noc(-c3cc(C)c(CC(C)C)cn3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126613 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)c(C4CCCC4)cn3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126615 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
497 12 3 9 2.7 CCc1cc(-c2noc(-c3cc(C)c(N(CC)CC)cn3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126619 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)cc(C4CCCC4)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126624 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
508 11 3 8 3.7 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cnc1C1CCCC1
CHEMBL3124957 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
496 12 3 8 3.7 CCc1cc(-c2noc(-c3cc(C)nc(C(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3799305 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
484 11 3 9 2.6 CCc1cc(-c2noc(-c3cc(C)nc(OC(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL4761456 s1pr1_human Human No 9.7 EC50 = 0.2 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
553 6 2 7 5.6 O=C(O)[C@H]1CCCN(CC(O)c2ccc3c(c2)CCc2c(-c4noc(-c5ccccc5)c4C(F)(F)F)noc2-3)C1
CHEMBL3793145 s1pr1_human Human No 9.7 EC50 = 0.2 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
445 8 1 8 3.9 CCCc1c(-c2ccccn2)noc1-c1nc(-c2ccc(CN3CC(C(=O)O)C3)cc2)no1
CHEMBL391870 s1pr1_human Human No 9.7 EC50 = 0.2 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
446 6 1 5 5.7 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL379310 s1pr1_human Human No 9.6 EC50 = 0.2 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
443 9 1 6 4.8 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(CF)CF)c(C#N)c2)s1
CHEMBL2048293 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1
CHEMBL3908750 s1pr1_human Human No 9.6 EC50 = 0.3 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
497 5 1 7 5.1 O=C(O)C1CN(Cc2ccc3c(c2)OCc2c-3noc2-c2onc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL2057283 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
485 9 1 6 5.4 CCc1c(CCN2CC(C(=O)O)C2)cccc1-c1nsc(-c2ccc(OC(C)C)c(Cl)c2)n1
CHEMBL2059686 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
505 8 1 6 5.8 CCc1c(CN2CC(C(=O)O)C2)cccc1-c1nsc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL2059688 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
519 9 1 6 5.8 CCc1c(CCN2CC(C(=O)O)C2)cccc1-c1nsc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL2018177 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3ccc4c(CCC(=O)O)c[nH]c4c3)no2)cc1Cl
CHEMBL2018306 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
460 7 2 6 5.1 CC(C)Oc1ncc(-c2nc(-c3cccc4c(CCC(=O)O)c[nH]c34)no2)cc1C(F)(F)F
CHEMBL3102904 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human S1P1R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P1R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
511 13 3 7 5.2 CCCCCCCCOc1ccc(-c2nnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F
CHEMBL4757149 s1pr1_human Human No 9.6 EC50 = 0.3 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
497 5 1 7 5.1 O=C(O)C1CN(Cc2ccc3c(c2)OCc2c-3noc2-c2noc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL3799701 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
458 9 1 7 4.9 CCCCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccc1
CHEMBL3794064 s1pr1_human Human Yes 9.6 EC50 = 0.3 nM Bind
Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 minsInduction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins
470 6 1 7 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1
CHEMBL209778 s1pr1_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
421 8 1 6 5.2 CCC(C)Oc1ccc(-c2nnc(-c3ccc(CCC(=O)O)cc3C)s2)cc1C#N
CHEMBL366208 s1pr1_human Human Yes 9.6 EC50 = 0.3 nM Bind
Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 minsInduction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL366208 s1pr1_rat Rat Yes 9.5 EC50 = 0.3 nM Funct
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS bindingAgonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL366208 s1pr1_rat Rat Yes 9.5 EC50 = 0.3 nM Funct
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL114606 s1pr1_human Human Yes 9.5 EC50 = 0.3 nM Funct
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL366208 s1pr1_human Human Yes 9.5 EC50 = 0.3 nM Funct
Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL314854 s1pr1_human Human Yes 9.5 EC50 = 0.3 nM Bind
Agonist activity at S1P1 receptor (unknown origin)Agonist activity at S1P1 receptor (unknown origin)
307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N
CHEMBL2207778 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
468 9 1 6 4.3 CCCCN(C(=O)c1ccccc1F)c1nnc(-c2ccc(CN3CC(C(=O)O)C3)cc2)s1
CHEMBL366208 s1pr1_human Human Yes 9.5 EC50 = 0.3 nM Funct
Agonist activity at SIP1 receptorAgonist activity at SIP1 receptor
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL1950572 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysisAgonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysis
447 7 2 5 4.9 N[C@H](CCc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1)C(=O)O
CHEMBL3400916 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
454 6 3 4 5.0 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(OC(F)(F)F)c(Cl)c3)cc21
CHEMBL3797951 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
424 9 1 7 4.1 CCCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1CC(C)C
CHEMBL2336064 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
494 10 2 4 6.4 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)c(F)c1
CHEMBL2336086 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
476 10 2 4 6.3 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)cc1
CHEMBL3126603 s1pr1_human Human No 9.5 EC50 = 0.3 nM Bind
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assayAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assay
454 10 3 8 2.6 CCc1cc(-c2noc(-c3ccnc(C(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126434 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
454 10 3 8 2.4 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc(C)n1
CHEMBL3126589 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
508 11 3 8 3.7 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc(C2CCCC2)n1
CHEMBL3126603 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
454 10 3 8 2.6 CCc1cc(-c2noc(-c3ccnc(C(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126608 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
511 13 3 9 2.9 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cnc1N(CC)CC
CHEMBL3797647 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
502 12 3 9 2.8 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)sc1CN(C)C
CHEMBL3797447 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.2 CCc1cc(-c2noc(-c3cnc(C4CCCC4)c(OC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3799872 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
498 12 3 9 2.7 CCc1cc(-c2noc(-c3cc(CC(C)C)nc(OC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3800120 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
496 11 3 9 2.8 CCc1cc(-c2noc(-c3cc(C)nc(OC4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3800133 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
496 11 3 9 2.8 CCc1cc(-c2noc(-c3cc(OC)nc(C4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL241050 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
448 7 1 5 5.8 Cc1cc(CC(C)C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1
CHEMBL3959509 s1pr1_rat Rat No 9.5 EC50 = 0.3 nM Bind
Agonist activity at rat S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at rat S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
495 5 1 6 5.3 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2onc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL391581 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL2018324 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
453 8 1 6 5.8 CCn1cc(CCC(=O)O)c2cccc(-c3noc(-c4ccc(OC(C)C)c(Cl)c4)n3)c21
CHEMBL2032311 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
454 8 1 4 6.8 O=C(O)CCCCCc1cnc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1
CHEMBL2032429 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
468 8 1 4 6.1 CN(CCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1)CC(=O)O
CHEMBL3358955 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12
CHEMBL3358920 h9euw9_macmu Rhesus macaque Yes 9.5 EC50 = 0.3 nM Funct
Agonist activity at monkey S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at monkey S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1
CHEMBL3358920 s1pr1_rat Rat Yes 9.5 EC50 = 0.3 nM Funct
Agonist activity at rat S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at rat S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1
CHEMBL3908750 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.
497 5 1 7 5.1 O=C(O)C1CN(Cc2ccc3c(c2)OCc2c-3noc2-c2onc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL4784344 s1pr1_human Human No 9.5 EC50 = 0.3 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
511 5 1 6 5.8 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2nsc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL4792990 s1pr1_human Human No 9.5 EC50 = 0.3 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
567 7 2 7 6.0 O=C(O)C[C@H]1CCCN(CC(O)c2ccc3c(c2)CCc2c(-c4noc(-c5ccccc5)c4C(F)(F)F)noc2-3)C1
CHEMBL3358920 w5vnf7_canlf Dog Yes 9.5 EC50 = 0.3 nM Funct
Agonist activity at dog S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at dog S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1
CHEMBL1091103 s1pr1_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assayAgonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay
413 12 4 4 3.5 CCCCCCCCc1ccc2c(c1)CC[C@@H](C(N)(CO)COP(=O)(O)O)C2
CHEMBL114606 s1pr1_human Human Yes 9.5 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL3931243 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
482 9 1 8 3.6 COCCS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL1935584 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
423 8 1 3 4.8 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OC[C@@H](C)Cc3ccc(F)cc3)ccc21
CHEMBL1963634 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
423 8 1 3 4.8 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OC[C@@H](C)Cc3ccc(F)cc3)ccc21
CHEMBL366208 s1pr1_human Human Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS bindingAgonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL366208 s1pr1_human Human Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL114606 s1pr1_human Human Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor by GTPgammaS binding assayAgonist activity at human S1P1 receptor by GTPgammaS binding assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL3800091 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
450 7 1 7 4.1 CC(C)Cc1onc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)c1C(F)(F)F
CHEMBL2018179 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
426 7 2 6 4.7 CC(C)Oc1ncc(-c2nc(-c3cccc4c(CCC(=O)O)c[nH]c34)no2)cc1Cl
CHEMBL2018318 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
439 8 2 5 5.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCCC(=O)O)c[nH]c34)no2)cc1Cl
CHEMBL2032318 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
453 8 1 3 7.4 O=C(O)CCCCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1
CHEMBL2032435 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
481 5 1 5 5.4 O=C(O)CN1CCN(c2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1
CHEMBL2032440 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
466 6 1 4 5.7 O=C(O)C1CN(CCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)C1
CHEMBL2011747 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assayAgonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assay
530 9 1 6 6.2 CCCCN(C(=O)c1ccc(C(F)(F)F)cc1)c1nnc(-c2ccc(CCC(=O)O)c3c2ccn3C)s1
CHEMBL211689 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
420 7 1 5 5.1 CCOc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F
CHEMBL366208 s1pr1_human Human Yes 9.4 EC50 = 0.4 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL2336071 s1pr1_human Human Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C
CHEMBL2336066 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
554 10 2 4 7.0 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)c(Br)c1
CHEMBL2336069 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
516 11 2 4 7.1 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)c(C2CC2)c1
CHEMBL4786296 s1pr1_human Human No 9.4 EC50 = 0.4 nM Bind
Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysisAgonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis
411 9 3 4 3.7 CCOCCC[C@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1
CHEMBL3121977 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
444 9 2 5 5.0 CCc1sc(C(=O)CCc2cc(C)c(OC[C@@H](O)CO)c(C)c2)c2c1CC(C)(C)CC2
CHEMBL3121978 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
472 11 2 5 5.8 CCc1sc(C(=O)CCc2cc(C)c(OC[C@@H](O)CO)c(C)c2)c2c1CC(CC)(CC)CC2
CHEMBL3121980 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
470 9 2 5 5.5 CCc1sc(C(=O)CCc2cc(C)c(OC[C@@H](O)CO)c(C)c2)c2c1CC1(CCCC1)CC2
CHEMBL3126435 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
468 11 3 8 2.8 CCCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc(C)n1
CHEMBL3126591 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
469 11 4 9 2.3 CCNc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc(C)n1
CHEMBL3800336 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
512 13 3 9 3.4 CCc1cc(-c2noc(-c3cc(OC)nc(C(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3707247 s1pr1_human Human Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at S1P1 receptor (unknown origin) after 120 mins in presence of [35S]-GTPgammaS by Topcount methodAgonist activity at S1P1 receptor (unknown origin) after 120 mins in presence of [35S]-GTPgammaS by Topcount method
404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C
CHEMBL3403622 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
473 6 2 3 6.5 O=C(O)CC1OCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL3358917 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
445 7 2 2 6.5 CC(C)Cc1ccc(COc2ccc3[nH]c4c(c3c2)CCC4CC(=O)O)cc1C(F)(F)F
CHEMBL3799693 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
444 8 1 7 4.5 CCCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccc1
CHEMBL3800257 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
444 8 1 7 4.5 CCCc1c(-c2ccccc2)noc1-c1nc(-c2ccc(CN3CC(C(=O)O)C3)cc2)no1
CHEMBL3102903 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human S1P1R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P1R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
510 13 3 6 5.9 CCCCCCCCOc1ccc(-c2cnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F
CHEMBL3358920 s1pr1_mouse Mouse Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at mouse S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at mouse S1P1 receptor assessed as cAMP accumulation by HTRF assay
457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1
CHEMBL241052 s1pr1_human Human No 9.4 EC50 = 0.4 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
392 7 1 7 3.8 Cc1nc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL3358913 s1pr1_human Human No 9.4 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
443 6 2 2 6.5 O=C(O)CC1CCc2c1[nH]c1ccc(OCc3ccc(C4CCC4)c(C(F)(F)F)c3)cc21
CHEMBL473269 s1pr1_human Human No 9.4 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding
443 13 4 5 4.2 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1F
CHEMBL391581 s1pr1_human Human No 9.4 EC50 = 0.5 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL3794064 s1pr1_human Human Yes 9.3 EC50 = 0.5 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
470 6 1 7 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1
CHEMBL3794064 s1pr1_human Human Yes 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
470 6 1 7 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1
CHEMBL3794064 s1pr1_human Human Yes 9.3 EC50 = 0.5 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
470 6 1 7 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1
CHEMBL3930827 s1pr1_human Human No 9.3 EC50 = 0.5 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
495 5 1 6 5.3 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2noc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL3403629 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
465 9 1 5 5.1 O=C(O)CC1OCCn2c1cc1cc(OCc3ccc(OC(CF)CF)c(Cl)c3)ccc12
CHEMBL3358915 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
431 7 2 2 6.2 CCCc1ccc(COc2ccc3[nH]c4c(c3c2)CCC4CC(=O)O)cc1C(F)(F)F
CHEMBL3359514 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
414 6 1 4 5.7 N#Cc1cc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)ccc1C1CCCC1
CHEMBL425563 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1
CHEMBL2207793 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
512 9 1 6 5.4 CCCCN(C(=O)c1ccccc1Cl)c1nnc(-c2cc(C)c(CN3CC(C(=O)O)C3)c(C)c2)s1
CHEMBL208168 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
390 6 1 4 5.8 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1
CHEMBL1950569 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysisAgonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysis
476 7 3 6 4.3 N[C@@H](CC(=O)O)C(=O)Nc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1
CHEMBL1950573 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysisAgonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysis
447 7 2 5 4.9 N[C@@H](CCc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1)C(=O)O
CHEMBL3892012 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
500 7 1 8 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCN(C)CC3)no2)cc1C#N
CHEMBL3894218 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
403 5 0 7 4.6 CC(=O)O[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3895985 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 7 1 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N(C)CCO)no2)cc1C#N
CHEMBL3897236 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
450 7 1 6 5.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCc3ccccc3)no2)cc1C#N
CHEMBL3898672 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
482 8 1 8 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N(CCO)S(C)(=O)=O)no2)cc1C#N
CHEMBL3900230 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
452 7 1 7 4.0 CCS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3901430 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
521 9 1 8 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CCCC3)no2)cc1C#N
CHEMBL3901636 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
538 9 1 9 4.2 COC(=O)C(C)(C)CS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3903701 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
443 7 1 7 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CC3)no2)cc1C#N
CHEMBL3903769 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
472 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@H](N)C3)no2)cc1C#N
CHEMBL3904131 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
507 9 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCN3CCC3)no2)cc1C#N
CHEMBL3908034 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
536 9 2 9 2.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CCNCC3)no2)cc1C#N
CHEMBL3908601 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
494 10 5 10 1.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC[C@@H](O)[C@H](O)[C@H](O)CO)no2)cc1C#N
CHEMBL3909636 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
390 4 1 5 4.8 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1C(F)(F)F
CHEMBL3909764 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
495 9 1 8 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCN(C)C)no2)cc1C#N
CHEMBL3910164 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
432 7 2 7 4.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC(C)(C)CO)no2)cc1C#N
CHEMBL3910562 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
430 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CC[C@H](O)C3)no2)cc1C#N
CHEMBL3910952 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
471 7 1 7 4.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)CN3CCCC3)no2)cc1C#N
CHEMBL3912865 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
500 6 1 7 4.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@H](N(C)C)C3)no2)cc1C#N
CHEMBL3913638 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
472 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@H](N)C3)no2)cc1C#N
CHEMBL3915059 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
459 7 0 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N(C)CC(=O)N(C)C)no2)cc1C#N
CHEMBL3915866 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
537 9 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCN3CC[C@H](O)C3)no2)cc1C#N
CHEMBL3916866 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
490 7 2 7 5.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCc3nc4ccccc4[nH]3)no2)cc1C#N
CHEMBL3917386 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
483 6 0 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(C(=O)N4CCC4)C3)no2)cc1C#N
CHEMBL3917838 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 8 0 7 4.5 CCN(CC(=O)N(C)C)[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3917848 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
404 4 1 5 5.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1C(F)(F)F
CHEMBL3918619 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
537 9 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCN3CC[C@@H](O)C3)no2)cc1C#N
CHEMBL3922297 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
444 6 1 7 4.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC3CCOCC3)no2)cc1C#N
CHEMBL3923599 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
500 6 1 7 4.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@H](N(C)C)C3)no2)cc1C#N
CHEMBL3923850 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
424 7 1 6 4.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(F)F)no2)cc1C#N
CHEMBL3923859 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
481 9 2 8 3.2 CNCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3924436 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
472 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@@H](N)C3)no2)cc1C#N
CHEMBL3926349 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
501 6 2 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCC(CO)CC3)no2)cc1C#N
CHEMBL3926357 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
500 6 1 7 4.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@@H](N(C)C)C3)no2)cc1C#N
CHEMBL3926589 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
480 8 1 7 4.6 CC(C)CS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3926935 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
485 7 1 7 4.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCCCC3)no2)cc1C#N
CHEMBL3927205 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
432 7 2 7 4.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(C)(C)O)no2)cc1C#N
CHEMBL3929478 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
367 5 1 7 3.7 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1[N+](=O)[O-]
CHEMBL3929906 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
459 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(C)C(=O)N(C)C)no2)cc1C#N
CHEMBL3932230 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
367 5 1 7 3.7 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1[N+](=O)[O-]
CHEMBL3932346 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
543 7 1 8 5.0 COC(=O)CC1CCN(C(=O)N[C@@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)CC1
CHEMBL3935123 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 8 2 7 3.9 CC(C)COc1ccc(-c2nc(-c3cccc4c3CCC4NCCO)no2)cc1C#N
CHEMBL3935588 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
346 4 1 6 3.6 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N
CHEMBL3937491 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
450 7 1 6 5.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCc3ccccc3)no2)cc1C#N
CHEMBL3938436 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
413 5 1 7 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1S(C)(=O)=O
CHEMBL3939061 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCC[C@H](O)C3)no2)cc1C#N
CHEMBL3940768 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCC(O)CC3)no2)cc1C#N
CHEMBL3941001 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
472 5 2 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCNCC3)no2)cc1C#N
CHEMBL3941503 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
551 9 2 9 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CCC(O)CC3)no2)cc1C#N
CHEMBL3941697 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
430 5 0 7 4.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCOCC3)no2)cc1C#N
CHEMBL3945024 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
457 7 2 6 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCO)no2)cc1Br
CHEMBL3947083 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
537 9 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CC[C@H](O)C3)no2)cc1C#N
CHEMBL3948795 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCC[C@@H](O)C3)no2)cc1C#N
CHEMBL3952397 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
388 5 0 6 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)C)no2)cc1C#N
CHEMBL3955110 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
446 7 1 7 3.9 CC(=O)N(CCO)[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3957013 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
500 7 1 7 5.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)c3ccccc3)no2)cc1C#N
CHEMBL3961112 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
537 9 1 9 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CCOCC3)no2)cc1C#N
CHEMBL3961448 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
514 8 1 7 5.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)Cc3ccccc3)no2)cc1C#N
CHEMBL3961775 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
457 8 1 7 4.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NCCN3CCCC3)no2)cc1C#N
CHEMBL3962124 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
454 7 2 7 4.9 Cc1cc(CN[C@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)[nH]n1
CHEMBL3963265 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
430 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CC[C@@H](O)C3)no2)cc1C#N
CHEMBL3968780 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
514 6 1 7 4.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(N(C)C)CC3)no2)cc1C#N
CHEMBL3969600 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 9 1 7 4.5 CCN(CC)C(=O)CN[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3969882 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@@H](C)O)no2)cc1C#N
CHEMBL3969945 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
454 7 2 7 4.9 Cc1c[nH]c(CN[C@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)n1
CHEMBL3970883 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
440 7 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCc3cnc[nH]3)no2)cc1C#N
CHEMBL3971247 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
529 7 2 7 4.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCC(CC(=O)O)CC3)no2)cc1C#N
CHEMBL3971447 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
429 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CC[C@H](N)C3)no2)cc1C#N
CHEMBL3971459 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
432 6 1 7 4.8 CCOC(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3972501 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
402 6 1 6 5.0 CC(C)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3972933 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
535 9 1 8 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CCCCC3)no2)cc1C#N
CHEMBL3974011 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
432 6 1 7 4.8 CCOC(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3977589 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
459 10 1 7 5.0 CCN(CC)CCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3980948 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
372 5 1 6 4.0 N#Cc1cc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)ccc1OCC1CC1
CHEMBL3981224 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 8 1 7 4.3 COCCN[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3982183 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
537 9 1 9 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCN3CCOCC3)no2)cc1C#N
CHEMBL3982194 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
473 8 1 8 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NCCN3CCOCC3)no2)cc1C#N
CHEMBL3985481 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N[C@@H](C)CO)no2)cc1C#N
CHEMBL3986043 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
500 6 1 7 4.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@@H](N(C)C)C3)no2)cc1C#N
CHEMBL3986508 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P1 expressed in CRE-bla CHOK1 cells assessed as inhibition of forskolin-induced cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
417 8 2 7 3.9 CNCCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21
CHEMBL3753602 s1pr1_human Human No 9.3 EC50 = 0.5 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
447 8 2 9 2.9 CC(C)Oc1ncc(-c2nc(-c3cc(F)c(OC[C@H](N)CO)cc3Cl)no2)cc1C#N
CHEMBL3754163 s1pr1_human Human No 9.3 EC50 = 0.5 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
427 7 2 8 3.6 Cc1cc(-c2nc(-c3ccc(OC[C@H]4COC(=O)N4)c(F)c3)no2)cc(NC(C)C)n1
CHEMBL3341785 s1pr1_human Human No 9.3 EC50 = 0.5 nM Bind
Agonist activity at human S1P1 receptor expressed in human EDG1-bla U2OS cells after 18 hrs by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in human EDG1-bla U2OS cells after 18 hrs by beta-arrestin recruitment assay
547 9 3 9 2.2 N[C@H](COc1cc(Cl)c(-c2nc(N3CCN(C(=O)C4CCCC4)CC3)no2)cc1F)COP(=O)(O)O
CHEMBL3344419 s1pr1_human Human No 9.3 EC50 = 0.5 nM Bind
Agonist activity at human S1P1 receptor expressed in human EDG1-bla U2OS cells after 18 hrs by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in human EDG1-bla U2OS cells after 18 hrs by beta-arrestin recruitment assay
483 7 2 8 2.5 N[C@@H](CO)COc1cc(Cl)c(-c2nnc(N3CCN(C(=O)C4CCCC4)CC3)s2)cc1F
CHEMBL3121966 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
487 10 3 8 3.7 Cc1cc(-c2noc(-c3sc(C)c(CC(C)C)c3C)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3121989 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
487 10 3 6 3.9 Cc1cc(CCC(=O)c2sc(C)c3c2CCC(C)(C)C3)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3126617 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
482 11 3 8 3.0 CCc1cc(-c2noc(-c3cc(C)cc(CC(C)C)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3798837 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
530 13 3 9 3.6 CCc1cc(-c2noc(-c3cc(C)c(CN(C)CC(C)C)s3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3799441 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
530 14 3 9 3.6 CCCN(C)Cc1sc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc1CC
CHEMBL2032438 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
508 7 1 4 6.9 O=C(O)C1CCCN(CCCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)C1
CHEMBL2048293 s1pr1_mouse Mouse No 9.3 EC50 = 0.5 nM Funct
Agonist activity against mouse S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against mouse S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1
CHEMBL514302 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding
422 11 4 5 2.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccccc2)cc1
CHEMBL475405 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Antagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation countingAntagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting
470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1
CHEMBL1089557 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
441 12 4 5 3.4 CCCCOc1ccc(-c2ccc(CCC(N)(CO)COP(=O)(O)O)cc2)c(F)c1
CHEMBL1199009 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
441 12 4 5 3.4 CCCCOc1ccc(-c2ccc(CCC(N)(CO)COP(=O)(O)O)cc2)c(F)c1
CHEMBL3798735 s1pr1_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
466 7 1 7 4.7 CC(F)(F)c1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccc1
CHEMBL225155 s1pr1_human Human Yes 9.3 EC50 = 0.6 nM Funct
Activity at human recombinant S1P1 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P1 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O
CHEMBL474689 s1pr1_human Human No 9.3 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding
425 13 4 5 4.1 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1
CHEMBL1935587 s1pr1_human Human No 9.3 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
439 8 1 3 5.3 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OC[C@@H](C)Cc3ccc(Cl)cc3)ccc21
CHEMBL1962536 s1pr1_human Human No 9.3 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
439 8 1 3 5.3 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OC[C@@H](C)Cc3ccc(Cl)cc3)ccc21
CHEMBL3797415 s1pr1_human Human No 9.3 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
458 8 1 7 4.8 CC(C)Cc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccc1
CHEMBL4782854 s1pr1_human Human No 9.2 EC50 = 0.6 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
511 5 1 6 5.8 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2snc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL4074505 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
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 methodAgonist 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
436 9 1 5 4.4 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)n1
CHEMBL4092538 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
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 methodAgonist 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
421 8 1 4 4.6 CCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1
CHEMBL2048296 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 1 7 5.1 N#Cc1cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)ccc1OC(F)(F)F
CHEMBL3959509 s1pr1_human Human No 9.2 EC50 = 0.6 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
495 5 1 6 5.3 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2onc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL3930827 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.
495 5 1 6 5.3 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2noc(-c3ccccc3)c2C(F)(F)F)C1
CHEMBL211228 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
447 7 1 6 5.0 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OCC(F)(F)F)c(C#N)c2)s1
CHEMBL1950568 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysisAgonist activity at eGFP-tagged human S1P1 receptor expressed in U2OS cells assessed as receptor internalization after 1 hr by Hoechst dye-based microscopic analysis
476 7 3 6 4.3 N[C@H](CC(=O)O)C(=O)Nc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1
CHEMBL1935579 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
405 8 1 3 5.0 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OCCC(C)c3ccccc3)ccc21
CHEMBL1963631 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
405 8 1 3 5.0 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OCCC(C)c3ccccc3)ccc21
CHEMBL3754018 s1pr1_human Human No 9.2 EC50 = 0.6 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
461 7 2 8 4.2 Cc1cc(-c2nc(-c3cc(F)c(OC[C@H]4COC(=O)N4)cc3Cl)no2)cc(NC(C)C)n1
CHEMBL2336065 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
510 10 2 4 6.9 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)c(Cl)c1
CHEMBL2336085 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
462 10 2 4 5.9 C/C(=N\OCc1ccc(C2CCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)cc1
CHEMBL4637401 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
459 8 3 4 4.5 COc1ccccc1CC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1
CHEMBL3121969 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
459 10 3 8 3.1 Cc1cc(-c2noc(-c3ccc(CC(C)C)s3)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3121995 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
515 12 3 6 4.4 CCc1cc(CCC(=O)c2sc(CC)c3c2CCC(C)(C)C3)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3105487 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
411 7 1 4 4.6 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OCC(N)=O
CHEMBL3126592 s1pr1_human Human Yes 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
497 12 3 9 2.7 CCc1cc(-c2noc(-c3cc(C)nc(N(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126592 s1pr1_human Human Yes 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
497 12 3 9 2.7 CCc1cc(-c2noc(-c3cc(C)nc(N(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3797940 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
516 13 3 9 3.3 CCCN(C)Cc1sc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc1C
CHEMBL3126592 s1pr1_human Human Yes 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
497 12 3 9 2.7 CCc1cc(-c2noc(-c3cc(C)nc(N(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3797626 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.2 CCc1cc(-c2noc(-c3cc(OC)nc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3799953 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.2 CCc1cc(-c2noc(-c3cc(OC)c(C4CCCC4)cn3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL2048298 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assay
442 6 1 7 5.0 CC(C)Oc1ccc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)cc1C#N
CHEMBL211826 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
419 8 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OCC3CC3)c(C#N)c2)s1
CHEMBL3359523 s1pr1_human Human No 9.2 EC50 = 0.6 nM Bind
Agonist activity at human S1P1 receptor by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor by beta-arrestin recruitment assay
481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F
CHEMBL1092577 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
457 12 4 5 3.9 CCCCOc1ccc(-c2ccc(CCC(N)(CO)COP(=O)(O)O)c(Cl)c2)cc1
CHEMBL3359522 s1pr1_human Human No 9.2 EC50 = 0.6 nM Bind
Agonist activity at human S1P1 receptor by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor by beta-arrestin recruitment assay
438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N
CHEMBL2032431 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
466 4 1 4 6.5 O=C(O)C1CCN(c2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1
CHEMBL3359519 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
447 7 1 4 6.0 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C(F)(F)F
CHEMBL1096210 s1pr1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
455 12 4 4 4.5 CCCCCc1ccc(-c2ccc(CCC(N)(CO)COP(=O)(O)O)c(Cl)c2)cc1
CHEMBL1935580 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
405 8 1 3 4.7 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OCC(C)Cc3ccccc3)ccc21
CHEMBL1962533 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
405 8 1 3 4.7 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OCC(C)Cc3ccccc3)ccc21
CHEMBL3403634 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
462 7 2 5 5.1 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCNC2CC(=O)O)cc1C(F)(F)F
CHEMBL190006 s1pr1_human Human Yes 9.2 EC50 = 0.7 nM Funct
Activity at human recombinant S1P1 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P1 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1
CHEMBL210695 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1
CHEMBL2336068 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
504 11 2 4 6.8 CCc1cc(/C(C)=N/OCc2ccc(C3CCCCC3)c(C(F)(F)F)c2)ccc1CNCCC(=O)O
CHEMBL366208 s1pr1_human Human Yes 9.2 EC50 = 0.7 nM Funct
Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N
CHEMBL3105248 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
440 6 2 7 4.4 Cc1cc(-c2nc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)no2)cc(C)c1OC[C@@H](O)CO
CHEMBL3105249 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
440 6 2 7 4.4 Cc1cc(-c2nnc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)o2)cc(C)c1OCC(O)CO
CHEMBL3126602 s1pr1_human Human No 9.2 EC50 = 0.7 nM Bind
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assayAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assay
454 11 3 8 2.5 CCCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)ccn1
CHEMBL3126602 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
454 11 3 8 2.5 CCCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)ccn1
CHEMBL3126626 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
473 11 3 8 3.4 CCc1cc(-c2noc(-c3ccc(CC(C)C)s3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3800591 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
530 14 3 9 3.7 CCCCN(C)Cc1sc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc1C
CHEMBL3797747 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.2 CCc1cc(-c2noc(-c3cc(OC)cc(C4CCCC4)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3800402 s1pr1_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.1 CCc1cc(-c2noc(-c3cnc(OC4CCCC4)c(C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL114606 s1pr1_human Human Yes 9.2 EC50 = 0.7 nM Funct
Agonist activity at recombinant human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL3794145 s1pr1_human Human No 9.2 EC50 = 0.7 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
471 6 1 8 4.0 O=C(O)C1CN(Cc2ccc(-c3noc(-c4onc(-c5ccccn5)c4C(F)(F)F)n3)cc2)C1
CHEMBL210695 s1pr1_human Human No 9.1 EC50 = 0.7 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1
CHEMBL3942289 s1pr1_human Human No 9.1 EC50 = 0.7 nM Funct
GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.
484 6 1 4 5.8 CC(C)Cc1ccc(-c2onc3c2CCc2cc(CN4CC(C(=O)O)C4)ccc2-3)cc1C(F)(F)F
CHEMBL3954922 s1pr1_human Human No 9.1 EC50 = 0.7 nM Funct
GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.
475 6 1 6 4.8 CC(C)Cc1onc(-c2onc3c2CCc2cc(CN4CC(C(=O)O)C4)ccc2-3)c1C(F)(F)F
CHEMBL2048287 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1
CHEMBL2048293 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1
CHEMBL3900885 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.
499 4 1 6 5.4 O=C(O)C1CN(c2cc3c(cc2F)-c2noc(-c4onc(-c5ccccc5)c4C(F)(F)F)c2CC3)C1
CHEMBL3092445 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Modulation of human S1P1 receptor assessed as increase in agonist-induced [35S]GTPgamma binding after 30 mins by cell-based beta counting analysisModulation of human S1P1 receptor assessed as increase in agonist-induced [35S]GTPgamma binding after 30 mins by cell-based beta counting analysis
545 14 3 3 7.5 Cc1ccc(CC(CCCSc2ccc(CNCCCP(=O)(O)O)cc2)c2cccc(Cl)c2)cc1C
CHEMBL378970 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
419 7 1 6 5.0 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC3CCC3)c(C#N)c2)s1
CHEMBL2057285 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
502 9 1 6 5.8 CCc1c(CCN2CCC(C(=O)O)CC2)cccc1-c1nsc(-c2ccc(CC(C)C)c(C#N)c2)n1
CHEMBL2057286 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
474 9 1 6 5.1 CCc1c(CCN2CC(C(=O)O)C2)cccc1-c1nsc(-c2ccc(CC(C)C)c(C#N)c2)n1
CHEMBL2032437 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
508 7 1 4 6.9 O=C(O)C1CCN(CCCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1
CHEMBL382739 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Binding potency at human S1P1 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P1 receptor by [35S]GTP-gamma-S binding assay
373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C
CHEMBL224005 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
461 7 1 4 5.8 Cc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1
CHEMBL3751872 s1pr1_human Human No 9.1 EC50 = 0.8 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
459 7 2 7 4.4 Cc1cc(-c2nc(-c3cc(F)c(OC[C@H]4CCC(=O)N4)cc3Cl)no2)cc(NC(C)C)n1
CHEMBL3753209 s1pr1_human Human No 9.1 EC50 = 0.8 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
459 6 2 7 4.4 Cc1cc(-c2nc(-c3cc(F)c(O[C@@H]4CCC(=O)NC4)cc3Cl)no2)cc(NC(C)C)n1
CHEMBL3754270 s1pr1_human Human No 9.1 EC50 = 0.8 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
450 8 2 7 4.3 Cc1cc(-c2nnc(-c3cc(F)c(OC[C@H](N)CO)cc3Cl)s2)cc(CC(C)C)n1
CHEMBL3754653 s1pr1_human Human No 9.1 EC50 = 0.8 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
448 6 2 8 3.9 Cc1cc(-c2nc(-c3cc(F)c(O[C@H]4COC[C@H]4O)cc3Cl)no2)cc(NC(C)C)n1
CHEMBL3102993 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
428 8 2 5 4.5 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OC[C@@H](O)CO
CHEMBL3126614 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
494 10 3 8 3.5 CCc1cc(-c2noc(-c3ccc(C4CCCC4)c(C)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL247766 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
403 6 1 6 4.6 Cc1cc([C@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL1096211 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
423 12 4 5 3.3 CCCCOc1ccc(-c2ccc(CCC(N)(CO)COP(=O)(O)O)cc2)cc1
CHEMBL3793185 s1pr1_human Human No 9.1 EC50 = 0.8 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
445 8 1 8 3.9 CCCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccn1
CHEMBL1916564 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
465 6 1 5 5.5 O=C(O)CCC(=O)N1CCc2cc(-c3noc(-c4ccc(C5CCCC5)c(Cl)c4)n3)ccc21
CHEMBL3403631 s1pr1_human Human No 9.1 EC50 = 0.8 nM Bind
Agonist activity at human S1P1 receptor by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor by beta-arrestin recruitment assay
454 7 1 6 5.1 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CCOC2CC(=O)O)cc1C#N
CHEMBL1935576 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
409 8 1 3 4.6 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OCCCc3ccc(F)cc3)ccc21
CHEMBL1963630 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
409 8 1 3 4.6 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OCCCc3ccc(F)cc3)ccc21
CHEMBL1090819 s1pr1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
491 11 4 5 4.5 NC(CO)(CCc1ccc(-c2ccc(SCc3ccccc3)cc2F)cc1)COP(=O)(O)O
CHEMBL1084929 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
373 13 3 4 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)COP(=O)(O)O)cc1
CHEMBL1935583 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
423 8 1 3 4.8 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OC[C@H](C)Cc3ccc(F)cc3)ccc21
CHEMBL1963633 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
423 8 1 3 4.8 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OC[C@H](C)Cc3ccc(F)cc3)ccc21
CHEMBL4758827 s1pr1_human Human No 9.1 EC50 = 0.9 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
509 5 1 6 5.6 Cc1cc2c(cc1CN1CC(C(=O)O)C1)CCc1c-2noc1-c1noc(-c2ccccc2)c1C(F)(F)F
CHEMBL2207791 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
484 9 1 6 4.8 CCCCN(C(=O)c1ccccc1Cl)c1nnc(-c2ccc(CN3CC(C(=O)O)C3)cc2)s1
CHEMBL209567 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
401 7 1 5 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C(F)(F)C(C)C)cn2)n1
CHEMBL3806205 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
409 9 3 3 4.8 CCCCCC[C@@H]1CCC2=C(C1)C=CC(=C2)[C@H]3CC[C@@](C3)(COP(=O)(O)O)N
CHEMBL3121971 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
445 10 3 8 2.9 CCCc1ccc(-c2nc(-c3cc(C)c(OCC(O)CNC(=O)CO)c(C)c3)no2)s1
CHEMBL3121985 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
499 10 3 8 3.6 CCc1cc(-c2noc(-c3sc(CC)c4c3CCCC4)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3105483 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
469 10 2 5 4.7 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OCCCNC(=O)CO
CHEMBL3126596 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C4CCCC4)cc(C)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126621 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
496 12 3 8 3.7 CCc1cc(-c2noc(-c3cnc(C(CC)CC)c(C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3800086 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
488 11 3 9 2.6 CCc1cc(-c2noc(-c3cc(C)c(CN(C)C)s3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3806205 s1pr1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at recombinant human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
409 9 3 3 4.8 CCCCCC[C@@H]1CCC2=C(C1)C=CC(=C2)[C@H]3CC[C@@](C3)(COP(=O)(O)O)N
CHEMBL225155 s1pr1_human Human Yes 9.1 EC50 = 0.9 nM Bind
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O
CHEMBL3806205 s1pr1_human Human No 9.0 EC50 = 0.9 nM Funct
Agonist activity at human S1P1 receptor by GTPgammaS binding assayAgonist activity at human S1P1 receptor by GTPgammaS binding assay
409 9 3 3 4.8 CCCCCC[C@@H]1CCC2=C(C1)C=CC(=C2)[C@H]3CC[C@@](C3)(COP(=O)(O)O)N
CHEMBL377181 s1pr1_human Human No 9.0 EC50 = 0.9 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1ccc(-c2ccc(OC(C)C)c(C#N)c2)s1
CHEMBL391581 s1pr1_human Human No 9.0 EC50 = 0.9 nM Funct
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL380040 s1pr1_human Human No 9.0 EC50 = 1.0 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-n1nnc(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL4750972 s1pr1_human Human No 9.0 EC50 = 1.0 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
510 5 1 4 6.7 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2ccc(C3CCCCC3)c(C(F)(F)F)c2)C1
CHEMBL3800349 s1pr1_human Human No 9.0 EC50 = 1.0 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
470 6 1 7 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4noc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1
CHEMBL3798784 s1pr1_human Human No 9.0 EC50 = 1.0 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
478 7 1 7 5.2 O=C(O)C1CN(Cc2ccc(-c3noc(-c4noc(-c5ccccc5)c4-c4ccccc4)n3)cc2)C1
CHEMBL2057232 s1pr1_human Human Yes 9.0 EC50 = 1 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
429 9 1 5 5.4 CCc1c(CCCC(=O)O)cccc1-c1cnc(-c2ccc(OC(C)C)c(C#N)c2)nc1
CHEMBL2207790 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
450 9 1 6 4.2 CCCCN(C(=O)c1ccccc1)c1nnc(-c2ccc(CN3CC(C(=O)O)C3)cc2)s1
CHEMBL2032433 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
480 5 1 4 6.4 O=C(O)CN1CCC(c2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1
CHEMBL4776597 s1pr1_human Human No 9.0 EC50 = 1 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
496 5 1 7 4.7 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2onc(-c3ccccn3)c2C(F)(F)F)C1
CHEMBL1951154 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgamma binding
433 7 1 7 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(Oc5ccccc5)cc4)n3)s2)C1
CHEMBL4279752 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]GTPgammaS binding assay
496 11 3 7 4.2 CCCCOCCOc1nc2c(s1)-c1ccc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)cc1CC2
CHEMBL3793394 s1pr1_human Human No 9.0 EC50 = 1 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
445 7 1 8 4.1 CC(C)c1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccn1
CHEMBL4085321 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
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 methodAgonist 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
449 9 1 4 5.2 COc1cc(CC(C)C)ccc1COc1ccc2c(c1)CCC(CN1CC(C(=O)O)C1)=C2C
CHEMBL4093489 s1pr1_human Human Yes 9.0 EC50 = 1 nM Funct
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 methodAgonist 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
435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1
CHEMBL1916409 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
443 3 0 5 5.3 COc1ccc2c(c1)CCN(c1noc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)n1)C2
CHEMBL1916570 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
477 7 1 7 4.1 COc1ccc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)cc1OC(F)(F)F
CHEMBL3105250 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
439 6 2 6 5.0 Cc1cc(-c2cnc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)o2)cc(C)c1OCC(O)CO
CHEMBL3126586 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
508 10 3 8 3.9 CCc1cc(-c2noc(-c3cc(C)nc(C4CCCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126633 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
482 11 3 8 3.0 CCc1cc(-c2noc(-c3cnc(CC(C)C)c(C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3797596 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
524 14 3 8 3.5 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)ccc1CN(CC)CC
CHEMBL3799718 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
510 13 3 8 3.1 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)ccc1CN(C)CC
CHEMBL3800019 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.1 CCc1cc(-c2noc(-c3cc(C)nc(OC4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3800028 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.1 CCc1cc(-c2noc(-c3cc(C)cc(OC4CCCC4)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL1916399 s1pr1_rat Rat No 9.0 EC50 = 1 nM Funct
Agonist activity at rat S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at rat S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
472 6 1 7 3.9 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)c1
CHEMBL3605517 s1pr1_human Human No 9.0 EC50 = 1 nM Bind
Antagonist activity against human S1P1 receptor expressed in human U2OS cells co-expressing GFP assessed as inhibition of S1P-induced receptor translocationAntagonist activity against human S1P1 receptor expressed in human U2OS cells co-expressing GFP assessed as inhibition of S1P-induced receptor translocation
415 5 1 4 4.5 CCn1c([C@@H](C)NS(=O)(=O)c2ccc(Cl)cc2)nc2cc(F)c(Cl)cc21
CHEMBL199791 s1pr1_human Human Yes 9.0 EC50 = 1 nM Funct
Binding potency at human S1P1 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P1 receptor by [35S]GTP-gamma-S binding assay
337 14 4 4 2.9 CCCCCCCCCC/C=C/[C@@H](O)[C@@H](N)COP(=O)(O)O
CHEMBL371758 s1pr1_human Human No 9.0 EC50 = 1 nM Funct
Binding potency at human S1P1 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P1 receptor by [35S]GTP-gamma-S binding assay
607 21 4 10 5.9 C[C@@](N)(CCc1ccc(OCCCCCCCCCCCNc2ccc([N+](=O)[O-])c3nonc23)cc1)COP(=O)(O)O
CHEMBL2048287 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1
CHEMBL211081 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)o1
CHEMBL444799 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
429 8 1 6 4.7 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OCC(F)F)c(C#N)c2)s1
CHEMBL2207792 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
498 9 1 6 5.1 CCCCN(C(=O)c1ccccc1Cl)c1nnc(-c2ccc(CN3CC(C(=O)O)C3)cc2C)s1
CHEMBL212580 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
396 8 1 6 4.5 COc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C
CHEMBL3359521 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
459 8 1 4 6.0 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(OCC4CC4)c(C(F)(F)F)c3)ccc12
CHEMBL473238 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding
484 11 4 5 4.1 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCc2ccc(-c3ccccc3)cc2)cc1
CHEMBL515921 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding
420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1F
CHEMBL2022905 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor by [S35]GTPgammaS binding assayAgonist activity at human S1P1 receptor by [S35]GTPgammaS binding assay
484 10 1 6 6.4 CCCc1cc(-c2cnc(-c3sc(CN4CC(C(=O)O)C4)cc3CC)s2)ccc1OC(C)C
CHEMBL4473672 s1pr1_human Human No 9.0 EC50 = 1.1 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cell membranes measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes measured after 45 mins by [35S]GTP-gammaS binding assay
548 8 2 8 5.7 O=C(O)C[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4noc(C5CCCCC5)c4C(F)(F)F)n3)cc2)C1
CHEMBL1935585 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
437 9 1 3 5.2 CC[C@H](COc1ccc2c(c1)CCC(CN1CC(C(=O)O)C1)=C2C)Cc1ccc(F)cc1
CHEMBL1962534 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium levelAgonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of intracellular calcium level
437 9 1 3 5.2 CC[C@H](COc1ccc2c(c1)CCC(CN1CC(C(=O)O)C1)=C2C)Cc1ccc(F)cc1
CHEMBL1951588 s1pr1_human Human Yes 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS bindingAgonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
422 11 3 5 3.3 Cc1ccc(CCCC(=O)c2ccc(CC[C@@](C)(N)COP(=O)(O)O)n2C)cc1
CHEMBL1951588 s1pr1_human Human Yes 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
422 11 3 5 3.3 Cc1ccc(CCCC(=O)c2ccc(CC[C@@](C)(N)COP(=O)(O)O)n2C)cc1
CHEMBL1916569 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
446 7 1 7 3.8 CC(C)Oc1cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)ccc1C#N
CHEMBL1092272 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
475 11 4 5 3.8 NC(CO)(CCc1ccc(-c2ccc(OCc3ccccc3)cc2F)cc1)COP(=O)(O)O
CHEMBL1095889 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
363 11 4 4 2.3 CCCCCc1ccc(CCC(N)(CO)COP(=O)(O)O)c(F)c1
CHEMBL3121979 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
442 9 2 5 4.7 CCc1sc(C(=O)CCc2cc(C)c(OC[C@@H](O)CO)c(C)c2)c2c1CC1(CC2)CC1
CHEMBL3121987 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
525 10 3 8 4.0 CCc1cc(-c2noc(-c3sc(CC)c4c3CCC3(CC3)C4)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3102985 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
469 11 2 5 5.2 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OCCCNCC(=O)O
CHEMBL3102988 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
438 7 1 4 5.8 Cc1sc(C(=O)CCc2cc(Cl)c(OCCO)c(Cl)c2)c2c1[C@H]1[C@@H](C2)C1(C)C
CHEMBL3105247 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
440 6 2 7 4.4 Cc1cc(-c2noc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)n2)cc(C)c1OC[C@@H](O)CO
CHEMBL3799355 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
552 14 3 8 4.3 CCc1cc(-c2noc(-c3cc(CN(C)CC(C)C)cc(C(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3799888 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
538 14 3 8 3.8 CCc1cc(CN(C)CC(C)C)cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)c1
CHEMBL3797486 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
512 13 3 9 3.4 CCc1cc(-c2noc(-c3cc(C(CC)CC)cc(OC)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3798969 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
524 12 3 9 3.4 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc(OC2CCCC2)n1
CHEMBL3799580 s1pr1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 12 3 9 3.0 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cc(OC2CCC2)n1
CHEMBL1916399 s1pr1_mouse Mouse No 9.0 EC50 = 1.1 nM Funct
Agonist activity at mouse S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at mouse S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
472 6 1 7 3.9 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)c1
CHEMBL4579553 s1pr1_human Human Yes 8.9 EC50 = 1.2 nM Bind
Activation of human recombinant S1P1 expressed in CHO cell membranes after 120 mins by GTP-gamma-35S-binding assayActivation of human recombinant S1P1 expressed in CHO cell membranes after 120 mins by GTP-gamma-35S-binding assay
455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1
CHEMBL114606 s1pr1_human Human Yes 8.9 EC50 = 1.2 nM Funct
Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL3403620 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
487 6 2 3 6.7 CC1(CC(=O)O)OCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL3403619 s1pr1_human Human Yes 8.9 EC50 = 1.2 nM Bind
Agonist activity at human S1P1 receptor by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor by beta-arrestin recruitment assay
472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL4458575 s1pr1_human Human No 8.9 EC50 = 1.2 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO cell membranes measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes measured after 45 mins by [35S]GTP-gammaS binding assay
542 8 2 8 5.3 O=C(O)C[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1
CHEMBL4087932 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
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 methodAgonist 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
450 9 1 5 4.7 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)n1
CHEMBL4095920 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
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 methodAgonist 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
449 9 1 4 5.3 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1
CHEMBL1916399 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
472 6 1 7 3.9 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)c1
CHEMBL1916558 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
470 5 2 5 5.3 O=C(O)CCc1nc2cc(-c3noc(-c4cc(C(F)(F)F)cc(C(F)(F)F)c4)n3)ccc2[nH]1
CHEMBL1089558 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
459 12 4 5 3.5 CCCCOc1cc(F)c(-c2ccc(CCC(N)(CO)COP(=O)(O)O)cc2)cc1F
CHEMBL3344412 s1pr1_human Human No 8.9 EC50 = 1.2 nM Bind
Agonist activity at human S1P1 receptor expressed in human EDG1-bla U2OS cells after 18 hrs by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in human EDG1-bla U2OS cells after 18 hrs by beta-arrestin recruitment assay
481 7 2 8 2.5 N[C@@H](CO)COc1cc(Cl)c(-c2nc(N3CCN(C(=O)C4CCCCC4)CC3)no2)cc1F
CHEMBL3105484 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
485 10 3 6 3.6 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3121990 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
501 12 3 6 4.8 Cc1cc(CCC(=O)c2sc(C)c3c2CCC(C)(C)C3)cc(C)c1OCC(O)CNCCC(=O)O
CHEMBL3121994 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
501 11 3 6 4.1 CCc1cc(CCC(=O)c2sc(C)c3c2CCC(C)(C)C3)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3800001 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
512 13 3 9 3.4 CCc1cc(-c2noc(-c3cc(OC)cc(C(CC)CC)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3911661 s1pr1_human Human No 8.9 EC50 = 1.2 nM Funct
GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.
404 6 1 5 4.4 CCCc1ccc(-c2onc3c2COc2cc(CN4CC(C(=O)O)C4)ccc2-3)cc1
CHEMBL2059516 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
435 9 1 6 5.5 CCc1c(CCCC(=O)O)cccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)s1
CHEMBL2059518 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
435 9 1 6 5.5 CCc1c(CCCC(=O)O)cccc1-c1nc(-c2ccc(OC(C)C)c(C#N)c2)ns1
CHEMBL2059671 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
433 9 1 5 5.9 CCc1c(CCCC(=O)O)cccc1-c1nsc(-c2ccc(CC(C)C)c(C#N)c2)n1
CHEMBL2032432 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
480 5 1 4 6.9 O=C(O)CC1CCN(c2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1
CHEMBL1836171 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells expressing beta-arrestin 2 after 105 mins by chemi-luminescence assayAgonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells expressing beta-arrestin 2 after 105 mins by chemi-luminescence assay
489 8 2 8 3.2 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(CC(=O)N[C@@H](C)CO)C2
CHEMBL2011736 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assayAgonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assay
556 11 2 7 4.4 CCCCN(C(=O)c1ccc(C(F)(F)F)cc1)c1nnc(-c2ccc(S(=O)(=O)NCCC(=O)O)cc2)s1
CHEMBL2011739 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assayAgonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assay
444 6 1 4 6.2 CCCCN(C(=O)c1ccc(C(F)(F)F)cc1)c1nnc(-c2cccc3[nH]ccc23)s1
CHEMBL224853 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
475 7 1 4 6.1 Cc1cc(CN2CC(C(=O)O)C2)cc(C)c1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1
CHEMBL389880 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
465 7 1 4 5.7 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(F)c2)C1
CHEMBL114606 s1pr1_human Human Yes 8.9 EC50 = 1.3 nM Funct
Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL2207779 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
482 9 1 6 4.7 CCCCN(C(=O)c1ccccc1F)c1nnc(-c2ccc(CN3CCC(C(=O)O)C3)cc2)s1
CHEMBL3942289 s1pr1_human Human No 8.9 EC50 = 1.3 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
484 6 1 4 5.8 CC(C)Cc1ccc(-c2onc3c2CCc2cc(CN4CC(C(=O)O)C4)ccc2-3)cc1C(F)(F)F
CHEMBL4747682 s1pr1_human Human No 8.9 EC50 = 1.3 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
495 5 1 6 5.3 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c(-c4onc(-c5ccccc5)c4C(F)(F)F)noc2-3)C1
CHEMBL4757437 s1pr1_human Human No 8.9 EC50 = 1.3 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
473 5 1 6 4.7 CC1(c2onc(-c3onc4c3CCc3cc(CN5CC(C(=O)O)C5)ccc3-4)c2C(F)(F)F)CC1
CHEMBL2022906 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human S1P1 receptor by [S35]GTPgammaS binding assayAgonist activity at human S1P1 receptor by [S35]GTPgammaS binding assay
484 9 1 6 6.5 CCc1cc(CN2CC(C(=O)O)C2)sc1-c1ncc(-c2ccc(OC(C)C)c(C(C)C)c2)s1
CHEMBL3800513 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
444 7 1 7 4.7 CC(C)c1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccc1
CHEMBL1916565 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
513 6 1 6 5.9 O=C(O)CCC(=O)N1CCc2cc(-c3noc(-c4ccc(-c5cccs5)c(C(F)(F)F)c4)n3)ccc21
CHEMBL1091630 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
441 12 4 5 3.4 CCCCOc1ccc(-c2ccc(CCC(N)(CO)COP(=O)(O)O)cc2)cc1F
CHEMBL3121996 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
529 13 3 6 4.8 CCCc1sc(C(=O)CCc2cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c2)c2c1CC(C)(C)CC2
CHEMBL3121997 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
555 11 3 6 4.8 CCc1cc(CCC(=O)c2sc(C(F)(F)F)c3c2CCC(C)(C)C3)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3121998 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
517 12 3 7 3.8 CCc1cc(CCC(=O)c2sc(OC)c3c2CCC(C)(C)C3)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3105478 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
497 8 3 8 3.5 Cc1cc(-c2noc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3105484 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
485 10 3 6 3.6 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3126597 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
497 12 3 9 2.7 CCc1cc(-c2noc(-c3cc(C)cc(N(CC)CC)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126618 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
482 11 3 8 3.0 CCc1cc(-c2noc(-c3cc(CC(C)C)cc(C)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3797412 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
502 12 3 9 2.9 CCc1cc(-c2noc(-c3cc(C)c(CN(C)CC)s3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3799916 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysisAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount analysis
496 12 3 8 2.7 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)ccc1CN(C)C
CHEMBL1916559 s1pr1_rat Rat No 8.9 EC50 = 1.3 nM Funct
Agonist activity at rat S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at rat S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
499 5 1 5 5.2 O=C(O)CCC(=O)N1CCc2cc(-c3noc(-c4cc(C(F)(F)F)cc(C(F)(F)F)c4)n3)ccc21
CHEMBL114606 s1pr1_human Human Yes 8.9 EC50 = 1.3 nM Bind
Effective concentration against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assay
387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N
CHEMBL3946363 s1pr1_human Human No 8.9 EC50 = 1.3 nM Funct
GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.
404 6 1 5 4.4 CCCc1ccc(-c2noc3c2COc2cc(CN4CC(C(=O)O)C4)ccc2-3)cc1
CHEMBL224571 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
481 7 1 4 6.2 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1
CHEMBL375488 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
475 8 1 4 6.1 CCc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1
CHEMBL2048287 s1pr1_rat Rat No 8.9 EC50 = 1.4 nM Funct
Agonist activity against rat S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against rat S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1
CHEMBL3403621 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
471 6 2 2 7.3 O=C(O)CC1CCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21
CHEMBL4071753 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
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 methodAgonist 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
407 7 1 4 4.3 COc1cc(C)ccc1COc1ccc2c(c1)CCC(CN1CC(C(=O)O)C1)=C2C
CHEMBL3752968 s1pr1_human Human No 8.9 EC50 = 1.4 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
423 7 1 8 3.5 Cc1cc(-c2nc(-c3cnc(OC[C@H]4COC(=O)N4)c(C)c3)no2)cc(CC(C)C)n1
CHEMBL2336061 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
477 10 2 5 5.7 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)cn1
CHEMBL3105478 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
497 8 3 8 3.5 Cc1cc(-c2noc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3121961 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
511 11 2 7 5.9 CCc1cc(-c2noc(-c3sc(CC)c4c3CCC(C)(C)C4)n2)cc(C)c1OCCNCCC(=O)O
CHEMBL3103656 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
428 8 2 5 4.5 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OC[C@H](O)CO
CHEMBL3103658 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
397 7 1 4 5.1 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OCCN
CHEMBL3798690 s1pr1_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.2 CCc1cc(-c2noc(-c3ccc(C4CCCC4)c(OC)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL1916559 s1pr1_mouse Mouse No 8.9 EC50 = 1.4 nM Funct
Agonist activity at mouse S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at mouse S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
499 5 1 5 5.2 O=C(O)CCC(=O)N1CCc2cc(-c3noc(-c4cc(C(F)(F)F)cc(C(F)(F)F)c4)n3)ccc21
CHEMBL1093429 s1pr1_human Human No 8.8 EC50 = 1.4 nM Funct
Antagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation countingAntagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting
538 10 4 5 4.8 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(C(F)(F)F)c1
CHEMBL3954922 s1pr1_human Human No 8.8 EC50 = 1.5 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
475 6 1 6 4.8 CC(C)Cc1onc(-c2onc3c2CCc2cc(CN4CC(C(=O)O)C4)ccc2-3)c1C(F)(F)F
CHEMBL3970572 s1pr1_human Human No 8.8 EC50 = 1.5 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
486 6 1 5 5.4 CC(C)Oc1ccc(-c2onc3c2CCc2cc(CN4CC(C(=O)O)C4)ccc2-3)cc1C(F)(F)F
CHEMBL3359520 s1pr1_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N
CHEMBL1916568 s1pr1_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
459 8 1 7 3.8 COc1cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)ccc1OC(F)F
CHEMBL3121967 s1pr1_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
473 10 3 8 3.4 Cc1cc(-c2noc(-c3scc(CC(C)C)c3C)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3121968 s1pr1_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
473 10 3 8 3.4 Cc1cc(-c2noc(-c3cc(CC(C)C)c(C)s3)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3122000 s1pr1_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
513 9 3 8 4.0 CCc1cc(-c2noc(-c3sc(C)c4c3CCC(C)(C)C4)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3105481 s1pr1_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
485 11 3 6 4.2 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(C)c1OCC(O)CNCC(=O)O
CHEMBL3797365 s1pr1_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
498 12 3 9 2.7 CCc1cc(-c2noc(-c3cc(OC)cc(CC(C)C)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3799227 s1pr1_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDPAgonist activity at human recombinant S1PR1 expressed in CHO cell membranes incubated for 30 mins by [35S]GTPgammaS binding assay in presence of GDP
510 11 3 9 3.2 CCc1cc(-c2noc(-c3cnc(OC)c(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL1951304 s1pr1_rat Rat Yes 8.8 EC50 = 1.5 nM Funct
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS bindingAgonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
461 8 1 7 5.3 CCc1cc(CN2CC(C(=O)O)C2)sc1-c1noc(-c2ccc(Oc3ccccc3)cc2)n1
CHEMBL2059527 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
427 9 1 3 6.6 CCc1c(CCCC(=O)O)cccc1-c1ccc(-c2ccc(OC(C)C)c(C#N)c2)cc1
CHEMBL2018307 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
406 7 2 6 4.4 Cc1cc(-c2nc(-c3cccc4c(CCC(=O)O)c[nH]c34)no2)cnc1OC(C)C
CHEMBL3769933 s1pr1_human Human No 8.8 EC50 = 1.6 nM Bind
Agonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells by beta-arrestin recruitment assay
461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C
CHEMBL2010813 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assayAgonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assay
550 9 1 6 6.8 CCCCN(C(=O)c1ccc(C(F)(F)F)cc1)c1nnc(-c2cccc3c2c(Cl)cn3CCC(=O)O)s1
CHEMBL210345 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-c1nnn(-c2ccc(OC(C)C)c(C#N)c2)n1
CHEMBL2207784 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
466 8 1 6 3.9 O=C(O)C1CN(Cc2ccc(-c3nnc(N(CC4CC4)C(=O)c4ccccc4F)s3)cc2)C1
CHEMBL1088177 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P1 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
443 7 2 6 3.2 Cc1cc(S(N)(=O)=O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1
CHEMBL4758481 s1pr1_human Human No 8.8 EC50 = 1.6 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
561 7 2 8 4.0 CS(=O)(=O)CCNC(=O)C(O)c1ccc2c(c1)CCc1c(-c3noc(-c4ccccc4)c3C(F)(F)F)noc1-2
CHEMBL4763970 s1pr1_human Human No 8.8 EC50 = 1.6 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
510 5 1 7 5.1 CN1Cc2c(noc2-c2onc(-c3ccccc3)c2C(F)(F)F)-c2ccc(CN3CC(C(=O)O)C3)cc21
CHEMBL4764300 s1pr1_human Human No 8.8 EC50 = 1.6 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
513 5 1 6 5.4 O=C(O)C1CN(Cc2cc3c(cc2F)-c2noc(-c4noc(-c5ccccc5)c4C(F)(F)F)c2CC3)C1
CHEMBL4793933 s1pr1_human Human No 8.8 EC50 = 1.6 nM Bind
Agonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting methodAgonist activity at human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgamma-S binding measured after 45 mins by liquid scintillation counting method
448 8 1 6 4.4 CCOc1ccc(-c2onc3c2CCc2cc(CN4CC(C(=O)O)C4)ccc2-3)cc1OCC
CHEMBL3800595 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
430 7 1 7 4.1 CCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccc1
CHEMBL1090223 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
491 11 4 5 4.3 NC(CO)(CCc1ccc(-c2ccc(OCc3ccccc3)cc2)cc1Cl)COP(=O)(O)O
CHEMBL2336070 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assayAgonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
502 8 1 4 6.5 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CN2CC(C(=O)O)C2)c(C)c1
CHEMBL3121964 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
499 8 3 8 3.8 Cc1cc(-c2noc(-c3sc(C)c4c3CCC(C)(C)C4)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3121981 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
430 9 2 5 4.6 CCc1sc(C(=O)CCc2cc(C)c(OCC(O)CO)c(C)c2)c2c1CC(C)CC2
CHEMBL1093823 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Antagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation countingAntagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting
547 9 4 5 5.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1
CHEMBL1916563 s1pr1_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assayAgonist activity at human S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
514 5 2 6 4.1 N[C@@H](CC(=O)N1CCc2cc(-c3noc(-c4cc(C(F)(F)F)cc(C(F)(F)F)c4)n3)ccc21)C(=O)O
CHEMBL3358906 s1pr1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assayAgonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay
430 6 2 4 5.0 N#Cc1cc(COc2ccc3[nH]c4c(c3c2)CCC4CC(=O)O)ccc1OC(F)(F)F
CHEMBL3403628 s1pr1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
420 7 1 6 4.4 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCOC2CC(=O)O)cc1C#N
CHEMBL3403635 s1pr1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assayAgonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
493 6 1 6 5.1 CN1CCn2c(c(Cl)c3cc(OCc4cc(C#N)cc(OC(F)(F)F)c4)ccc32)C1CC(=O)O
CHEMBL3799276 s1pr1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assayAgonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
416 6 1 7 3.9 Cc1c(-c2ccccc2)noc1-c1nc(-c2ccc(CN3CC(C(=O)O)C3)cc2)no1
CHEMBL4093077 s1pr1_human Human No 8.8 EC50 = 1.7 nM Funct
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 methodAgonist 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
417 7 1 3 4.9 CC1=C(CN2CC(C(=O)O)C2)CCc2cc(OCCC3CCc4ccccc43)ccc21
CHEMBL3344410 s1pr1_human Human No 8.8 EC50 = 1.7 nM Bind
Agonist activity at human S1P1 receptor expressed in human EDG1-bla U2OS cells after 18 hrs by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in human EDG1-bla U2OS cells after 18 hrs by beta-arrestin recruitment assay
467 7 2 8 2.1 N[C@@H](CO)COc1cc(Cl)c(-c2nc(N3CCN(C(=O)C4CCCC4)CC3)no2)cc1F
CHEMBL3121999 s1pr1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
499 9 3 8 3.7 CCc1cc(-c2noc(-c3scc4c3CCC(C)(C)C4)n2)cc(C)c1OCC(O)CNC(=O)CO
CHEMBL3909064 s1pr1_human Human No 8.8 EC50 = 1.7 nM Funct
GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.GTPgammaS Binding Assay: Compounds were loaded in a 384 Falcon v-bottom plate (0.5 ul/well in a 11 point, 3-fold dilution). Membranes prepared from S1P1/CHO cells or EDG3-Ga15-bla HEK293T cells were added to the compound plate (40 ul/well, final protein 3 ug/well) with multidrop. [35S]GTP (1250 Ci/mmol, Perkin Elmer) was diluted in assay buffer: 20 mM HEPES, pH7.5, 10 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 1 mM DTT, 10 uM GDP, 0.1% fatty acid free BSA, and 10 ug/ml Saponin to 0.4 nM. 40 ul of the [35S] GTP solution was added to the compound plate with a final concentration of 0.2 nM. The reaction was kept at room temperature for 45 min. At the end of incubation, all the mixtures in the compound plate were transferred to Millipore 384-well FB filter plates via the Velocity11 Vprep liquid handler. The filter plate was washed with water 4 times by using the manifold Embla plate washer and dried at 60° C. for 45 min. MicroScint 20 scintillation fluid (30 u) was added to each well.
520 5 2 7 5.0 N#CC1(NC(=O)C(O)c2ccc3c(c2)CCc2c-3noc2-c2noc(-c3ccccc3)c2C(F)(F)F)CC1
CHEMBL2048287 s1pr1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against human S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1
CHEMBL1093686 s1pr1_human Human No 8.8 EC50 = 1.8 nM Funct
Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@H]([C@@](C)(N)COP(=O)(O)O)C2
CHEMBL2048287 s1pr1_rat Rat No 8.7 EC50 = 1.8 nM Funct
Agonist activity against rat S1P1 assessed as accumulation of cAMP by HTRF assayAgonist activity against rat S1P1 assessed as accumulation of cAMP by HTRF assay
468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1
CHEMBL1092284 s1pr1_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilizationAgonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
457 10 4 5 4.2 Cc1ccc(Oc2ccc(-c3ccc(CCC(N)(CO)COP(=O)(O)O)cc3)cc2)cc1
CHEMBL3121975 s1pr1_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as membrane-bound 35S-GTPgammaS incubated 30 mins prior to substrate addition measured after 1 hr by topcount scintillation counting analysis
529 10 3 9 3.7 CCc1cc(-c2noc(-c3sc(OC)c4c3CCC(C)(C)C4)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3102989 s1pr1_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
418 7 1 4 5.5 Cc1cc(CCC(=O)c2sc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc(Cl)c1OCCO
CHEMBL3126604 s1pr1_human Human No 8.7 EC50 = 1.8 nM Bind
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assayAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to 35SGTP-gammaS addition measured after 1 hr by 35SGTP-gammaS binding assay
468 12 3 8 2.9 CCCCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)ccn1
CHEMBL3126604 s1pr1_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
468 12 3 8 2.9 CCCCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)ccn1
CHEMBL1951588 s1pr1_rat Rat Yes 8.7 EC50 = 1.8 nM Funct
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS bindingAgonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
422 11 3 5 3.3 Cc1ccc(CCCC(=O)c2ccc(CC[C@@](C)(N)COP(=O)(O)O)n2C)cc1
CHEMBL1951588 s1pr1_rat Rat Yes 8.7 EC50 = 1.8 nM Funct
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
422 11 3 5 3.3 Cc1ccc(CCCC(=O)c2ccc(CC[C@@](C)(N)COP(=O)(O)O)n2C)cc1
CHEMBL210038 s1pr1_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding
431 6 1 6 5.8 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(-c3cccs3)c(C#N)c2)s1
CHEMBL380253 s1pr1_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
384 7 1 5 4.7 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(F)c2)n1
CHEMBL3752339 s1pr1_human Human No 8.7 EC50 = 1.9 nM Bind
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
419 8 2 5 5.1 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H](C)N[C@H]4C[C@@H](C(=O)O)C4)cc3)no2)cc1
CHEMBL3126593 s1pr1_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
495 10 3 9 2.4 CCc1cc(-c2noc(-c3cc(C)nc(N4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO
CHEMBL3126634 s1pr1_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P1 receptor expressed in CHO cells incubated for 30 mins prior to [35S]-GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
482 11 3 8 3.0 CCc1cc(-c2noc(-c3cnc(CC(C)C)c(C)c3)n2)cc(C)c1OC[C@H](O)CNC(=O)CO
CHEMBL1091103 s1pr1_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human S1P1 receptor assess