Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

24986380 74957 0 None - 1 Human 11.0 pEC50 = 11 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 425 7 1 6 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3ccn4CCC(=O)O)no2)cc1Cl 10.1016/j.bmcl.2012.04.095
CHEMBL2032300 74957 0 None - 1 Human 11.0 pEC50 = 11 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 425 7 1 6 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3ccn4CCC(=O)O)no2)cc1Cl 10.1016/j.bmcl.2012.04.095
11452022 3596 39 None -1 6 Human 10.9 pEC50 = 10.9 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2010.02.006
6996 3596 39 None -1 6 Human 10.9 pEC50 = 10.9 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2010.02.006
CHEMBL366208 3596 39 None -1 6 Human 10.9 pEC50 = 10.9 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2010.02.006
44547315 73667 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCC(=O)O)c[nH]c34)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
CHEMBL2018176 73667 0 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCC(=O)O)c[nH]c34)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
57522815 76444 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 493 10 2 6 5.5 CCc1c(CCNCC(=O)O)cccc1-c1nsc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1021/jm2016107
CHEMBL2059683 76444 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 493 10 2 6 5.5 CCc1c(CCNCC(=O)O)cccc1-c1nsc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1021/jm2016107
46884020 8440 0 None 8 4 Human 10.7 pEC50 = 10.7 Functional
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
ChEMBL 397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@H]([C@@](C)(N)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
CHEMBL1093686 8440 0 None 8 4 Human 10.7 pEC50 = 10.7 Functional
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
ChEMBL 397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@H]([C@@](C)(N)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
57522939 76445 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 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 10.1021/jm2016107
CHEMBL2059684 76445 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 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 10.1021/jm2016107
53362086 116355 0 None -2 7 Human 10.7 pEC50 = 10.7 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
CHEMBL3359523 116355 0 None -2 7 Human 10.7 pEC50 = 10.7 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
67250226 116354 0 None -3 7 Human 10.6 pEC50 = 10.6 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359522 116354 0 None -3 7 Human 10.6 pEC50 = 10.6 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
70696401 74958 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 459 7 1 6 5.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3c(Cl)cn4CCC(=O)O)no2)cc1Cl 10.1016/j.bmcl.2012.04.095
CHEMBL2032301 74958 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 459 7 1 6 5.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3c(Cl)cn4CCC(=O)O)no2)cc1Cl 10.1016/j.bmcl.2012.04.095
10883396 3649 45 None -1 15 Human 10.6 pEC50 = 10.6 Functional
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
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.006
5283560 3649 45 None -1 15 Human 10.6 pEC50 = 10.6 Functional
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
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.006
911 3649 45 None -1 15 Human 10.6 pEC50 = 10.6 Functional
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
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.006
CHEMBL225155 3649 45 None -1 15 Human 10.6 pEC50 = 10.6 Functional
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
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.006
11502996 158727 42 None -5 3 Human 10.6 pEC50 = 10.6 Functional
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
ChEMBL 435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
CHEMBL4093489 158727 42 None -5 3 Human 10.6 pEC50 = 10.6 Functional
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
ChEMBL 435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
11502996 158727 42 None 5 3 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL 435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
CHEMBL4093489 158727 42 None 5 3 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL 435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
44412971 138934 0 None 102 3 Human 10.5 pEC50 = 10.5 Functional
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
ChEMBL 445 7 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL378436 138934 0 None 102 3 Human 10.5 pEC50 = 10.5 Functional
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
ChEMBL 445 7 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
49839234 117951 1 None -3 8 Human 10.5 pEC50 = 10.5 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
CHEMBL3403619 117951 1 None -3 8 Human 10.5 pEC50 = 10.5 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
70681258 73685 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 424 7 2 5 4.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCC(N)=O)c[nH]c34)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
CHEMBL2018320 73685 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 424 7 2 5 4.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCC(N)=O)c[nH]c34)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
70694325 74973 0 None 7943 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 454 8 2 4 5.8 O=C(O)CNCCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.04.095
CHEMBL2032428 74973 0 None 7943 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 454 8 2 4 5.8 O=C(O)CNCCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.04.095
70681687 74975 0 None 6309 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 454 8 2 4 5.8 O=C(O)CCNCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.04.095
CHEMBL2032430 74975 0 None 6309 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 454 8 2 4 5.8 O=C(O)CCNCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.04.095
53235481 151142 0 None -6 3 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human S1P1 assessed as stimulation of cAMP accumulationAgonist activity at human S1P1 assessed as stimulation of cAMP accumulation
ChEMBL 495 5 1 6 5.3 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2onc(-c3ccccc3)c2C(F)(F)F)C1 10.1021/acs.jmedchem.6b01099
CHEMBL3959509 151142 0 None -6 3 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human S1P1 assessed as stimulation of cAMP accumulationAgonist activity at human S1P1 assessed as stimulation of cAMP accumulation
ChEMBL 495 5 1 6 5.3 O=C(O)C1CN(Cc2ccc3c(c2)CCc2c-3noc2-c2onc(-c3ccccc3)c2C(F)(F)F)C1 10.1021/acs.jmedchem.6b01099
67250226 116354 0 None 1 7 Rhesus macaque 10.4 pEC50 = 10.4 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359522 116354 0 None 1 7 Rhesus macaque 10.4 pEC50 = 10.4 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
70683347 73686 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 438 7 2 5 5.0 CNC(=O)CCc1c[nH]c2c(-c3noc(-c4ccc(OC(C)C)c(Cl)c4)n3)cccc12 10.1016/j.bmcl.2012.02.083
CHEMBL2018321 73686 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 438 7 2 5 5.0 CNC(=O)CCc1c[nH]c2c(-c3noc(-c4ccc(OC(C)C)c(Cl)c4)n3)cccc12 10.1016/j.bmcl.2012.02.083
70695743 73186 0 None 39810 2 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 516 9 1 6 6.1 CCCCN(C(=O)c1ccc(C(F)(F)F)cc1)c1nnc(-c2cccc3c2ccn3CCC(=O)O)s1 10.1016/j.bmcl.2012.02.016
CHEMBL2011746 73186 0 None 39810 2 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 516 9 1 6 6.1 CCCCN(C(=O)c1ccc(C(F)(F)F)cc1)c1nnc(-c2cccc3c2ccn3CCC(=O)O)s1 10.1016/j.bmcl.2012.02.016
49839234 117951 1 None -1 8 Dog 10.4 pEC50 = 10.4 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
CHEMBL3403619 117951 1 None -1 8 Dog 10.4 pEC50 = 10.4 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
44623998 1596 38 None -3 8 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 10.1021/ml500389m
9331 1596 38 None -3 8 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 10.1021/ml500389m
CHEMBL3358920 1596 38 None -3 8 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 10.1021/ml500389m
DB14766 1596 38 None -3 8 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 10.1021/ml500389m
49872506 117606 1 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 419 7 3 5 4.1 CC(C)Oc1ccc(COc2ccc3[nH]c4c(c3c2)CCNC4CC(=O)O)cc1C#N 10.1016/j.bmcl.2014.11.089
CHEMBL3400909 117606 1 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 419 7 3 5 4.1 CC(C)Oc1ccc(COc2ccc3[nH]c4c(c3c2)CCNC4CC(=O)O)cc1C#N 10.1016/j.bmcl.2014.11.089
49872600 117607 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 460 7 3 3 5.6 CC(C)Cc1ccc(COc2ccc3[nH]c4c(c3c2)CCNC4CC(=O)O)cc1C(F)(F)F 10.1016/j.bmcl.2014.11.089
CHEMBL3400910 117607 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 460 7 3 3 5.6 CC(C)Cc1ccc(COc2ccc3[nH]c4c(c3c2)CCNC4CC(=O)O)cc1C(F)(F)F 10.1016/j.bmcl.2014.11.089
49873101 117963 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 497 7 1 5 6.2 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CCOC2CC(=O)O)cc1C(F)(F)F 10.1016/j.bmcl.2014.11.089
CHEMBL3403630 117963 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 497 7 1 5 6.2 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CCOC2CC(=O)O)cc1C(F)(F)F 10.1016/j.bmcl.2014.11.089
49873102 117964 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 454 7 1 6 5.1 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CCOC2CC(=O)O)cc1C#N 10.1016/j.bmcl.2014.11.089
CHEMBL3403631 117964 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 454 7 1 6 5.1 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CCOC2CC(=O)O)cc1C#N 10.1016/j.bmcl.2014.11.089
49872980 117965 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 507 6 1 4 7.1 O=C(O)CC1OCCn2c1c(Cl)c1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1016/j.bmcl.2014.11.089
CHEMBL3403632 117965 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 507 6 1 4 7.1 O=C(O)CC1OCCn2c1c(Cl)c1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1016/j.bmcl.2014.11.089
49839234 117951 1 None 1 8 Rat 10.4 pEC50 = 10.4 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
CHEMBL3403619 117951 1 None 1 8 Rat 10.4 pEC50 = 10.4 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
46174905 116288 0 None 162 3 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
CHEMBL3358955 116288 0 None 162 3 Human 10.4 pEC50 = 10.4 Functional
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
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
67250226 116354 0 None -1 7 Dog 10.3 pEC50 = 10.3 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359522 116354 0 None -1 7 Dog 10.3 pEC50 = 10.3 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
53362086 116355 0 None 1 7 Dog 10.3 pEC50 = 10.3 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
CHEMBL3359523 116355 0 None 1 7 Dog 10.3 pEC50 = 10.3 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
52938549 142599 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 406 7 1 6 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCF)no2)cc1C#N nan
CHEMBL3891354 142599 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 406 7 1 6 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCF)no2)cc1C#N nan
58344550 142847 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCOCC3)no2)cc1C#N nan
CHEMBL3893180 142847 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCOCC3)no2)cc1C#N nan
58344711 142944 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 417 6 2 7 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)CN)no2)cc1C#N nan
CHEMBL3894084 142944 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 417 6 2 7 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)CN)no2)cc1C#N nan
67194420 143012 0 None 645 4 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCO)no2)cc1C#N nan
CHEMBL3894716 143012 0 None 645 4 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCO)no2)cc1C#N nan
68300617 143143 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 431 7 2 7 3.4 CNC(=O)CN[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3895822 143143 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 431 7 2 7 3.4 CNC(=O)CN[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
58344764 143153 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 448 9 2 8 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N(CCO)CCO)no2)cc1C#N nan
CHEMBL3895901 143153 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 448 9 2 8 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N(CCO)CCO)no2)cc1C#N nan
52939914 143230 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 446 8 1 8 4.2 COC(=O)CCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3896496 143230 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 446 8 1 8 4.2 COC(=O)CCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
58344591 143301 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 374 5 1 6 4.3 CN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3897106 143301 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 374 5 1 6 4.3 CN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
58344549 143561 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 501 6 2 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(CO)CC3)no2)cc1C#N nan
CHEMBL3899152 143561 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 501 6 2 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(CO)CC3)no2)cc1C#N nan
58344646 143625 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 416 5 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(O)C3)no2)cc1C#N nan
CHEMBL3899733 143625 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 416 5 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(O)C3)no2)cc1C#N nan
58344748 143658 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
CHEMBL3899952 143658 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
52939289 143951 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 402 7 1 6 5.0 CCCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3902406 143951 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 402 7 1 6 5.0 CCCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
58344635 144023 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCOCC3)no2)cc1C#N nan
CHEMBL3902939 144023 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCOCC3)no2)cc1C#N nan
58344612 144284 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 471 6 0 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(C(=O)N(C)C)C3)no2)cc1C#N nan
CHEMBL3905058 144284 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 471 6 0 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(C(=O)N(C)C)C3)no2)cc1C#N nan
58344524 144368 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 431 5 1 6 4.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N(C)C)no2)cc1C#N nan
CHEMBL3905765 144368 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 431 5 1 6 4.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N(C)C)no2)cc1C#N nan
52938927 144438 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 457 7 1 7 3.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCC3)no2)cc1C#N nan
CHEMBL3906427 144438 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 457 7 1 7 3.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCC3)no2)cc1C#N nan
52938803 144549 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 444 5 1 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCC(O)CC3)no2)cc1C#N nan
CHEMBL3907353 144549 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 444 5 1 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCC(O)CC3)no2)cc1C#N nan
52939528 144571 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 7 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCN(CCO)CC3)no2)cc1C#N nan
CHEMBL3907543 144571 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 7 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCN(CCO)CC3)no2)cc1C#N nan
58344665 145009 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 472 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@@H](N)C3)no2)cc1C#N nan
CHEMBL3910977 145009 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 472 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@@H](N)C3)no2)cc1C#N nan
58344709 145273 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 551 8 1 9 2.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CCOCC3)no2)cc1C#N nan
CHEMBL3912931 145273 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 551 8 1 9 2.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CCOCC3)no2)cc1C#N nan
58344522 145544 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 404 4 1 5 5.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C(F)(F)F nan
CHEMBL3915065 145544 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 404 4 1 5 5.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C(F)(F)F nan
58344718 145782 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 434 8 3 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@H](O)CO)no2)cc1C#N nan
CHEMBL3916821 145782 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 434 8 3 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@H](O)CO)no2)cc1C#N nan
58344716 145935 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N[C@@H](C)CO)no2)cc1C#N nan
CHEMBL3918031 145935 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N[C@@H](C)CO)no2)cc1C#N nan
52939412 145957 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 5 1 7 4.4 COC(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3918159 145957 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 5 1 7 4.4 COC(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
89788823 145976 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 511 11 3 9 2.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCNCCO)no2)cc1C#N nan
CHEMBL3918328 145976 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 511 11 3 9 2.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCNCCO)no2)cc1C#N nan
58344498 146003 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 8 1 7 4.3 COCCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3918503 146003 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 8 1 7 4.3 COCCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
52939784 146156 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 430 5 0 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CCOC3=O)no2)cc1C#N nan
CHEMBL3919810 146156 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 430 5 0 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CCOC3=O)no2)cc1C#N nan
52938806 146174 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 347 4 1 6 3.7 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1C#N nan
CHEMBL3919920 146174 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 347 4 1 6 3.7 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1C#N nan
58344846 146179 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@H](O)C3)no2)cc1C#N nan
CHEMBL3919959 146179 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@H](O)C3)no2)cc1C#N nan
58344556 146292 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)CN(C)C)no2)cc1C#N nan
CHEMBL3920863 146292 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)CN(C)C)no2)cc1C#N nan
52939414 146296 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 5 1 7 4.4 COC(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3920889 146296 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 5 1 7 4.4 COC(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
52938925 146522 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 347 4 1 6 3.7 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C#N nan
CHEMBL3922629 146522 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 347 4 1 6 3.7 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C#N nan
52939658 146716 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 434 8 3 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@@H](O)CO)no2)cc1C#N nan
CHEMBL3924073 146716 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 434 8 3 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@@H](O)CO)no2)cc1C#N nan
134141745 146749 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 420 7 2 8 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N(CO)CO)no2)cc1C#N nan
CHEMBL3924318 146749 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 420 7 2 8 3.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N(CO)CO)no2)cc1C#N nan
52939654 146821 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 448 7 2 8 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)OCCO)no2)cc1C#N nan
CHEMBL3924832 146821 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 448 7 2 8 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)OCCO)no2)cc1C#N nan
58344783 146977 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 432 7 1 7 3.8 COCC(=O)NC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3926299 146977 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 432 7 1 7 3.8 COCC(=O)NC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
52939166 147011 9 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 402 5 1 6 4.2 CC(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3926586 147011 9 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 402 5 1 6 4.2 CC(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
52939657 147034 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 403 7 2 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NCCN)no2)cc1C#N nan
CHEMBL3926787 147034 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 403 7 2 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NCCN)no2)cc1C#N nan
58344864 147097 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 7 2 8 3.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CC[C@@H](O)C3)no2)cc1C#N nan
CHEMBL3927322 147097 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 7 2 8 3.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CC[C@@H](O)C3)no2)cc1C#N nan
58344898 147436 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 7 2 8 3.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CC[C@H](O)C3)no2)cc1C#N nan
CHEMBL3930042 147436 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 7 2 8 3.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CC[C@H](O)C3)no2)cc1C#N nan
58344894 147503 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 7 1 8 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCOCC3)no2)cc1C#N nan
CHEMBL3930528 147503 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 7 1 8 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCOCC3)no2)cc1C#N nan
58344883 147653 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@@H](O)C3)no2)cc1C#N nan
CHEMBL3931604 147653 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@@H](O)C3)no2)cc1C#N nan
58344542 147676 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCCS(C)(=O)=O)no2)cc1C#N nan
CHEMBL3931785 147676 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCCS(C)(=O)=O)no2)cc1C#N nan
58344586 148000 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 529 7 2 7 4.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(CC(=O)O)CC3)no2)cc1C#N nan
CHEMBL3934309 148000 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 529 7 2 7 4.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(CC(=O)O)CC3)no2)cc1C#N nan
58344819 148020 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCS(C)(=O)=O)no2)cc1C#N nan
CHEMBL3934482 148020 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCS(C)(=O)=O)no2)cc1C#N nan
52939655 148026 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 430 5 0 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CCOC3=O)no2)cc1C#N nan
CHEMBL3934530 148026 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 430 5 0 7 4.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CCOC3=O)no2)cc1C#N nan
58344685 148087 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
CHEMBL3935065 148087 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
58344814 148220 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
CHEMBL3936105 148220 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
58344901 148427 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 444 6 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(C(=O)O)C3)no2)cc1C#N nan
CHEMBL3937763 148427 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 444 6 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N3CC(C(=O)O)C3)no2)cc1C#N nan
58344763 148466 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 515 6 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(C(=O)O)CC3)no2)cc1C#N nan
CHEMBL3938039 148466 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 515 6 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(C(=O)O)CC3)no2)cc1C#N nan
58344841 148500 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 472 5 2 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCNCC3)no2)cc1C#N nan
CHEMBL3938278 148500 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 472 5 2 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCNCC3)no2)cc1C#N nan
52938305 148578 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 481 9 2 8 3.2 CNS(=O)(=O)CCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3939008 148578 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 481 9 2 8 3.2 CNS(=O)(=O)CCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
52938424 148731 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 429 5 1 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCNCC3)no2)cc1C#N nan
CHEMBL3940245 148731 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 429 5 1 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4N3CCNCC3)no2)cc1C#N nan
58344644 148764 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 471 6 0 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CC(C(=O)N(C)C)C3)no2)cc1C#N nan
CHEMBL3940511 148764 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 471 6 0 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CC(C(=O)N(C)C)C3)no2)cc1C#N nan
52938928 148912 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 471 7 1 7 4.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCCC3)no2)cc1C#N nan
CHEMBL3941756 148912 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 471 7 1 7 4.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N3CCCC3)no2)cc1C#N nan
58344790 149055 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 432 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)CC(=O)O)no2)cc1C#N nan
CHEMBL3942853 149055 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 432 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)CC(=O)O)no2)cc1C#N nan
58344871 149186 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 432 6 1 7 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)C(=O)CO)no2)cc1C#N nan
CHEMBL3943755 149186 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 432 6 1 7 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)C(=O)CO)no2)cc1C#N nan
52939916 149307 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 446 8 1 8 4.2 CC(=O)OCCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3944842 149307 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 446 8 1 8 4.2 CC(=O)OCCNC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
58344622 149352 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 482 8 2 8 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)O)no2)cc1C#N nan
CHEMBL3945226 149352 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 482 8 2 8 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)O)no2)cc1C#N nan
52939169 149636 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 406 7 1 6 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCCF)no2)cc1C#N nan
CHEMBL3947288 149636 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 406 7 1 6 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCCF)no2)cc1C#N nan
58344707 149656 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 495 9 1 8 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN(C)C)no2)cc1C#N nan
CHEMBL3947411 149656 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 495 9 1 8 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN(C)C)no2)cc1C#N nan
68300608 149662 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 457 6 1 7 3.7 CNC(=O)C1CN([C@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)C1 nan
CHEMBL3947465 149662 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 457 6 1 7 3.7 CNC(=O)C1CN([C@H]2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)C1 nan
89788777 149946 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 537 9 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CC[C@@H](O)C3)no2)cc1C#N nan
CHEMBL3949785 149946 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 537 9 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CC[C@@H](O)C3)no2)cc1C#N nan
58344551 150228 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 438 6 1 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(C)(=O)=O)no2)cc1C#N nan
CHEMBL3952253 150228 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 438 6 1 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(C)(=O)=O)no2)cc1C#N nan
134144722 150448 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 446 8 1 7 4.2 CCOCC(=O)NC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3954097 150448 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 446 8 1 7 4.2 CCOCC(=O)NC1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
58344650 150479 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 537 8 2 9 2.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CC(O)C3)no2)cc1C#N nan
CHEMBL3954350 150479 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 537 8 2 9 2.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CC(O)C3)no2)cc1C#N nan
58344892 150555 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@@H](O)C3)no2)cc1C#N nan
CHEMBL3954873 150555 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC[C@@H](O)C3)no2)cc1C#N nan
58344509 150573 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 1 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)CCO)no2)cc1C#N nan
CHEMBL3955035 150573 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 1 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N(C)CCO)no2)cc1C#N nan
52938804 150885 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1OCC nan
CHEMBL3957449 150885 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@H]4O)no2)cc1OCC nan
58344675 150893 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@H](O)C3)no2)cc1C#N nan
CHEMBL3957491 150893 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 473 5 2 7 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC[C@H](O)C3)no2)cc1C#N nan
58344887 150921 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 432 8 1 7 4.4 CCN(CCO)[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3957713 150921 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 432 8 1 7 4.4 CCN(CCO)[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
58344619 150967 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC[C@@H](O)C3)no2)cc1C#N nan
CHEMBL3958210 150967 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC[C@@H](O)C3)no2)cc1C#N nan
52938805 151241 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1OCC nan
CHEMBL3960138 151241 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1OCC nan
52939168 151289 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 424 7 1 6 4.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCC(F)F)no2)cc1C#N nan
CHEMBL3960551 151289 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 424 7 1 6 4.9 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCC(F)F)no2)cc1C#N nan
52938180 151546 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 464 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)C3CC3)no2)cc1C#N nan
CHEMBL3963066 151546 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 464 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)C3CC3)no2)cc1C#N nan
58344567 151666 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 416 5 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CC(O)C3)no2)cc1C#N nan
CHEMBL3964002 151666 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 416 5 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N3CC(O)C3)no2)cc1C#N nan
58344770 151670 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 515 6 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCC(C(=O)O)CC3)no2)cc1C#N nan
CHEMBL3964055 151670 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 515 6 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CCC(C(=O)O)CC3)no2)cc1C#N nan
89787335 151764 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 507 9 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CCC3)no2)cc1C#N nan
CHEMBL3964817 151764 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 507 9 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CCC3)no2)cc1C#N nan
52938548 151833 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 402 5 3 6 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=N)N)no2)cc1C#N nan
CHEMBL3965400 151833 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 402 5 3 6 3.5 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=N)N)no2)cc1C#N nan
52939288 151841 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 374 5 1 6 4.3 CN[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3965441 151841 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 374 5 1 6 4.3 CN[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
68300855 152027 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 461 9 3 8 2.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)NCCO)no2)cc1C#N nan
CHEMBL3967098 152027 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 461 9 3 8 2.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)NCCO)no2)cc1C#N nan
52938053 152028 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 457 7 1 8 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCc3cncs3)no2)cc1C#N nan
CHEMBL3967100 152028 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 457 7 1 8 5.3 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCc3cncs3)no2)cc1C#N nan
89788838 152144 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 523 9 2 9 2.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CC(O)C3)no2)cc1C#N nan
CHEMBL3968024 152144 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 523 9 2 9 2.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCN3CC(O)C3)no2)cc1C#N nan
58344664 152268 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 390 4 1 5 4.8 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C(F)(F)F nan
CHEMBL3969165 152268 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 390 4 1 5 4.8 CCOc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4O)no2)cc1C(F)(F)F nan
58344540 152321 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)CN(C)C)no2)cc1C#N nan
CHEMBL3969712 152321 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)CN(C)C)no2)cc1C#N nan
58344876 152429 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 565 8 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CCC(O)CC3)no2)cc1C#N nan
CHEMBL3970705 152429 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 565 8 2 9 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N3CCC(O)CC3)no2)cc1C#N nan
58344660 152444 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@H](C)O)no2)cc1C#N nan
CHEMBL3970830 152444 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NC[C@H](C)O)no2)cc1C#N nan
58344745 152550 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
CHEMBL3971646 152550 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
58344878 152664 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N[C@H](C)CO)no2)cc1C#N nan
CHEMBL3972549 152664 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N[C@H](C)CO)no2)cc1C#N nan
58344568 152811 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 448 7 2 8 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)OCCO)no2)cc1C#N nan
CHEMBL3973804 152811 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 448 7 2 8 3.8 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)OCCO)no2)cc1C#N nan
58344842 152941 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N[C@H](C)CO)no2)cc1C#N nan
CHEMBL3975029 152941 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 418 7 2 7 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4N[C@H](C)CO)no2)cc1C#N nan
58344624 153073 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 509 8 1 8 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N(C)C)no2)cc1C#N nan
CHEMBL3976048 153073 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 509 8 1 8 3.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CC(=O)N(C)C)no2)cc1C#N nan
58344805 153199 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(O)CC3)no2)cc1C#N nan
CHEMBL3977164 153199 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC(O)CC3)no2)cc1C#N nan
58344642 153233 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC[C@H](O)C3)no2)cc1C#N nan
CHEMBL3977376 153233 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 487 5 2 7 4.2 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CCC[C@H](O)C3)no2)cc1C#N nan
89787333 153308 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 464 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)C3CC3)no2)cc1C#N nan
CHEMBL3978076 153308 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 464 7 1 7 4.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)C3CC3)no2)cc1C#N nan
52938304 153502 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NCCS(C)(=O)=O)no2)cc1C#N nan
CHEMBL3979740 153502 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 466 8 1 8 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CCC4NCCS(C)(=O)=O)no2)cc1C#N nan
58344686 153511 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 388 6 1 6 4.7 CCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3979815 153511 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 388 6 1 6 4.7 CCN[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
52939915 154056 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 458 6 0 8 4.2 COC(=O)C1CN(C2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)C1 nan
CHEMBL3984513 154056 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 458 6 0 8 4.2 COC(=O)C1CN(C2CCc3c(-c4noc(-c5ccc(OC(C)C)c(C#N)c5)n4)cccc32)C1 nan
58344775 154181 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
CHEMBL3985742 154181 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 nan
89787334 154359 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 496 10 1 8 4.0 CCOCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3987033 154359 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 496 10 1 8 4.0 CCOCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
58344532 154366 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 481 9 2 8 3.2 CNCCS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3987097 154366 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 481 9 2 8 3.2 CNCCS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
67250226 116354 0 None -1 7 Mouse 10.3 pEC50 = 10.3 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359522 116354 0 None -1 7 Mouse 10.3 pEC50 = 10.3 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
49839234 117951 1 None -1 8 Mouse 10.3 pEC50 = 10.3 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
CHEMBL3403619 117951 1 None -1 8 Mouse 10.3 pEC50 = 10.3 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
53362086 116355 0 None -1 7 Rat 10.3 pEC50 = 10.3 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
CHEMBL3359523 116355 0 None -1 7 Rat 10.3 pEC50 = 10.3 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
44548061 73684 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 453 9 2 5 6.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCCCC(=O)O)c[nH]c34)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
CHEMBL2018319 73684 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 453 9 2 5 6.1 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCCCC(=O)O)c[nH]c34)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
53362086 116355 0 None -1 7 Rhesus macaque 10.2 pEC50 = 10.2 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
CHEMBL3359523 116355 0 None -1 7 Rhesus macaque 10.2 pEC50 = 10.2 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
49839234 117951 1 None -3 8 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
CHEMBL3403619 117951 1 None -3 8 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
10883396 3649 45 None -1 15 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml500389m
5283560 3649 45 None -1 15 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml500389m
911 3649 45 None -1 15 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml500389m
CHEMBL225155 3649 45 None -1 15 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml500389m
53362086 116355 0 None -1 7 Mouse 10.2 pEC50 = 10.2 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
CHEMBL3359523 116355 0 None -1 7 Mouse 10.2 pEC50 = 10.2 Functional
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
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
58329611 116351 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 447 7 1 4 6.0 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
CHEMBL3359519 116351 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 447 7 1 4 6.0 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
44412936 138766 0 None 213 3 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 405 8 1 6 4.8 CC[C@H](C)Oc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C#N 10.1016/j.bmcl.2006.04.084
CHEMBL378054 138766 0 None 213 3 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 405 8 1 6 4.8 CC[C@H](C)Oc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C#N 10.1016/j.bmcl.2006.04.084
11619303 158950 0 None 3 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 449 9 1 4 5.3 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
CHEMBL4095920 158950 0 None 3 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 449 9 1 4 5.3 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
67250226 116354 0 None -1 7 Rat 10.1 pEC50 = 10.1 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359522 116354 0 None -1 7 Rat 10.1 pEC50 = 10.1 Functional
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
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
44602504 116280 6 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 457 6 2 2 6.9 O=C(O)CC1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1021/ml500389m
CHEMBL3358912 116280 6 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 457 6 2 2 6.9 O=C(O)CC1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1021/ml500389m
44623997 116279 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 471 6 2 2 7.3 O=C(O)CC1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCCC4)c(C(F)(F)F)c3)cc21 10.1021/ml500389m
CHEMBL3358911 116279 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 471 6 2 2 7.3 O=C(O)CC1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCCC4)c(C(F)(F)F)c3)cc21 10.1021/ml500389m
25192001 8059 0 None 2 4 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 413 12 4 4 3.5 CCCCCCCCc1ccc2c(c1)CC[C@@H](C(N)(CO)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
CHEMBL1091103 8059 0 None 2 4 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 413 12 4 4 3.5 CCCCCCCCc1ccc2c(c1)CC[C@@H](C(N)(CO)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
70683348 73687 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 449 7 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCc5nnn[nH]5)c[nH]c34)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
CHEMBL2018322 73687 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 449 7 2 7 4.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c(CCc5nnn[nH]5)c[nH]c34)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
70694327 74979 0 None 12589 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 494 6 1 4 6.8 O=C(O)CCN1CCC(c2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1 10.1016/j.bmcl.2012.04.095
CHEMBL2032434 74979 0 None 12589 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 494 6 1 4 6.8 O=C(O)CCN1CCC(c2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1 10.1016/j.bmcl.2012.04.095
44138103 75783 0 None -2 4 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048293 75783 0 None -2 4 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
24825338 77710 0 None 467 3 Human 10.1 pEC50 = 10.1 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL208924 77710 0 None 467 3 Human 10.1 pEC50 = 10.1 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
11689680 79640 0 None 102 3 Human 10.1 pEC50 = 10.1 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL211505 79640 0 None 102 3 Human 10.1 pEC50 = 10.1 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
44624141 116278 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 428 6 2 3 6.2 N#Cc1cc(COc2ccc3[nH]c4c(c3c2)CCC4CC(=O)O)ccc1C1CCCCC1 10.1021/ml500389m
CHEMBL3358910 116278 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 428 6 2 3 6.2 N#Cc1cc(COc2ccc3[nH]c4c(c3c2)CCC4CC(=O)O)ccc1C1CCCCC1 10.1021/ml500389m
25192005 7736 0 None 3 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@@H]([C@@](C)(N)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
CHEMBL1089004 7736 0 None 3 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@@H]([C@@](C)(N)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
24825338 77710 0 None 467 3 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL208924 77710 0 None 467 3 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.04.084
58344520 146576 0 None 169 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCC(=O)N(C)C)no2)cc1C#N nan
CHEMBL3922998 146576 0 None 169 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCC(=O)N(C)C)no2)cc1C#N nan
67196597 147963 0 None 562 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 482 9 1 8 3.6 COCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3933952 147963 0 None 562 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 482 9 1 8 3.6 COCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
44624067 116287 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 457 6 2 2 6.9 O=C(O)C[C@@H]1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1021/ml500389m
CHEMBL3358919 116287 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 457 6 2 2 6.9 O=C(O)C[C@@H]1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1021/ml500389m
46174905 116288 0 None 162 3 Human 10.0 pEC50 = 10.0 Functional
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
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
CHEMBL3358955 116288 0 None 162 3 Human 10.0 pEC50 = 10.0 Functional
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
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
54576288 76448 0 None 25118 2 Human 10.0 pEC50 = 10 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 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 10.1021/jm2016107
CHEMBL2059687 76448 0 None 25118 2 Human 10.0 pEC50 = 10 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 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 10.1021/jm2016107
44138103 75783 0 None 2 4 Rat 10.0 pEC50 = 10 Functional
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
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048293 75783 0 None 2 4 Rat 10.0 pEC50 = 10 Functional
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
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
11689680 79640 0 None 102 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL211505 79640 0 None 102 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
11626664 77928 0 None 239 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 455 7 1 6 5.1 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C(F)(F)F)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL209484 77928 0 None 239 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 455 7 1 6 5.1 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C(F)(F)F)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
44412994 78320 0 None 7 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1016/j.bmcl.2006.04.084
CHEMBL210942 78320 0 None 7 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1016/j.bmcl.2006.04.084
70690096 74986 0 None 1258 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 480 7 1 4 6.1 O=C(O)C1CN(CCCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)C1 10.1016/j.bmcl.2012.04.095
CHEMBL2032441 74986 0 None 1258 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 480 7 1 4 6.1 O=C(O)C1CN(CCCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)C1 10.1016/j.bmcl.2012.04.095
58344502 142845 0 None 398 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC(O)C3)no2)cc1C#N nan
CHEMBL3893172 142845 0 None 398 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC(O)C3)no2)cc1C#N nan
58344715 143073 0 None 575 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCO)no2)cc1C#N nan
CHEMBL3895230 143073 0 None 575 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCO)no2)cc1C#N nan
58344692 144922 0 None 758 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC(O)C3)no2)cc1C#N nan
CHEMBL3910269 144922 0 None 758 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC(O)C3)no2)cc1C#N nan
76325522 105734 0 None 7413 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 480 10 3 8 3.2 CCc1cc(-c2noc(-c3ccnc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126433 105734 0 None 7413 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 480 10 3 8 3.2 CCc1cc(-c2noc(-c3ccnc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
68555865 105737 0 None 331 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126436 105737 0 None 331 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/jm4014696
76310992 105740 0 None 239 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 480 10 3 8 3.1 CCc1cc(-c2noc(-c3cc(C)nc(C4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126584 105740 0 None 239 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 480 10 3 8 3.1 CCc1cc(-c2noc(-c3cc(C)nc(C4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
76314622 105744 0 None 50 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126588 105744 0 None 50 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/jm4014696
76321895 105762 0 None 13489 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 482 12 3 8 3.4 CCc1cc(-c2noc(-c3ccnc(C(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126607 105762 0 None 13489 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 482 12 3 8 3.4 CCc1cc(-c2noc(-c3ccnc(C(CC)CC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
76336364 105775 0 None 4265 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126620 105775 0 None 4265 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/jm4014696
76314625 105777 0 None 251 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 494 10 3 8 3.5 CCc1cc(-c2noc(-c3cnc(C4CCCC4)c(C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126622 105777 0 None 251 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 494 10 3 8 3.5 CCc1cc(-c2noc(-c3cnc(C4CCCC4)c(C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
68762699 105778 0 None 288 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126623 105778 0 None 288 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/jm4014696
16038017 139418 0 None 398 3 Human 10.0 pEC50 = 10.0 Functional
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
ChEMBL 431 7 1 6 4.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OCC(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL379380 139418 0 None 398 3 Human 10.0 pEC50 = 10.0 Functional
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
ChEMBL 431 7 1 6 4.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OCC(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
11496072 146024 0 None 32 3 Human 9.9 pEC50 = 9.9 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 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 10.1016/j.bmcl.2006.10.057
CHEMBL391869 146024 0 None 32 3 Human 9.9 pEC50 = 9.9 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 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 10.1016/j.bmcl.2006.10.057
58344592 154566 0 None 100 4 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N(C)C)no2)cc1C#N nan
CHEMBL3921214 154566 0 None 100 4 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N(C)C)no2)cc1C#N nan
CHEMBL3991184 154566 0 None 100 4 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N(C)C)no2)cc1C#N nan
67249162 116352 0 None 912 2 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359520 116352 0 None 912 2 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
49872979 117959 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 473 6 1 4 6.4 O=C(O)CC1OCCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1016/j.bmcl.2014.11.089
CHEMBL3403626 117959 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 473 6 1 4 6.4 O=C(O)CC1OCCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1016/j.bmcl.2014.11.089
11222939 67575 9 None 4 4 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
44438254 67575 9 None 4 4 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL190006 67575 9 None 4 4 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
11603726 76830 0 None 588 3 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL206940 76830 0 None 588 3 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.064
58329611 116351 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 447 7 1 4 6.0 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
CHEMBL3359519 116351 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 447 7 1 4 6.0 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
67249162 116352 0 None 912 2 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359520 116352 0 None 912 2 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
49873283 117969 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 520 6 1 4 7.0 CN1CCn2c(c(Cl)c3cc(OCc4ccc(C5CCCC5)c(C(F)(F)F)c4)ccc32)C1CC(=O)O 10.1016/j.bmcl.2014.11.089
CHEMBL3403636 117969 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 520 6 1 4 7.0 CN1CCn2c(c(Cl)c3cc(OCc4ccc(C5CCCC5)c(C(F)(F)F)c4)ccc32)C1CC(=O)O 10.1016/j.bmcl.2014.11.089
54576291 76041 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 513 9 1 6 6.2 CCc1c(CCN2CCC(C(=O)O)CC2)cccc1-c1nsc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1021/jm2016107
CHEMBL2057282 76041 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 513 9 1 6 6.2 CCc1c(CCN2CCC(C(=O)O)CC2)cccc1-c1nsc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1021/jm2016107
70681688 74981 0 None 3162 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 494 6 1 4 6.5 O=C(O)C1CCN(CCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1 10.1016/j.bmcl.2012.04.095
CHEMBL2032436 74981 0 None 3162 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 494 6 1 4 6.5 O=C(O)C1CCN(CCc2ccc3oc(-c4ccc(-c5ccccc5)c(C(F)(F)F)c4)nc3c2)CC1 10.1016/j.bmcl.2012.04.095
52938427 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
5383 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
8709 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
CHEMBL3707247 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
DB12612 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
52938427 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2018.10.042
5383 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2018.10.042
8709 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2018.10.042
CHEMBL3707247 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2018.10.042
DB12612 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2018.10.042
44412828 77491 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 405 7 1 5 5.3 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(CC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL208718 77491 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 405 7 1 5 5.3 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(CC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
52938427 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
5383 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
8709 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
CHEMBL3707247 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
DB12612 2984 55 None 33 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
25110382 146109 0 None 354 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CCC4O)no2)cc1OCC nan
CHEMBL3919445 146109 0 None 354 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CCC4O)no2)cc1OCC nan
58344526 150128 4 None 95 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCO)no2)cc1C#N nan
CHEMBL3951270 150128 4 None 95 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 404 7 2 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCO)no2)cc1C#N nan
58344778 154537 0 None 117 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 360 4 1 6 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N nan
CHEMBL3902160 154537 0 None 117 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 360 4 1 6 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N nan
CHEMBL3990889 154537 0 None 117 5 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 360 4 1 6 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N nan
11654374 78382 0 None 660 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1ncc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL211046 78382 0 None 660 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1ncc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
52938426 3376 12 None 70 5 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N nan
9889 3376 12 None 70 5 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N nan
CHEMBL3899384 3376 12 None 70 5 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N nan
11568622 158201 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 450 9 1 5 4.7 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)n1 10.1021/acs.jmedchem.7b00785
CHEMBL4087932 158201 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 450 9 1 5 4.7 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)n1 10.1021/acs.jmedchem.7b00785
49848139 76397 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 419 9 1 6 5.0 CCc1c(CCCC(=O)O)cccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1021/jm2016107
CHEMBL2059515 76397 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 419 9 1 6 5.0 CCc1c(CCCC(=O)O)cccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1021/jm2016107
44547461 73669 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3ccc4[nH]c(CCC(=O)O)cc4c3)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
CHEMBL2018178 73669 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3ccc4[nH]c(CCC(=O)O)cc4c3)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
10174255 85217 0 None 8 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 485 6 1 6 5.7 O=C(O)C1CN(Cc2ccc(-c3noc(-c4cc(-c5ccccc5)c(C(F)(F)F)s4)n3)cc2)C1 10.1021/jm0492507
CHEMBL225575 85217 0 None 8 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 485 6 1 6 5.7 O=C(O)C1CN(Cc2ccc(-c3noc(-c4cc(-c5ccccc5)c(C(F)(F)F)s4)n3)cc2)C1 10.1021/jm0492507
44412813 138670 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 407 7 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL377767 138670 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 407 7 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
11603726 76830 0 None 588 3 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL206940 76830 0 None 588 3 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
11646599 77666 0 None 1047 3 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 380 7 1 5 4.8 Cc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C 10.1016/j.bmcl.2006.04.084
CHEMBL208898 77666 0 None 1047 3 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 380 7 1 5 4.8 Cc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C 10.1016/j.bmcl.2006.04.084
57335019 70704 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 461 7 2 5 5.3 C[C@@](N)(CCc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1)C(=O)O 10.1016/j.bmcl.2011.12.073
CHEMBL1950574 70704 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 461 7 2 5 5.3 C[C@@](N)(CCc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1)C(=O)O 10.1016/j.bmcl.2011.12.073
10174255 85217 0 None 8 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 485 6 1 6 5.7 O=C(O)C1CN(Cc2ccc(-c3noc(-c4cc(-c5ccccc5)c(C(F)(F)F)s4)n3)cc2)C1 10.1016/j.bmcl.2013.09.058
CHEMBL225575 85217 0 None 8 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 485 6 1 6 5.7 O=C(O)C1CN(Cc2ccc(-c3noc(-c4cc(-c5ccccc5)c(C(F)(F)F)s4)n3)cc2)C1 10.1016/j.bmcl.2013.09.058
25031140 105643 0 None 229 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3124957 105643 0 None 229 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/jm4014696
68553624 105741 0 None 234 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)nc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126585 105741 0 None 234 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)nc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
76314621 105743 0 None 18 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126587 105743 0 None 18 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/jm4014696
76325532 105760 0 None 3801 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 468 11 3 8 2.7 CCc1cc(-c2noc(-c3ccnc(CC(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126605 105760 0 None 3801 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 468 11 3 8 2.7 CCc1cc(-c2noc(-c3ccnc(CC(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
44218002 105766 0 None 776 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126611 105766 0 None 776 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/jm4014696
76325533 105768 0 None 537 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)c(C4CCCC4)cn3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126613 105768 0 None 537 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)c(C4CCCC4)cn3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
76318198 105770 0 None 3090 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126615 105770 0 None 3090 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/jm4014696
76314624 105774 0 None 4365 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)cc(C4CCCC4)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126619 105774 0 None 4365 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 494 10 3 8 3.5 CCc1cc(-c2noc(-c3cc(C)cc(C4CCCC4)n3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
76321896 105779 0 None 120 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 508 11 3 8 3.7 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cnc1C1CCCC1 10.1021/jm4014696
CHEMBL3126624 105779 0 None 120 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 508 11 3 8 3.7 CCc1cc(-c2nc(-c3cc(C)c(OC[C@@H](O)CNC(=O)CO)c(CC)c3)no2)cnc1C1CCCC1 10.1021/jm4014696
25031140 105643 0 None 229 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1016/j.ejmech.2016.03.048
CHEMBL3124957 105643 0 None 229 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1016/j.ejmech.2016.03.048
127046184 139880 0 None 478 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1016/j.ejmech.2016.03.020
CHEMBL3799305 139880 0 None 478 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1016/j.ejmech.2016.03.020
44439850 146027 0 None 24 3 Human 9.7 pEC50 = 9.7 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 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 10.1016/j.bmcl.2006.10.057
CHEMBL391870 146027 0 None 24 3 Human 9.7 pEC50 = 9.7 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 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 10.1016/j.bmcl.2006.10.057
44412704 139370 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 443 9 1 6 4.8 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(CF)CF)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL379310 139370 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 443 9 1 6 4.8 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(CF)CF)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
44138103 75783 0 None -2 4 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048293 75783 0 None -2 4 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
54576290 76042 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 485 9 1 6 5.4 CCc1c(CCN2CC(C(=O)O)C2)cccc1-c1nsc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1021/jm2016107
CHEMBL2057283 76042 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 485 9 1 6 5.4 CCc1c(CCN2CC(C(=O)O)C2)cccc1-c1nsc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1021/jm2016107
57522812 76447 0 None 10000 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 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 10.1021/jm2016107
CHEMBL2059686 76447 0 None 10000 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 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 10.1021/jm2016107
54576289 76449 0 None 12589 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 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 10.1021/jm2016107
CHEMBL2059688 76449 0 None 12589 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity against S1P1 receptor by cell based FRET assayAgonist activity against S1P1 receptor by cell based FRET assay
ChEMBL 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 10.1021/jm2016107
44547318 73668 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3ccc4c(CCC(=O)O)c[nH]c4c3)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
CHEMBL2018177 73668 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 425 7 2 5 5.3 CC(C)Oc1ccc(-c2nc(-c3ccc4c(CCC(=O)O)c[nH]c4c3)no2)cc1Cl 10.1016/j.bmcl.2012.02.083
44547605 73674 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 460 7 2 6 5.1 CC(C)Oc1ncc(-c2nc(-c3cccc4c(CCC(=O)O)c[nH]c34)no2)cc1C(F)(F)F 10.1016/j.bmcl.2012.02.083
CHEMBL2018306 73674 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 460 7 2 6 5.1 CC(C)Oc1ncc(-c2nc(-c3cccc4c(CCC(=O)O)c[nH]c34)no2)cc1C(F)(F)F 10.1016/j.bmcl.2012.02.083
59384310 104391 0 None 2 3 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 511 13 3 7 5.2 CCCCCCCCOc1ccc(-c2nnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F 10.1021/ml400194r
CHEMBL3102904 104391 0 None 2 3 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 511 13 3 7 5.2 CCCCCCCCOc1ccc(-c2nnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F 10.1021/ml400194r
46846899 139946 0 None 2511 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 458 9 1 7 4.9 CCCCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccc1 10.1021/acs.jmedchem.6b00089
CHEMBL3799701 139946 0 None 2511 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 458 9 1 7 4.9 CCCCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1-c1ccccc1 10.1021/acs.jmedchem.6b00089
44413039 78012 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 421 8 1 6 5.2 CCC(C)Oc1ccc(-c2nnc(-c3ccc(CCC(=O)O)cc3C)s2)cc1C#N 10.1016/j.bmcl.2006.04.064
CHEMBL209778 78012 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 421 8 1 6 5.2 CCC(C)Oc1ccc(-c2nnc(-c3ccc(CCC(=O)O)cc3C)s2)cc1C#N 10.1016/j.bmcl.2006.04.064
11452022 3596 39 None 1 6 Rat 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.ejmech.2012.02.022
6996 3596 39 None 1 6 Rat 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.ejmech.2012.02.022
CHEMBL366208 3596 39 None 1 6 Rat 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.ejmech.2012.02.022
11452022 3596 39 None 1 6 Rat 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
6996 3596 39 None 1 6 Rat 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
CHEMBL366208 3596 39 None 1 6 Rat 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
2924 1640 43 None 2 7 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
44398069 1640 43 None 2 7 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
9908268 1640 43 None 2 7 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
CHEMBL114606 1640 43 None 2 7 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
11452022 3596 39 None -1 6 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm050242f
6996 3596 39 None -1 6 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm050242f
CHEMBL366208 3596 39 None -1 6 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm050242f
45377662 84117 0 None 204 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
ChEMBL 468 9 1 6 4.3 CCCCN(C(=O)c1ccccc1F)c1nnc(-c2ccc(CN3CC(C(=O)O)C3)cc2)s1 10.1016/j.bmcl.2012.09.110
CHEMBL2207778 84117 0 None 204 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at S1P1 receptor by [35S]GTPgammaS binding assayAgonist activity at S1P1 receptor by [35S]GTPgammaS binding assay
ChEMBL 468 9 1 6 4.3 CCCCN(C(=O)c1ccccc1F)c1nnc(-c2ccc(CN3CC(C(=O)O)C3)cc2)s1 10.1016/j.bmcl.2012.09.110
11452022 3596 39 None -1 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at SIP1 receptorAgonist activity at SIP1 receptor
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2012.04.095
6996 3596 39 None -1 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at SIP1 receptorAgonist activity at SIP1 receptor
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2012.04.095
CHEMBL366208 3596 39 None -1 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at SIP1 receptorAgonist activity at SIP1 receptor
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2012.04.095
57401335 70702 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 447 7 2 5 4.9 N[C@H](CCc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1)C(=O)O 10.1016/j.bmcl.2011.12.073
CHEMBL1950572 70702 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 447 7 2 5 4.9 N[C@H](CCc1ccc(-c2nc3ccc(C4(c5ccccc5)CC4)nc3s2)c(F)c1)C(=O)O 10.1016/j.bmcl.2011.12.073
49872602 117613 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 454 6 3 4 5.0 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(OC(F)(F)F)c(Cl)c3)cc21 10.1016/j.bmcl.2014.11.089
CHEMBL3400916 117613 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 454 6 3 4 5.0 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(OC(F)(F)F)c(Cl)c3)cc21 10.1016/j.bmcl.2014.11.089
46846913 139679 0 None 2818 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 424 9 1 7 4.1 CCCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1CC(C)C 10.1021/acs.jmedchem.6b00089
CHEMBL3797951 139679 0 None 2818 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 424 9 1 7 4.1 CCCc1c(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)noc1CC(C)C 10.1021/acs.jmedchem.6b00089
59982944 87591 0 None 7244 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 494 10 2 4 6.4 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)c(F)c1 10.1021/ml300396r
CHEMBL2336064 87591 0 None 7244 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 494 10 2 4 6.4 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)c(F)c1 10.1021/ml300396r
57570498 87612 0 None 5011 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 476 10 2 4 6.3 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)cc1 10.1021/ml300396r
CHEMBL2336086 87612 0 None 5011 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 476 10 2 4 6.3 C/C(=N\OCc1ccc(C2CCCCC2)c(C(F)(F)F)c1)c1ccc(CNCCC(=O)O)cc1 10.1021/ml300396r
25031771 105735 0 None 5011 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126434 105735 0 None 5011 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/jm4014696
76325528 105745 0 None 7 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126589 105745 0 None 7 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/jm4014696
76336361 105758 1 None 12882 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 454 10 3 8 2.6 CCc1cc(-c2noc(-c3ccnc(C(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
CHEMBL3126603 105758 1 None 12882 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 454 10 3 8 2.6 CCc1cc(-c2noc(-c3ccnc(C(C)C)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1021/jm4014696
44218604 105763 0 None 100 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/jm4014696
CHEMBL3126608 105763 0 None 100 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/jm4014696
66829275 139632 0 None 147 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1016/j.ejmech.2016.03.048
CHEMBL3797647 139632 0 None 147 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1016/j.ejmech.2016.03.048
127046548 139603 0 None 234 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 510 11 3 9 3.2 CCc1cc(-c2noc(-c3cnc(C4CCCC4)c(OC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.020
CHEMBL3797447 139603 0 None 234 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 510 11 3 9 3.2 CCc1cc(-c2noc(-c3cnc(C4CCCC4)c(OC)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.020
68547259 139976 0 None 89 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1016/j.ejmech.2016.03.020
CHEMBL3799872 139976 0 None 89 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1016/j.ejmech.2016.03.020
127046185 140017 0 None 363 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 496 11 3 9 2.8 CCc1cc(-c2noc(-c3cc(C)nc(OC4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.020
CHEMBL3800120 140017 0 None 363 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 496 11 3 9 2.8 CCc1cc(-c2noc(-c3cc(C)nc(OC4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.020
127047020 140020 0 None 72 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 496 11 3 9 2.8 CCc1cc(-c2noc(-c3cc(OC)nc(C4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.020
CHEMBL3800133 140020 0 None 72 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 496 11 3 9 2.8 CCc1cc(-c2noc(-c3cc(OC)nc(C4CCC4)c3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.020
11662328 91765 0 None 33 3 Human 9.5 pEC50 = 9.5 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 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 10.1016/j.bmcl.2006.10.057
CHEMBL241050 91765 0 None 33 3 Human 9.5 pEC50 = 9.5 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 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 10.1016/j.bmcl.2006.10.057
44439851 145647 0 None 37 3 Human 9.5 pEC50 = 9.5 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 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 10.1016/j.bmcl.2006.10.057
CHEMBL391581 145647 0 None 37 3 Human 9.5 pEC50 = 9.5 Functional
Displacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cellsDisplacement of [35S]GTPgammaS from human S1P1 receptor expressed in CHO cells
ChEMBL 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 10.1016/j.bmcl.2006.10.057
44547909 73688 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 453 8 1 6 5.8 CCn1cc(CCC(=O)O)c2cccc(-c3noc(-c4ccc(OC(C)C)c(Cl)c4)n3)c21 10.1016/j.bmcl.2012.02.083
CHEMBL2018324 73688 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at S1P1 receptor by Tango assayAgonist activity at S1P1 receptor by Tango assay
ChEMBL 453 8 1 6 5.8 CCn1cc(CCC(=O)O)c2cccc(-c3noc(-c4ccc(OC(C)C)c(Cl)c4)n3)c21 10.1016/j.bmcl.2012.02.083
70688066 74965 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 454 8 1 4 6.8 O=C(O)CCCCCc1cnc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.04.095
CHEMBL2032311 74965 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 454 8 1 4 6.8 O=C(O)CCCCCc1cnc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.04.095
70692256 74974 0 None 3162 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL 468 8 1 4 6.1 CN(CCCc1ccc2oc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)nc2c1)CC(=O)O 10.1016/j.bmcl.2012.04.095
CHEMBL2032429 74974 0 None 3162 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at SIP1 receptor by tango assayAgonist activity at SIP1 receptor by tango assay
ChEMBL