Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
77846754 181950 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 435 5 1 3 6.3 Cc1cc(OC2CCC3(CCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4787458 181950 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 435 5 1 3 6.3 Cc1cc(OC2CCC3(CCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
77846502 180048 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 6 2 3 6.1 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4754965 180048 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 6 2 3 6.1 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
12573 978 1 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
77846592 978 1 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
CHEMBL4748198 978 1 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
77847762 182831 0 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 397 7 2 3 5.7 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4798593 182831 0 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 397 7 2 3 5.7 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
77846503 181718 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 6 2 3 6.9 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4784199 181718 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 6 2 3 6.9 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
11452022 3526 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 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 3526 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 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 3526 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 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
25192001 7961 0 None -2 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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 7961 0 None -2 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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
11502996 158169 36 None -11 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 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 158169 36 None -11 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 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
11452022 3526 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
6996 3526 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
CHEMBL366208 3526 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
11452022 3526 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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 3526 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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 3526 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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
11452022 3526 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assayAgonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.0c00631
6996 3526 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assayAgonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.0c00631
CHEMBL366208 3526 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assayAgonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.0c00631
2924 1602 37 None -4 7 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.5b00448
44398069 1602 37 None -4 7 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.5b00448
9908268 1602 37 None -4 7 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.5b00448
CHEMBL114606 1602 37 None -4 7 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.5b00448
11222939 67218 6 None -9 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 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 67218 6 None -9 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 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 67218 6 None -9 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 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
46881623 6670 0 None 5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 477 9 2 6 4.1 Cc1cc(CN2CC(C(=O)O)C2)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1083828 6670 0 None 5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 477 9 2 6 4.1 Cc1cc(CN2CC(C(=O)O)C2)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
59384310 103899 0 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R 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 103899 0 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R 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
11452022 3526 33 None -3 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.8b01695
6996 3526 33 None -3 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.8b01695
CHEMBL366208 3526 33 None -3 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.8b01695
2924 1602 37 None -4 7 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.0c01109
44398069 1602 37 None -4 7 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.0c01109
9908268 1602 37 None -4 7 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.0c01109
CHEMBL114606 1602 37 None -4 7 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.0c01109
44412994 77902 0 None -7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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 77902 0 None -7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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
77846505 179426 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 6 2 3 6.5 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CCC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4747262 179426 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 6 2 3 6.5 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CCC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
10883396 3579 39 None -2 15 Human 9.0 pEC50 = 9.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR 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.2006.10.014
5283560 3579 39 None -2 15 Human 9.0 pEC50 = 9.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR 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.2006.10.014
911 3579 39 None -2 15 Human 9.0 pEC50 = 9.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR 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.2006.10.014
CHEMBL225155 3579 39 None -2 15 Human 9.0 pEC50 = 9.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR 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.2006.10.014
11568622 157644 0 None -1 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 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 157644 0 None -1 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 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
77847765 182807 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 5 1 3 6.0 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4798181 182807 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 5 1 3 6.0 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
44599207 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
5326 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
9289 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
CHEMBL2336071 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
DB12371 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
11619303 158392 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 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 158392 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 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
77846753 180257 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 449 5 1 3 6.7 Cc1cc(OC2CCC3(CCCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4757160 180257 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 449 5 1 3 6.7 Cc1cc(OC2CCC3(CCCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
90324880 179766 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 343 11 2 3 4.7 CCCCCCOc1cc(C)c2ccccc2c1CNCCC(=O)O 10.1021/acsmedchemlett.0c00631
CHEMBL4751484 179766 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 343 11 2 3 4.7 CCCCCCOc1cc(C)c2ccccc2c1CNCCC(=O)O 10.1021/acsmedchemlett.0c00631
77847763 181216 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 411 8 2 3 6.1 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4778095 181216 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 411 8 2 3 6.1 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
46884020 8340 0 None -8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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 8340 0 None -8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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
10883396 3579 39 None -2 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml400194r
5283560 3579 39 None -2 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml400194r
911 3579 39 None -2 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml400194r
CHEMBL225155 3579 39 None -2 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml400194r
10904818 300 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 10.1016/j.bmcl.2005.09.038
2937 300 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 10.1016/j.bmcl.2005.09.038
CHEMBL382739 300 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 10.1016/j.bmcl.2005.09.038
44406004 72355 8 None -11 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 337 14 4 4 2.9 CCCCCCCCCC/C=C/[C@@H](O)[C@@H](N)COP(=O)(O)O 10.1016/j.bmcl.2005.09.038
CHEMBL199791 72355 8 None -11 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 337 14 4 4 2.9 CCCCCCCCCC/C=C/[C@@H](O)[C@@H](N)COP(=O)(O)O 10.1016/j.bmcl.2005.09.038
11678855 133907 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 607 21 4 10 5.9 C[C@@](N)(CCc1ccc(OCCCCCCCCCCCNc2ccc([N+](=O)[O-])c3nonc23)cc1)COP(=O)(O)O 10.1016/j.bmcl.2005.09.038
CHEMBL371758 133907 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 607 21 4 10 5.9 C[C@@](N)(CCc1ccc(OCCCCCCCCCCCNc2ccc([N+](=O)[O-])c3nonc23)cc1)COP(=O)(O)O 10.1016/j.bmcl.2005.09.038
16215109 146963 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
44438256 146963 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL393055 146963 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
16215109 146963 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2011.09.049
44438256 146963 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2011.09.049
CHEMBL393055 146963 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2011.09.049
78321974 139771 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acsmedchemlett.5b00448
CHEMBL3806205 139771 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acsmedchemlett.5b00448
78321974 139771 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.8b01695
CHEMBL3806205 139771 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.8b01695
78321974 139771 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
CHEMBL3806205 139771 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
66655386 166956 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCCC2(COc3cc(OCc4c(Cl)cccc4Cl)ccc32)C1 10.1016/j.bmcl.2017.12.018
CHEMBL4218296 166956 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCCC2(COc3cc(OCc4c(Cl)cccc4Cl)ccc32)C1 10.1016/j.bmcl.2017.12.018
CHEMBL4300113 166956 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCCC2(COc3cc(OCc4c(Cl)cccc4Cl)ccc32)C1 10.1016/j.bmcl.2017.12.018
66655175 167003 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 367 6 1 4 3.5 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4213649 167003 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 367 6 1 4 3.5 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300641 167003 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 367 6 1 4 3.5 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
46881912 6673 0 None -2 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 425 13 2 5 2.8 CCCCCCCOc1ccc(CC[C@](C)(N)CCN2CC(=O)NS2(=O)=O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1083841 6673 0 None -2 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 425 13 2 5 2.8 CCCCCCCOc1ccc(CC[C@](C)(N)CCN2CC(=O)NS2(=O)=O)cc1 10.1016/j.bmcl.2010.01.118
44412827 77373 0 None -89 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 432 9 1 4 6.9 Cc1cc(CCCCCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL209008 77373 0 None -89 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 432 9 1 4 6.9 Cc1cc(CCCCCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
44517795 67944 0 None -109 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assayAgonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assay
ChEMBL 472 6 1 7 3.9 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)c1 10.1016/j.bmcl.2011.05.110
CHEMBL1916399 67944 0 None -109 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assayAgonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assay
ChEMBL 472 6 1 7 3.9 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)c1 10.1016/j.bmcl.2011.05.110
42630194 75410 0 None -7 5 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048287 75410 0 None -7 5 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
2924 1602 37 None -4 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
44398069 1602 37 None -4 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
9908268 1602 37 None -4 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
CHEMBL114606 1602 37 None -4 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
25154344 6447 0 None -38 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 515 11 3 7 3.3 Cc1cc(S(=O)(=O)NCCC(=O)O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1082869 6447 0 None -38 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 515 11 3 7 3.3 Cc1cc(S(=O)(=O)NCCC(=O)O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
66655656 166988 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 431 5 1 3 5.4 O=C(O)CCN1CCC2(CC1)COc1cc(/C=C/c3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4218826 166988 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 431 5 1 3 5.4 O=C(O)CCN1CCC2(CC1)COc1cc(/C=C/c3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300415 166988 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 431 5 1 3 5.4 O=C(O)CCN1CCC2(CC1)COc1cc(/C=C/c3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
66655211 167163 0 None 316 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 451 6 1 4 5.5 O=C(O)CCN1CCC2(CC1)COc1cc(SCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4205124 167163 0 None 316 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 451 6 1 4 5.5 O=C(O)CCN1CCC2(CC1)COc1cc(SCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302786 167163 0 None 316 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 451 6 1 4 5.5 O=C(O)CCN1CCC2(CC1)COc1cc(SCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
58344592 154017 0 None -100 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 154017 0 None -100 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 154017 0 None -100 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
11654374 77964 0 None -660 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 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 77964 0 None -660 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 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
10883396 3579 39 None -2 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
5283560 3579 39 None -2 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
911 3579 39 None -2 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
CHEMBL225155 3579 39 None -2 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
77846594 180910 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 409 6 1 3 5.8 CC[C@H]1CC[C@@H](Oc2cc(C)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4764896 180910 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 409 6 1 3 5.8 CC[C@H]1CC[C@@H](Oc2cc(C)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
66655306 167048 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 6 1 4 5.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3C(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4208787 167048 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 6 1 4 5.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3C(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301342 167048 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 6 1 4 5.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3C(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
66655521 167153 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4204779 167153 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302677 167153 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
11689680 79215 0 None -102 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 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 79215 0 None -102 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 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
44439851 145102 0 None -37 3 Human 7.9 pEC50 = 7.9 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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 145102 0 None -37 3 Human 7.9 pEC50 = 7.9 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
46224767 197608 0 None -18 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 293 2 0 4 3.2 Cc1nn(C(=O)/C=C/c2ccncc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL590383 197608 0 None -18 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 293 2 0 4 3.2 Cc1nn(C(=O)/C=C/c2ccncc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
44412865 79478 0 None -616 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 417 7 1 6 5.0 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2cnc(OC(C)C)c(Cl)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL212420 79478 0 None -616 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 417 7 1 6 5.0 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2cnc(OC(C)C)c(Cl)c2)s1 10.1016/j.bmcl.2006.04.064
44438257 93380 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](CO)N[C@@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
44438258 93380 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](CO)N[C@@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL247698 93380 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](CO)N[C@@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
25110406 1265 47 None -70 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 409 9 2 7 3.8 OCCNC1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)OCC)OCC nan
2928 1265 47 None -70 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 409 9 2 7 3.8 OCCNC1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)OCC)OCC nan
CHEMBL3922179 1265 47 None -70 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 409 9 2 7 3.8 OCCNC1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)OCC)OCC nan
11603726 76462 0 None -588 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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 76462 0 None -588 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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
25182899 6031 0 None -11 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 350 7 2 5 3.2 CCCN(CC1CC1)c1cc(C(=O)Nc2ccc3[nH]ncc3c2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1080865 6031 0 None -11 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 350 7 2 5 3.2 CCCN(CC1CC1)c1cc(C(=O)Nc2ccc3[nH]ncc3c2)ncn1 10.1016/j.bmcl.2010.01.102
57390239 67551 0 None 1 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 339 3 0 4 3.7 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910687 67551 0 None 1 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 339 3 0 4 3.7 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
42630194 75410 0 None -7 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048287 75410 0 None -7 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
44412936 138224 0 None -213 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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 138224 0 None -213 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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
58344526 149583 2 None -95 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 149583 2 None -95 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
58344520 146031 0 None -169 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 146031 0 None -169 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
66655198 163097 0 None 79 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 7 1 4 5.2 O=C(O)CCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4204437 163097 0 None 79 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 7 1 4 5.2 O=C(O)CCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
66655680 167035 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4210234 167035 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4301008 167035 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
145947403 167096 0 None 125 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 8 1 4 5.1 CCCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4205878 167096 0 None 125 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 8 1 4 5.1 CCCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4301965 167096 0 None 125 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 8 1 4 5.1 CCCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
56601980 167114 0 None 19 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 4.9 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CC(C)C(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4205225 167114 0 None 19 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 4.9 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CC(C)C(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4302166 167114 0 None 19 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 4.9 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CC(C)C(=O)O)CC1 10.1016/j.bmcl.2017.12.018
11603528 139515 0 None -154 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-n1nnc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL380040 139515 0 None -154 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-n1nnc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
77846593 181917 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 457 6 1 3 6.6 Cc1cc(O[C@H]2CC[C@@H](c3ccccc3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4787014 181917 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 457 6 1 3 6.6 Cc1cc(O[C@H]2CC[C@@H](c3ccccc3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
66655846 167181 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4215002 167181 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4303021 167181 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
49848557 1077 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assayAgonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assay
ChEMBL 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 10.1021/acs.jmedchem.5b01512
9492 1077 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assayAgonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assay
ChEMBL 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 10.1021/acs.jmedchem.5b01512
CHEMBL3769933 1077 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assayAgonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assay
ChEMBL 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 10.1021/acs.jmedchem.5b01512
44125170 65609 1 None -16 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 446 7 1 7 4.2 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(CCC(=O)O)C2 10.1021/jm200609t
CHEMBL1836169 65609 1 None -16 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 446 7 1 7 4.2 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(CCC(=O)O)C2 10.1021/jm200609t
77846674 180368 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 549 5 1 3 6.7 CC(C)(C)[C@H]1CC[C@H](Oc2cc(I)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4758438 180368 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 549 5 1 3 6.7 CC(C)(C)[C@H]1CC[C@H](Oc2cc(I)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
11977938 70551 24 None -11 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptorAgonist activity at human S1P5 receptor
ChEMBL 461 8 1 7 5.3 CCc1cc(CN2CC(C(=O)O)C2)sc1-c1noc(-c2ccc(Oc3ccccc3)cc2)n1 10.1016/j.ejmech.2012.02.022
CHEMBL1951304 70551 24 None -11 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptorAgonist activity at human S1P5 receptor
ChEMBL 461 8 1 7 5.3 CCc1cc(CN2CC(C(=O)O)C2)sc1-c1noc(-c2ccc(Oc3ccccc3)cc2)n1 10.1016/j.ejmech.2012.02.022
9969355 58118 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as intracellular calcium levelsAgonist activity at human S1P5 receptor expressed in CHO cells assessed as intracellular calcium levels
ChEMBL 369 14 2 3 4.5 O=C(O)CCNCCCc1ccc(OCCCCCc2ccccc2)cc1 10.1016/j.bmcl.2011.01.029
CHEMBL1683041 58118 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as intracellular calcium levelsAgonist activity at human S1P5 receptor expressed in CHO cells assessed as intracellular calcium levels
ChEMBL 369 14 2 3 4.5 O=C(O)CCNCCCc1ccc(OCCCCCc2ccccc2)cc1 10.1016/j.bmcl.2011.01.029
52938055 147070 0 None -478 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
CHEMBL3931243 147070 0 None -478 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
11869937 197468 8 None -75 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 292 2 0 3 3.8 Cc1nn(C(=O)/C=C/c2ccccc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL589402 197468 8 None -75 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 292 2 0 3 3.8 Cc1nn(C(=O)/C=C/c2ccccc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
44422604 85009 0 None -9 5 Human 7.7 pEC50 = 7.7 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 432 15 4 4 4.4 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)CC(F)OP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL226612 85009 0 None -9 5 Human 7.7 pEC50 = 7.7 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 432 15 4 4 4.4 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)CC(F)OP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
46881875 7234 0 None -1 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 371 13 3 3 4.3 CCCCCCCOc1ccc(CC[C@](C)(N)CCP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1086170 7234 0 None -1 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 371 13 3 3 4.3 CCCCCCCOc1ccc(CC[C@](C)(N)CCP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
66655362 163056 0 None 79 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 423 8 1 4 4.6 CCc1cccc(CC)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4203755 163056 0 None 79 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 423 8 1 4 4.6 CCc1cccc(CC)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
66654900 167018 0 None 199 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 485 7 1 5 5.0 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3OC(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4217573 167018 0 None 199 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 485 7 1 5 5.0 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3OC(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300821 167018 0 None 199 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 485 7 1 5 5.0 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3OC(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
56599785 167088 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 487 7 2 5 4.4 O=P(O)(O)OCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4205748 167088 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 487 7 2 5 4.4 O=P(O)(O)OCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301854 167088 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 487 7 2 5 4.4 O=P(O)(O)OCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
53492750 65620 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 448 7 2 8 3.1 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(C(CO)CO)C2 10.1021/jm200609t
CHEMBL1836215 65620 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 448 7 2 8 3.1 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(C(CO)CO)C2 10.1021/jm200609t
25182769 6173 0 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 380 6 2 5 4.3 Cc1cc(O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1081645 6173 0 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 380 6 2 5 4.3 Cc1cc(O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
57390243 67565 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 383 6 0 5 3.7 COCC/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910802 67565 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 383 6 0 5 3.7 COCC/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
11222939 67218 6 None -9 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.02.006
44438254 67218 6 None -9 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.02.006
CHEMBL190006 67218 6 None -9 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.02.006
66655583 167004 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4210576 167004 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300642 167004 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3Cl)ccc12 10.1016/j.bmcl.2017.12.018
66655587 167064 0 None 5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)ccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4205714 167064 0 None 5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)ccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301563 167064 0 None 5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)ccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
68082485 166948 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 8 1 4 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(OCCCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4207162 166948 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 8 1 4 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(OCCCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300006 166948 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 8 1 4 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(OCCCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
59384375 103898 0 None -4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 510 13 3 6 5.9 CCCCCCCCOc1ccc(-c2cnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F 10.1021/ml400194r
CHEMBL3102903 103898 0 None -4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 510 13 3 6 5.9 CCCCCCCCOc1ccc(-c2cnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F 10.1021/ml400194r
46881847 6965 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1084929 6965 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
77847681 182698 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 409 5 1 3 5.6 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4796939 182698 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 409 5 1 3 5.6 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
66655236 167115 0 None 50 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 445 7 1 4 5.4 CCc1cccc(Cl)c1CSc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4210019 167115 0 None 50 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 445 7 1 4 5.4 CCc1cccc(Cl)c1CSc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4302167 167115 0 None 50 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 445 7 1 4 5.4 CCc1cccc(Cl)c1CSc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
11222939 67218 6 None -9 4 Human 8.5 pEC50 = 8.5 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
44438254 67218 6 None -9 4 Human 8.5 pEC50 = 8.5 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL190006 67218 6 None -9 4 Human 8.5 pEC50 = 8.5 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
58344778 153988 0 None -117 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 153988 0 None -117 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 153988 0 None -117 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
44412661 139000 0 None -14 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1cnc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL379612 139000 0 None -14 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1cnc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
46866185 7236 0 None -10 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 321 12 2 3 4.2 CCCCCCCOc1ccc(CC[C@](C)(N)CC(=O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1086172 7236 0 None -10 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 321 12 2 3 4.2 CCCCCCCOc1ccc(CC[C@](C)(N)CC(=O)O)cc1 10.1016/j.bmcl.2010.01.118
44138103 75416 0 None -131 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment 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 75416 0 None -131 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment 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
11676168 70591 9 None -19 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 422 11 3 5 3.3 Cc1ccc(CCCC(=O)c2ccc(CC[C@@](C)(N)COP(=O)(O)O)n2C)cc1 10.1021/ml100301k
CHEMBL1951588 70591 9 None -19 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 422 11 3 5 3.3 Cc1ccc(CCCC(=O)c2ccc(CC[C@@](C)(N)COP(=O)(O)O)n2C)cc1 10.1021/ml100301k
44438261 93414 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](CO)N[C@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
44438262 93414 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](CO)N[C@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL247901 93414 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](CO)N[C@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
11646599 77298 0 None -1047 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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 77298 0 None -1047 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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
10311 1262 34 None -37 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 405 5 0 5 3.9 COCCN=C1S/C(=C\c2cc(n(c2C)c2ccc(cc2F)F)C)/C(=O)N1C 10.1016/j.bmcl.2011.09.049
49835928 1262 34 None -37 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 405 5 0 5 3.9 COCCN=C1S/C(=C\c2cc(n(c2C)c2ccc(cc2F)F)C)/C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910803 1262 34 None -37 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 405 5 0 5 3.9 COCCN=C1S/C(=C\c2cc(n(c2C)c2ccc(cc2F)F)C)/C(=O)N1C 10.1016/j.bmcl.2011.09.049
57397321 67554 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 403 5 0 4 4.7 CC/N=C1\S/C(=C\c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
CHEMBL1910690 67554 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 403 5 0 4 4.7 CC/N=C1\S/C(=C\c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
11632823 137830 0 None -234 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1ccc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL377181 137830 0 None -234 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1ccc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
77846755 181290 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 381 5 1 3 5.2 Cc1cc(OC2CCCCC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4778961 181290 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 381 5 1 3 5.2 Cc1cc(OC2CCCCC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
49835989 67547 1 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 353 4 0 4 4.4 CC/N=C1\S/C(=C\c2cc(C)n(-c3ccccc3)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
CHEMBL1910681 67547 1 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 353 4 0 4 4.4 CC/N=C1\S/C(=C\c2cc(C)n(-c3ccccc3)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
11626664 77560 0 None -239 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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 77560 0 None -239 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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
11177439 67535 0 None -239 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 413 7 4 3 3.6 N[C@H](CNC(=O)c1cc2c(-c3ccccc3Cc3ccccc3)cccc2[nH]1)C(=O)O 10.1016/j.bmcl.2011.09.049
CHEMBL1910654 67535 0 None -239 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 413 7 4 3 3.6 N[C@H](CNC(=O)c1cc2c(-c3ccccc3Cc3ccccc3)cccc2[nH]1)C(=O)O 10.1016/j.bmcl.2011.09.049
66655406 166977 0 None 50 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 5.2 CC(C)c1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4205333 166977 0 None 50 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 5.2 CC(C)c1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4300295 166977 0 None 50 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 5.2 CC(C)c1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
66655633 167027 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 3 1 3 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4213894 167027 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 3 1 3 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300915 167027 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 3 1 3 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
25182621 6178 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 326 4 3 5 3.5 Cc1cc(O)ccc1NC(=O)c1cc(NC2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1081654 6178 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 326 4 3 5 3.5 Cc1cc(O)ccc1NC(=O)c1cc(NC2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
44412867 79317 0 None -660 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 420 7 1 5 5.1 CCOc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F 10.1016/j.bmcl.2006.04.084
CHEMBL211689 79317 0 None -660 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 420 7 1 5 5.1 CCOc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F 10.1016/j.bmcl.2006.04.084
44412868 79339 0 None -812 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 406 6 1 5 4.8 COc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F 10.1016/j.bmcl.2006.04.084
CHEMBL211806 79339 0 None -812 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 406 6 1 5 4.8 COc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F 10.1016/j.bmcl.2006.04.084
44412908 77215 0 None -109 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 318 3 0 3 5.8 Cc1ccccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL208786 77215 0 None -109 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 318 3 0 3 5.8 Cc1ccccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
76955634 182852 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 383 6 2 3 5.3 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4798888 182852 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 383 6 2 3 5.3 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
11682696 79520 0 None -245 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 396 8 1 6 4.5 COc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C 10.1016/j.bmcl.2006.04.084
CHEMBL212580 79520 0 None -245 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 396 8 1 6 4.5 COc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C 10.1016/j.bmcl.2006.04.084
69263869 104217 0 None -63 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P5 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
ChEMBL 436 6 1 5 6.0 CCc1cc(-c2noc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)n2)cc(C)c1CCC(=O)O 10.1021/jm4014373
CHEMBL3105479 104217 0 None -63 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P5 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
ChEMBL 436 6 1 5 6.0 CCc1cc(-c2noc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)n2)cc(C)c1CCC(=O)O 10.1021/jm4014373
24825339 91320 0 None -66 3 Human 7.5 pEC50 = 7.5 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 392 7 1 7 3.8 Cc1nc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL241052 91320 0 None -66 3 Human 7.5 pEC50 = 7.5 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 392 7 1 7 3.8 Cc1nc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
46866186 7235 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 307 11 2 3 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)C(=O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1086171 7235 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 307 11 2 3 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)C(=O)O)cc1 10.1016/j.bmcl.2010.01.118
44138103 75416 0 None -131 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment 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 75416 0 None -131 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment 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
44600476 57087 6 None -14 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assayAgonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assay
ChEMBL 459 6 1 5 5.1 O=C(O)C1CN(Cc2ccc(-c3nc4ccc(C5(c6ccccc6)CC5)nc4s3)c(F)c2)C1 10.1021/ml100306h
CHEMBL1651861 57087 6 None -14 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assayAgonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assay
ChEMBL 459 6 1 5 5.1 O=C(O)C1CN(Cc2ccc(-c3nc4ccc(C5(c6ccccc6)CC5)nc4s3)c(F)c2)C1 10.1021/ml100306h
44412971 138392 0 None -102 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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 138392 0 None -102 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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
2924 1602 37 None -4 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
44398069 1602 37 None -4 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
9908268 1602 37 None -4 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
CHEMBL114606 1602 37 None -4 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
118877433 176756 0 None -14 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 459 8 3 4 4.5 COc1ccccc1CC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.8b01695
CHEMBL4637401 176756 0 None -14 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 459 8 3 4 4.5 COc1ccccc1CC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.8b01695
118877603 179838 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 425 10 3 4 4.1 COCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
CHEMBL4752394 179838 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 425 10 3 4 4.1 COCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
77846507 179177 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 6 1 3 6.4 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(CC(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4744455 179177 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 6 1 3 6.4 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(CC(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
11496072 145479 0 None -32 3 Human 8.4 pEC50 = 8.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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 145479 0 None -32 3 Human 8.4 pEC50 = 8.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
44422601 85141 0 None -8 5 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 398 14 4 3 4.2 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL228139 85141 0 None -8 5 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 398 14 4 3 4.2 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
44422605 85135 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 329 11 3 3 3.1 CCCCCCc1ccc(OC[C@@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL228103 85135 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 329 11 3 3 3.1 CCCCCCc1ccc(OC[C@@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
66655585 166944 0 None 199 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 421 5 1 4 4.4 O=C(O)CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4209307 166944 0 None 199 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 421 5 1 4 4.4 O=C(O)CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4299904 166944 0 None 199 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 421 5 1 4 4.4 O=C(O)CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
66655579 166981 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCCN(CCC(=O)O)C1 10.1016/j.bmcl.2017.12.018
CHEMBL4206573 166981 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCCN(CCC(=O)O)C1 10.1016/j.bmcl.2017.12.018
CHEMBL4300331 166981 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCCN(CCC(=O)O)C1 10.1016/j.bmcl.2017.12.018
145947321 167094 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 436 6 1 5 4.2 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)nc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4218094 167094 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 436 6 1 5 4.2 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)nc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301951 167094 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 436 6 1 5 4.2 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)nc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
66655208 167111 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4210080 167111 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302153 167111 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
107970 1601 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
2407 1601 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
4167 1601 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
CHEMBL314854 1601 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
DB08868 1601 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
67194420 142468 0 None -645 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 142468 0 None -645 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
25192001 7961 0 None -2 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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 7961 0 None -2 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq 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
44412604 137865 0 None -10 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1cc(-c2ccc(OC(C)C)c(C#N)c2)cs1 10.1016/j.bmcl.2006.04.064
CHEMBL377339 137865 0 None -10 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1cc(-c2ccc(OC(C)C)c(C#N)c2)cs1 10.1016/j.bmcl.2006.04.064
44412605 139011 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1csc(-c2ccc(OC(C)C)c(C#N)c2)c1 10.1016/j.bmcl.2006.04.064
CHEMBL379660 139011 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1csc(-c2ccc(OC(C)C)c(C#N)c2)c1 10.1016/j.bmcl.2006.04.064
46224714 197567 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 360 2 0 3 4.9 Cc1nn(C(=O)/C=C/c2cccc(C(F)(F)F)c2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL590134 197567 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 360 2 0 3 4.9 Cc1nn(C(=O)/C=C/c2cccc(C(F)(F)F)c2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
11545181 3940 4 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
2930 3940 4 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
CHEMBL389033 3940 4 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
90660718 59654 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1509, AID1523, AID1563, AID1686, AID1701, AID1801, AID463107, AID463225, AID504400]PUBCHEM_BIOASSAY: Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1509, AID1523, AID1563, AID1686, AID1701, AID1801, AID463107, AID463225, AID504400]
ChEMBL 391 4 0 5 3.9 C/N=C1\S/C(=C/c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1OC nan
CHEMBL1734070 59654 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1509, AID1523, AID1563, AID1686, AID1701, AID1801, AID463107, AID463225, AID504400]PUBCHEM_BIOASSAY: Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1509, AID1523, AID1563, AID1686, AID1701, AID1801, AID463107, AID463225, AID504400]
ChEMBL 391 4 0 5 3.9 C/N=C1\S/C(=C/c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1OC nan
57400714 67553 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 375 3 0 4 4.0 C/N=C1\S/C(=C\c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910689 67553 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 375 3 0 4 4.0 C/N=C1\S/C(=C\c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
57390238 67546 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 377 2 0 4 4.4 C/N=C1\S/C(=C\c2cc(C)n(-c3ccc(Cl)cc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910680 67546 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 377 2 0 4 4.4 C/N=C1\S/C(=C\c2cc(C)n(-c3ccc(Cl)cc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
46224768 197609 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 293 2 0 4 3.2 Cc1nn(C(=O)/C=C/c2cccnc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL590384 197609 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 293 2 0 4 3.2 Cc1nn(C(=O)/C=C/c2cccnc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
77846675 178825 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 457 5 1 3 6.8 CC(C)(C)[C@H]1CC[C@H](Oc2cc(Cl)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4740175 178825 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 457 5 1 3 6.8 CC(C)(C)[C@H]1CC[C@H](Oc2cc(Cl)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
46881877 7011 0 None -5 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 359 13 2 5 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)CCc2nnn[nH]2)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1085191 7011 0 None -5 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 359 13 2 5 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)CCc2nnn[nH]2)cc1 10.1016/j.bmcl.2010.01.118
57398998 67555 0 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 375 3 0 4 4.0 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccc(F)cc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910691 67555 0 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 375 3 0 4 4.0 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccc(F)cc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
44439852 93400 0 None -47 2 Human 7.4 pEC50 = 7.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
CHEMBL247766 93400 0 None -47 2 Human 7.4 pEC50 = 7.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
77847766 180921 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 5 1 3 6.8 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(C)(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4765011 180921 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 5 1 3 6.8 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(C)(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
58344502 142301 0 None -398 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 142301 0 None -398 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
66655999 167082 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 361 3 1 3 3.3 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4208055 167082 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 361 3 1 3 3.3 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301752 167082 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 361 3 1 3 3.3 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
2924 1602 37 None -4 7 Human 8.4 pEC50 = 8.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmc.2006.10.060
44398069 1602 37 None -4 7 Human 8.4 pEC50 = 8.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmc.2006.10.060
9908268 1602 37 None -4 7 Human 8.4 pEC50 = 8.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmc.2006.10.060
CHEMBL114606 1602 37 None -4 7 Human 8.4 pEC50 = 8.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmc.2006.10.060
46872626 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
9496 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741589 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
52938427 2924 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
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 2924 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
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 2924 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
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 2924 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
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 2924 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
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
2924 1602 37 None -4 7 Human 8.3 pEC50 = 8.3 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 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)CCC(COP(=O)(O)O)(CO)N 10.1021/jm050242f
44398069 1602 37 None -4 7 Human 8.3 pEC50 = 8.3 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 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)CCC(COP(=O)(O)O)(CO)N 10.1021/jm050242f
9908268 1602 37 None -4 7 Human 8.3 pEC50 = 8.3 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 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)CCC(COP(=O)(O)O)(CO)N 10.1021/jm050242f
CHEMBL114606 1602 37 None -4 7 Human 8.3 pEC50 = 8.3 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 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)CCC(COP(=O)(O)O)(CO)N 10.1021/jm050242f
118877584 181861 0 None -7 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 411 9 3 4 3.7 CCOCCC[C@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
CHEMBL4786296 181861 0 None -7 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 411 9 3 4 3.7 CCOCCC[C@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
24825338 77342 0 None -467 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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 77342 0 None -467 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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
24825338 77342 0 None -467 3 Human 7.4 pEC50 = 7.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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 77342 0 None -467 3 Human 7.4 pEC50 = 7.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
44412854 165367 0 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 376 5 1 4 5.4 Cc1cc(CC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL425058 165367 0 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 376 5 1 4 5.4 Cc1cc(CC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
90318298 178991 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 371 13 2 3 5.5 CCCCCCCCOc1cc(C)c2ccccc2c1CNCCC(=O)O 10.1021/acsmedchemlett.0c00631
CHEMBL4742052 178991 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 371 13 2 3 5.5 CCCCCCCCOc1cc(C)c2ccccc2c1CNCCC(=O)O 10.1021/acsmedchemlett.0c00631
44422579 85140 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 356 13 4 3 3.9 CCCCCCCCc1cccc(NC[C@H](N)CCP(=O)(O)O)c1 10.1016/j.bmc.2006.10.060
CHEMBL228138 85140 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 356 13 4 3 3.9 CCCCCCCCc1cccc(NC[C@H](N)CCP(=O)(O)O)c1 10.1016/j.bmc.2006.10.060
44412578 77763 0 None -26 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-c1nnn(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL210345 77763 0 None -26 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-c1nnn(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
11575913 77753 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 444 7 1 5 5.3 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Br)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL210316 77753 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 444 7 1 5 5.3 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Br)c2)n1 10.1016/j.bmcl.2006.04.084
54764919 69543 36 None -123 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human S1P5 expressed in CHO-K1 cells coexpressing Gq/i5 assessed as calcium mobilization-induced bioluminescence change measured for 90 secs by fluorimetryAgonist activity at human S1P5 expressed in CHO-K1 cells coexpressing Gq/i5 assessed as calcium mobilization-induced bioluminescence change measured for 90 secs by fluorimetry
ChEMBL 415 4 2 4 4.7 COc1ccncc1C(=O)NC(=O)Nc1ccc(-c2ccccc2)c(C(F)(F)F)c1 10.1021/ml2001399
CHEMBL1938952 69543 36 None -123 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human S1P5 expressed in CHO-K1 cells coexpressing Gq/i5 assessed as calcium mobilization-induced bioluminescence change measured for 90 secs by fluorimetryAgonist activity at human S1P5 expressed in CHO-K1 cells coexpressing Gq/i5 assessed as calcium mobilization-induced bioluminescence change measured for 90 secs by fluorimetry
ChEMBL 415 4 2 4 4.7 COc1ccncc1C(=O)NC(=O)Nc1ccc(-c2ccccc2)c(C(F)(F)F)c1 10.1021/ml2001399
16038017 138875 0 None -398 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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 138875 0 None -398 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 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
52938426 3312 8 None -70 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 3312 8 None -70 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 3312 8 None -70 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
44412621 77977 0 None -416 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)o1 10.1016/j.bmcl.2006.04.064
CHEMBL211081 77977 0 None -416 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)o1 10.1016/j.bmcl.2006.04.064
44422606 85133 0 None 2 5 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 329 11 3 3 3.1 CCCCCCc1ccc(OC[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL228049 85133 0 None 2 5 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 329 11 3 3 3.1 CCCCCCc1ccc(OC[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
44342175 85081 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL227371 85081 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL422074 85081 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
67196597 147418 0 None -562 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 147418 0 None -562 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
44439850 145482 0 None -24 3 Human 8.3 pEC50 = 8.3 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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 145482 0 None -24 3 Human 8.3 pEC50 = 8.3 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
44439851 145102 0 None -37 3 Human 8.3 pEC50 = 8.3 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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 145102 0 None -37 3 Human 8.3 pEC50 = 8.3 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
46872626 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
9496 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741589 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
44438259 93381 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](COP(=O)(O)O)N[C@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
44438260 93381 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](COP(=O)(O)O)N[C@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL247699 93381 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](COP(=O)(O)O)N[C@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
44406009 72349 0 None -10 4 Human 7.3 pEC50 = 7.3 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 515 18 5 10 3.4 N[C@@H](COP(=O)(O)O)[C@H](O)/C=C/CCCCCCCCCCNc1ccc([N+](=O)[O-])c2nonc12 10.1016/j.bmcl.2005.09.038
CHEMBL199754 72349 0 None -10 4 Human 7.3 pEC50 = 7.3 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 515 18 5 10 3.4 N[C@@H](COP(=O)(O)O)[C@H](O)/C=C/CCCCCCCCCCNc1ccc([N+](=O)[O-])c2nonc12 10.1016/j.bmcl.2005.09.038
46224769 199148 0 None -251 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 331 2 1 3 4.3 Cc1nn(C(=O)/C=C/c2cccc3[nH]ccc23)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL601062 199148 0 None -251 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 331 2 1 3 4.3 Cc1nn(C(=O)/C=C/c2cccc3[nH]ccc23)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
57397320 67552 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 357 3 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910688 67552 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 357 3 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
11588811 3937 39 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](COP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
136212600 3937 39 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](COP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
3324 3937 39 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](COP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
CHEMBL228102 3937 39 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](COP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
11501873 139604 0 None -275 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 384 7 1 5 4.7 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(F)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL380253 139604 0 None -275 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 384 7 1 5 4.7 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(F)c2)n1 10.1016/j.bmcl.2006.04.084
52938427 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 145564 0 None -354 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 145564 0 None -354 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
58344715 142529 0 None -575 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 142529 0 None -575 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
11224984 8614 18 None -13 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 460 8 2 6 4.3 CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C 10.1021/jm100181s
CHEMBL1095833 8614 18 None -13 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 460 8 2 6 4.3 CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C 10.1021/jm100181s
44412882 76920 0 None -1174 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 390 6 1 4 5.8 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL208168 76920 0 None -1174 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 390 6 1 4 5.8 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
25182926 7844 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 451 11 3 6 3.8 O=C(O)CCNCc1ccc(NC(=O)c2cc(N(CC3CC3)C3CCCCC3)ncn2)cc1 10.1016/j.bmcl.2010.01.102
CHEMBL1090423 7844 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 451 11 3 6 3.8 O=C(O)CCNCc1ccc(NC(=O)c2cc(N(CC3CC3)C3CCCCC3)ncn2)cc1 10.1016/j.bmcl.2010.01.102
66655775 167113 0 None 158 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 453 6 1 4 4.9 O=C(O)CCN1CCC2(CC1)COc1c2ccc(OCc2c(Cl)cccc2Cl)c1F 10.1016/j.bmcl.2017.12.018
CHEMBL4208771 167113 0 None 158 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 453 6 1 4 4.9 O=C(O)CCN1CCC2(CC1)COc1c2ccc(OCc2c(Cl)cccc2Cl)c1F 10.1016/j.bmcl.2017.12.018
CHEMBL4302165 167113 0 None 158 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 453 6 1 4 4.9 O=C(O)CCN1CCC2(CC1)COc1c2ccc(OCc2c(Cl)cccc2Cl)c1F 10.1016/j.bmcl.2017.12.018
11689680 79215 0 None -102 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
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.2006.04.084
CHEMBL211505 79215 0 None -102 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
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.2006.04.084
11689680 79215 0 None -102 3 Human 8.2 pEC50 = 8.2 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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 79215 0 None -102 3 Human 8.2 pEC50 = 8.2 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
90318624 180743 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 5 1 3 6.1 CC(C)(C)[C@H]1CC[C@H](Oc2ccc3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4762836 180743 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 5 1 3 6.1 CC(C)(C)[C@H]1CC[C@H](Oc2ccc3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
57395471 67563 0 None -58 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 389 4 0 4 4.7 CC/N=C1\S/C(=C\c2cc(C)n(-c3ccc(F)cc3F)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
CHEMBL1910800 67563 0 None -58 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 389 4 0 4 4.7 CC/N=C1\S/C(=C\c2cc(C)n(-c3ccc(F)cc3F)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
45377662 83688 0 None -204 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
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 83688 0 None -204 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
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
56601979 167097 0 None 19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.0 CC(CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12)C(=O)O 10.1016/j.bmcl.2017.12.018
CHEMBL4217349 167097 0 None 19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.0 CC(CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12)C(=O)O 10.1016/j.bmcl.2017.12.018
CHEMBL4301966 167097 0 None 19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.0 CC(CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12)C(=O)O 10.1016/j.bmcl.2017.12.018
66655050 167129 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 419 6 1 4 4.3 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(F)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4207361 167129 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 419 6 1 4 4.3 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(F)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302356 167129 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 419 6 1 4 4.3 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(F)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
11452022 3526 33 None -3 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm200609t
6996 3526 33 None -3 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm200609t
CHEMBL366208 3526 33 None -3 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm200609t
57398996 67543 1 None -1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 343 2 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(-c3ccc(F)cc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910674 67543 1 None -1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 343 2 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(-c3ccc(F)cc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
77846591 181293 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 7 1 3 6.8 CCC(C)(C)[C@H]1CC[C@H](Oc2cc(C)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4779029 181293 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 7 1 3 6.8 CCC(C)(C)[C@H]1CC[C@H](Oc2cc(C)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
66655836 166987 0 None 39 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.1 Cc1cc(Cl)c(COc2ccc3c(c2)OCC32CCN(CCC(=O)O)CC2)c(Cl)c1 10.1016/j.bmcl.2017.12.018
CHEMBL4213167 166987 0 None 39 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.1 Cc1cc(Cl)c(COc2ccc3c(c2)OCC32CCN(CCC(=O)O)CC2)c(Cl)c1 10.1016/j.bmcl.2017.12.018
CHEMBL4300404 166987 0 None 39 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.1 Cc1cc(Cl)c(COc2ccc3c(c2)OCC32CCN(CCC(=O)O)CC2)c(Cl)c1 10.1016/j.bmcl.2017.12.018
1776080 67536 7 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 343 2 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(-c3ccccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910655 67536 7 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 343 2 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(-c3ccccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
11603726 76462 0 None -588 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 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 76462 0 None -588 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 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
44422573 85117 0 None -2 4 Human 7.1 pEC50 = 7.1 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1ccc(NC(=O)[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL227851 85117 0 None -2 4 Human 7.1 pEC50 = 7.1 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1ccc(NC(=O)[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
58344692 144377 0 None -758 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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 144377 0 None -758 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of 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
145948099 167146 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 5 1 5 3.8 O=C(O)CN1CCC2(CC1)COc1cc(S(=O)(=O)Cc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4209494 167146 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 5 1 5 3.8 O=C(O)CN1CCC2(CC1)COc1cc(S(=O)(=O)Cc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302573 167146 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 5 1 5 3.8 O=C(O)CN1CCC2(CC1)COc1cc(S(=O)(=O)Cc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
136212602 11633 7 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 369 11 4 4 3.6 CCCCCCCCc1ccc2nc([C@@H](N)COP(=O)(O)O)[nH]c2c1 10.1016/j.bmcl.2011.09.049
44394498 11633 7 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 369 11 4 4 3.6 CCCCCCCCc1ccc2nc([C@@H](N)COP(=O)(O)O)[nH]c2c1 10.1016/j.bmcl.2011.09.049
CHEMBL1181619 11633 7 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 369 11 4 4 3.6 CCCCCCCCc1ccc2nc([C@@H](N)COP(=O)(O)O)[nH]c2c1 10.1016/j.bmcl.2011.09.049
CHEMBL1910653 11633 7 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 369 11 4 4 3.6 CCCCCCCCc1ccc2nc([C@@H](N)COP(=O)(O)O)[nH]c2c1 10.1016/j.bmcl.2011.09.049
46224715 197568 0 None -7 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 371 3 1 5 2.5 Cc1nn(C(=O)/C=C/c2cccc(S(N)(=O)=O)c2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL590135 197568 0 None -7 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 371 3 1 5 2.5 Cc1nn(C(=O)/C=C/c2cccc(S(N)(=O)=O)c2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
11611053 77574 0 None -912 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 401 7 1 5 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C(F)(F)C(C)C)cn2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL209567 77574 0 None -912 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 401 7 1 5 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C(F)(F)C(C)C)cn2)n1 10.1016/j.bmcl.2006.04.084
44412883 76929 0 None -58 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 404 7 1 4 6.2 Cc1cc(CCCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL208224 76929 0 None -58 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 404 7 1 4 6.2 Cc1cc(CCCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
44547414 67986 0 None -67 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assayAgonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assay
ChEMBL 499 5 1 5 5.2 O=C(O)CCC(=O)N1CCc2cc(-c3noc(-c4cc(C(F)(F)F)cc(C(F)(F)F)c4)n3)ccc21 10.1016/j.bmcl.2011.05.110
CHEMBL1916559 67986 0 None -67 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assayAgonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assay
ChEMBL 499 5 1 5 5.2 O=C(O)CCC(=O)N1CCc2cc(-c3noc(-c4cc(C(F)(F)F)cc(C(F)(F)F)c4)n3)ccc21 10.1016/j.bmcl.2011.05.110
44439851 145102 0 None -37 3 Human 7.1 pEC50 = 7.1 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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 145102 0 None -37 3 Human 7.1 pEC50 = 7.1 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
11662328 91319 0 None -33 3 Human 8.0 pEC50 = 8 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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 91319 0 None -33 3 Human 8.0 pEC50 = 8 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 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
46224712 199108 0 None -35 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 352 4 0 5 3.9 COc1ccc(/C=C/C(=O)n2nc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc1OC 10.1016/j.bmcl.2009.11.045
CHEMBL600762 199108 0 None -35 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 352 4 0 5 3.9 COc1ccc(/C=C/C(=O)n2nc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc1OC 10.1016/j.bmcl.2009.11.045
11697013 77857 0 None -1318 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL210695 77857 0 None -1318 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.064
11697013 77857 0 None -1318 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL210695 77857 0 None -1318 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
25182773 7530 0 None -53 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 443 7 2 6 3.2 Cc1cc(S(N)(=O)=O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1088177 7530 0 None -53 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 443 7 2 6 3.2 Cc1cc(S(N)(=O)=O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
44607575 52252 0 None -69 5 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 375 4 1 3 5.8 COc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 nan
CHEMBL1592119 52252 0 None -69 5 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 375 4 1 3 5.8 COc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 nan
44607577 43630 0 None -120 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 415 5 1 2 7.8 CC(C)c1cccc(C(C)C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 nan
CHEMBL1511839 43630 0 None -120 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 415 5 1 2 7.8 CC(C)c1cccc(C(C)C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 nan
2328694 53431 2 None -8 5 Human 5.9 pIC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 408 6 2 3 5.2 O=C(Nc1ccccc1)Nc1cc(OCC(F)(F)F)cc(OCC(F)(F)F)c1 nan
CHEMBL1603615 53431 2 None -8 5 Human 5.9 pIC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 408 6 2 3 5.2 O=C(Nc1ccccc1)Nc1cc(OCC(F)(F)F)cc(OCC(F)(F)F)c1 nan
46872388 136235 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 303 8 1 3 3.4 CCCCCC(=O)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3741172 136235 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 303 8 1 3 3.4 CCCCCC(=O)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
4492589 30677 7 None -181 4 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at S1P5 receptorAntagonist activity at S1P5 receptor
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.06.132
CHEMBL1397874 30677 7 None -181 4 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at S1P5 receptorAntagonist activity at S1P5 receptor
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.06.132
44607578 52053 0 None -45 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 379 7 1 4 5.5 CCOc1ccc(OC)cc1-c1ccc(C(=O)Nc2c(C)cccc2CC)o1 nan
CHEMBL1589684 52053 0 None -45 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 379 7 1 4 5.5 CCOc1ccc(OC)cc1-c1ccc(C(=O)Nc2c(C)cccc2CC)o1 nan
59451874 136110 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 289 8 1 3 3.0 CCCCCC(=O)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740009 136110 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 289 8 1 3 3.0 CCCCCC(=O)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
46872386 136060 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 323 6 1 3 3.0 O=C(Cc1ccccc1)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739593 136060 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 323 6 1 3 3.0 O=C(Cc1ccccc1)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451795 136170 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 309 6 1 3 2.6 O=C(Cc1ccccc1)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740604 136170 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 309 6 1 3 2.6 O=C(Cc1ccccc1)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
6217704 32352 3 None 7 6 Human 7.5 pIC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 490 7 0 8 5.2 CCOC(=O)/C(=C\c1ccc(OC(F)F)cc1)C1=Nn2c(nnc2-c2ccc(Cl)cc2)SC1 nan
CHEMBL1412583 32352 3 None 7 6 Human 7.5 pIC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 490 7 0 8 5.2 CCOC(=O)/C(=C\c1ccc(OC(F)F)cc1)C1=Nn2c(nnc2-c2ccc(Cl)cc2)SC1 nan
59451808 136210 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 317 9 1 3 3.7 CCCCCCC(=O)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740964 136210 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 317 9 1 3 3.7 CCCCCCC(=O)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
46872389 136093 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 303 9 1 3 3.4 CCCCCCC(=O)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739887 136093 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 303 9 1 3 3.4 CCCCCCC(=O)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451857 136129 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 391 6 1 3 4.3 O=C(Cc1ccc(Cl)c(Cl)c1)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740180 136129 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 391 6 1 3 4.3 O=C(Cc1ccc(Cl)c(Cl)c1)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451852 136326 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 377 6 1 3 3.9 O=C(Cc1ccc(Cl)c(Cl)c1)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3741988 136326 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 377 6 1 3 3.9 O=C(Cc1ccc(Cl)c(Cl)c1)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
1363299 32709 10 None -37 5 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2ccc(Cl)cc2Cl)o1 nan
CHEMBL1415555 32709 10 None -37 5 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2ccc(Cl)cc2Cl)o1 nan
71450073 82163 0 None -288 4 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human S1P5R receptor expressed in CHO cell membranes by [35S]GTPgamma binding assayAntagonist activity at human S1P5R receptor expressed in CHO cell membranes by [35S]GTPgamma binding assay
ChEMBL 585 10 2 5 5.5 Cc1cc(S(=O)(=O)Nc2cccc(-c3cc(C)c(C(=O)N(C)[C@@H](CCN(C)C)C(=O)O)c(C)c3)c2)c(C)cc1Cl 10.1021/jm3009508
CHEMBL2178814 82163 0 None -288 4 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human S1P5R receptor expressed in CHO cell membranes by [35S]GTPgamma binding assayAntagonist activity at human S1P5R receptor expressed in CHO cell membranes by [35S]GTPgamma binding assay
ChEMBL 585 10 2 5 5.5 Cc1cc(S(=O)(=O)Nc2cccc(-c3cc(C)c(C(=O)N(C)[C@@H](CCN(C)C)C(=O)O)c(C)c3)c2)c(C)cc1Cl 10.1021/jm3009508
11363176 3088 42 None -3 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C None
5446 3088 42 None -3 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C None
9320 3088 42 None -3 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C None
CHEMBL1096146 3088 42 None -3 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C None
52938427 2924 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
5383 2924 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
8709 2924 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
CHEMBL3707247 2924 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
DB12612 2924 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
44599207 3539 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
5326 3539 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
9289 3539 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
CHEMBL2336071 3539 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
DB12371 3539 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
107970 1601 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
2407 1601 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
4167 1601 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
CHEMBL314854 1601 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
DB08868 1601 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
52938426 3312 8 None -70 5 Human 8.2 pEC50 = 8.2 Functional
As measured in a GTPγS assay.As measured in a GTPγS assay.
Guide to Pharmacology 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N 29608575
9889 3312 8 None -70 5 Human 8.2 pEC50 = 8.2 Functional
As measured in a GTPγS assay.As measured in a GTPγS assay.
Guide to Pharmacology 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N 29608575
CHEMBL3899384 3312 8 None -70 5 Human 8.2 pEC50 = 8.2 Functional
As measured in a GTPγS assay.As measured in a GTPγS assay.
Guide to Pharmacology 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N 29608575
44623998 1560 33 None -75 8 Human 7.6 pEC50 = 7.6 Functional
In a β-arrestin recruitment assay.In a β-arrestin recruitment assay.
Guide to Pharmacology 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 25516790
9331 1560 33 None -75 8 Human 7.6 pEC50 = 7.6 Functional
In a β-arrestin recruitment assay.In a β-arrestin recruitment assay.
Guide to Pharmacology 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 25516790
CHEMBL3358920 1560 33 None -75 8 Human 7.6 pEC50 = 7.6 Functional
In a β-arrestin recruitment assay.In a β-arrestin recruitment assay.
Guide to Pharmacology 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 25516790
DB14766 1560 33 None -75 8 Human 7.6 pEC50 = 7.6 Functional
In a β-arrestin recruitment assay.In a β-arrestin recruitment assay.
Guide to Pharmacology 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 25516790
46872626 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
46872626 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 29688337
9496 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
9496 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 29688337
CHEMBL3741589 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
CHEMBL3741589 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 29688337
52938427 2924 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
5383 2924 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
8709 2924 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
CHEMBL3707247 2924 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
DB12612 2924 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
44599207 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
44599207 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
44599207 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
5326 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
5326 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
5326 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
9289 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
9289 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
9289 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
CHEMBL2336071 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
CHEMBL2336071 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
CHEMBL2336071 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
DB12371 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
DB12371 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
DB12371 3539 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
16755143 499 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
In a GTP&gamma;S binding assay.In a GTP&gamma;S binding assay.
Guide to Pharmacology 442 4 1 5 5.6 C[C@@H](C(F)(F)F)Oc1ccc(cc1C(F)(F)F)c1onc(n1)c1ccc2c(c1)nc[nH]2 25347187
9569 499 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
In a GTP&gamma;S binding assay.In a GTP&gamma;S binding assay.
Guide to Pharmacology 442 4 1 5 5.6 C[C@@H](C(F)(F)F)Oc1ccc(cc1C(F)(F)F)c1onc(n1)c1ccc2c(c1)nc[nH]2 25347187
CHEMBL4297350 499 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
In a GTP&gamma;S binding assay.In a GTP&gamma;S binding assay.
Guide to Pharmacology 442 4 1 5 5.6 C[C@@H](C(F)(F)F)Oc1ccc(cc1C(F)(F)F)c1onc(n1)c1ccc2c(c1)nc[nH]2 25347187
DB11819 499 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
In a GTP&gamma;S binding assay.In a GTP&gamma;S binding assay.
Guide to Pharmacology 442 4 1 5 5.6 C[C@@H](C(F)(F)F)Oc1ccc(cc1C(F)(F)F)c1onc(n1)c1ccc2c(c1)nc[nH]2 25347187
46872626 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
9496 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
CHEMBL3741589 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
49848557 1077 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
In an aequorin calcium accumulation assay.In an aequorin calcium accumulation assay.
Guide to Pharmacology 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 26751273
9492 1077 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
In an aequorin calcium accumulation assay.In an aequorin calcium accumulation assay.
Guide to Pharmacology 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 26751273
CHEMBL3769933 1077 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
In an aequorin calcium accumulation assay.In an aequorin calcium accumulation assay.
Guide to Pharmacology 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 26751273
11259583 520 12 None -380 7 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
2925 520 12 None -380 7 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
CHEMBL4579553 520 12 None -380 7 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
11311 1839 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 440 8 1 7 5.1 OC(=O)CCCn1ccc2c1cccc2c1noc(n1)c1cnc(c(c1)Cl)OC(C)C 27128606
24988201 1839 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 440 8 1 7 5.1 OC(=O)CCCn1ccc2c1cccc2c1noc(n1)c1cnc(c(c1)Cl)OC(C)C 27128606
CHEMBL4297542 1839 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 440 8 1 7 5.1 OC(=O)CCCn1ccc2c1cccc2c1noc(n1)c1cnc(c(c1)Cl)OC(C)C 27128606
DB11987 1839 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 440 8 1 7 5.1 OC(=O)CCCn1ccc2c1cccc2c1noc(n1)c1cnc(c(c1)Cl)OC(C)C 27128606
52938427 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
5383 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
8709 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
CHEMBL3707247 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
DB12612 2924 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
10883396 3579 39 None -12 15 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
10883396 3579 39 None -12 15 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
5283560 3579 39 None -12 15 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
5283560 3579 39 None -12 15 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
911 3579 39 None -12 15 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
911 3579 39 None -12 15 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
CHEMBL225155 3579 39 None -12 15 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
CHEMBL225155 3579 39 None -12 15 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
10883396 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
10883396 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11967257
10883396 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
10883396 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 17114004
5283560 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
5283560 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11967257
5283560 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
5283560 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 17114004
911 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
911 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11967257
911 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
911 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 17114004
CHEMBL225155 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
CHEMBL225155 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11967257
CHEMBL225155 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
CHEMBL225155 3579 39 None -2 15 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 17114004
6992 3934 0 None 7 2 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 369 11 3 3 4.3 CCCCCCCCc1cccc(c1)C1CC(C1)(N)COP(=O)(O)O 21632869
73755254 3934 0 None 7 2 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 369 11 3 3 4.3 CCCCCCCCc1cccc(c1)C1CC(C1)(N)COP(=O)(O)O 21632869
10904818 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 11967257
10904818 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 14732717
2937 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 11967257
2937 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 14732717
CHEMBL382739 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 11967257
CHEMBL382739 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 14732717
2924 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 11967257
2924 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
2924 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 17114004
44398069 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 11967257
44398069 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
44398069 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 17114004
9908268 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 11967257
9908268 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
9908268 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 17114004
CHEMBL114606 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 11967257
CHEMBL114606 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
CHEMBL114606 1602 37 None -4 7 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 17114004
11259583 520 12 None -354 7 Mouse 6.5 pEC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
2925 520 12 None -354 7 Mouse 6.5 pEC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
CHEMBL4579553 520 12 None -354 7 Mouse 6.5 pEC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
11545181 3940 4 None -1 3 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 17113298
2930 3940 4 None -1 3 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 17113298
CHEMBL389033 3940 4 None -1 3 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 17113298
12573 978 1 None - 1 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 33738061
77846592 978 1 None - 1 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 33738061
CHEMBL4748198 978 1 None - 1 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 33738061
107970 1601 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
2407 1601 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
4167 1601 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
CHEMBL314854 1601 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
DB08868 1601 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
2924 1602 37 None -4 7 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
44398069 1602 37 None -4 7 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
9908268 1602 37 None -4 7 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
CHEMBL114606 1602 37 None -4 7 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
10430549 1029 33 None -1 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 16190743
2929 1029 33 None -1 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 16190743
CHEMBL194419 1029 33 None -1 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 16190743


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
10883396 3579 39 None - 4 Human 9.7 pEC50 = 9.7 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
5283560 3579 39 None - 4 Human 9.7 pEC50 = 9.7 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
911 3579 39 None - 4 Human 9.7 pEC50 = 9.7 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
CHEMBL225155 3579 39 None - 4 Human 9.7 pEC50 = 9.7 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
107970 1601 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
2407 1601 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
4167 1601 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
CHEMBL314854 1601 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
DB08868 1601 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
49868651 170572 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assay
ChEMBL 542 8 2 8 5.3 O=C(O)C[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1 10.1021/acs.jmedchem.6b00373
CHEMBL4458575 170572 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assay
ChEMBL 542 8 2 8 5.3 O=C(O)C[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1 10.1021/acs.jmedchem.6b00373
50925337 169874 6 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assay
ChEMBL 528 7 2 8 4.9 O=C(O)[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1 10.1021/acs.jmedchem.6b00373
CHEMBL4448752 169874 6 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assay
ChEMBL 528 7 2 8 4.9 O=C(O)[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1 10.1021/acs.jmedchem.6b00373
10883396 3579 39 None - 4 Human 8.8 pEC50 = 8.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2004.07.030
5283560 3579 39 None - 4 Human 8.8 pEC50 = 8.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2004.07.030
911 3579 39 None - 4 Human 8.8 pEC50 = 8.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2004.07.030
CHEMBL225155 3579 39 None - 4 Human 8.8 pEC50 = 8.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2004.07.030
134130131 141743 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1cccc(-c2cccc3cc(CNCCCC(=O)O)sc23)c1 10.1016/j.bmcl.2016.11.050
CHEMBL3885151 141743 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1cccc(-c2cccc3cc(CNCCCC(=O)O)sc23)c1 10.1016/j.bmcl.2016.11.050
46174905 115775 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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 115775 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
134129958 141736 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3885074 141736 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
44342468 11997 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1184089 11997 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL332050 11997 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
11682677 11662 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181748 11662 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL190865 11662 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
44342231 11979 3 None - 0 Human 5.9 pEC50 = 5.9 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 408 19 4 4 4.0 CCCCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL1183950 11979 3 None - 0 Human 5.9 pEC50 = 5.9 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 408 19 4 4 4.0 CCCCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL325408 11979 3 None - 0 Human 5.9 pEC50 = 5.9 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 408 19 4 4 4.0 CCCCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
134131071 141577 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883377 141577 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
134130884 141606 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883572 141606 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
134131188 141754 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 354 7 3 4 3.6 CCc1ccccc1-c1cccc2cc(CNCC(N)C(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885229 141754 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 354 7 3 4 3.6 CCc1ccccc1-c1cccc2cc(CNCC(N)C(=O)O)sc12 10.1016/j.bmcl.2016.11.050
44398049 13052 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 441 13 5 5 3.4 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1190950 13052 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 441 13 5 5 3.4 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL541890 13052 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 441 13 5 5 3.4 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
44342331 11296 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 428 16 4 4 4.5 CCCCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL116953 11296 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 428 16 4 4 4.5 CCCCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1180214 11296 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 428 16 4 4 4.5 CCCCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
44342244 64530 3 None - 0 Human 5.8 pEC50 = 5.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 380 17 4 4 3.2 CCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL182164 64530 3 None - 0 Human 5.8 pEC50 = 5.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 380 17 4 4 3.2 CCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL423691 64530 3 None - 0 Human 5.8 pEC50 = 5.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 380 17 4 4 3.2 CCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
134130571 141673 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)c1 10.1016/j.bmcl.2016.11.050
CHEMBL3884292 141673 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)c1 10.1016/j.bmcl.2016.11.050
44398076 12776 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 13 5 5 3.2 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1188968 12776 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 13 5 5 3.2 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL537849 12776 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 13 5 5 3.2 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
134131598 141726 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3c(-c4ccc5ccccc5c4)cccc3s2)C1 10.1016/j.bmcl.2016.11.050
CHEMBL3884966 141726 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3c(-c4ccc5ccccc5c4)cccc3s2)C1 10.1016/j.bmcl.2016.11.050
53362086 115842 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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 115842 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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
134131470 141751 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2cc(CNc3ccc(CC(=O)O)cc3)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885195 141751 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2cc(CNc3ccc(CC(=O)O)cc3)sc12 10.1016/j.bmcl.2016.11.050
134130538 141617 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 351 5 1 3 4.6 CCc1ccccc1-c1cccc2sc(CN3CC(C(=O)O)C3)cc12 10.1016/j.bmcl.2016.11.050
CHEMBL3883646 141617 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 351 5 1 3 4.6 CCc1ccccc1-c1cccc2sc(CN3CC(C(=O)O)C3)cc12 10.1016/j.bmcl.2016.11.050
134131301 141618 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3c(-c4ccc5ccccc5c4)cccc3s2)c1 10.1016/j.bmcl.2016.11.050
CHEMBL3883658 141618 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3c(-c4ccc5ccccc5c4)cccc3s2)c1 10.1016/j.bmcl.2016.11.050
124171453 136789 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 473 6 0 7 4.5 Cc1nc(CC(C)C)cc(-c2nc(-c3cc(F)c(O[C@@H]4CCC(=O)N(C)C4)cc3Cl)no2)n1 10.1016/j.bmcl.2015.11.090
CHEMBL3752660 136789 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 473 6 0 7 4.5 Cc1nc(CC(C)C)cc(-c2nc(-c3cc(F)c(O[C@@H]4CCC(=O)N(C)C4)cc3Cl)no2)n1 10.1016/j.bmcl.2015.11.090
134130169 141609 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3cc(-c4ccc5ccccc5c4)ccc3s2)C1 10.1016/j.bmcl.2016.11.050
CHEMBL3883597 141609 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3cc(-c4ccc5ccccc5c4)ccc3s2)C1 10.1016/j.bmcl.2016.11.050
134130662 141730 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 6 2 3 5.5 CC(CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3884995 141730 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 6 2 3 5.5 CC(CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
134130114 141727 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2cccc(-c3cccc4ccccc34)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884986 141727 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2cccc(-c3cccc4ccccc34)c2s1 10.1016/j.bmcl.2016.11.050
44623998 1560 33 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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 1560 33 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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 1560 33 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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 1560 33 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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
44394564 12137 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL1184660 12137 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL363076 12137 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
134130188 141648 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 367 9 2 3 5.5 CCc1ccccc1-c1cccc2cc(CNCCCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3884048 141648 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 367 9 2 3 5.5 CCc1ccccc1-c1cccc2cc(CNCCCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
134130519 141637 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883972 141637 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
134130022 141666 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.7 CCc1ccccc1-c1cccc2cc(CNCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3884172 141666 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.7 CCc1ccccc1-c1cccc2cc(CNCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
11675907 11656 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 409 12 4 4 4.3 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181694 11656 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 409 12 4 4 4.3 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL188881 11656 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 409 12 4 4 4.3 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
134130111 141759 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3885275 141759 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
134131081 141594 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883456 141594 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
134130375 141658 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1ccc(-c2cccc3cc(CNCCCC(=O)O)sc23)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3884099 141658 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1ccc(-c2cccc3cc(CNCCCC(=O)O)sc23)cc1 10.1016/j.bmcl.2016.11.050
44398170 11652 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 411 12 4 4 4.2 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181688 11652 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 411 12 4 4 4.2 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL188826 11652 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 411 12 4 4 4.2 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
134130732 141650 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 393 7 2 3 5.5 O=C(O)CCCNCc1cc2cccc(-c3cccc(C(F)(F)F)c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884056 141650 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 393 7 2 3 5.5 O=C(O)CCCNCc1cc2cccc(-c3cccc(C(F)(F)F)c3)c2s1 10.1016/j.bmcl.2016.11.050
134130546 141625 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883812 141625 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
134131256 141633 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 369 7 2 5 4.3 O=C(O)CCCNCc1cc2cccc(-c3ccc4c(c3)OCO4)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883947 141633 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 369 7 2 5 4.3 O=C(O)CCCNCc1cc2cccc(-c3ccc4c(c3)OCO4)c2s1 10.1016/j.bmcl.2016.11.050
134130150 141595 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3883471 141595 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
124171444 136872 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 435 7 1 7 4.0 Cc1cc(-c2nc(-c3cc(C)c(OC[C@@H]4CCC(=O)N4)c(C)n3)no2)cc(CC(C)C)n1 10.1016/j.bmcl.2015.11.090
CHEMBL3753300 136872 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 435 7 1 7 4.0 Cc1cc(-c2nc(-c3cc(C)c(OC[C@@H]4CCC(=O)N4)c(C)n3)no2)cc(CC(C)C)n1 10.1016/j.bmcl.2015.11.090
124171442 136911 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 422 6 2 8 3.3 Cc1cc(-c2nc(-c3ccc(O[C@H]4CCC(=O)NC4)c(C)n3)no2)cc(NC(C)C)n1 10.1016/j.bmcl.2015.11.090
CHEMBL3753609 136911 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 422 6 2 8 3.3 Cc1cc(-c2nc(-c3ccc(O[C@H]4CCC(=O)NC4)c(C)n3)no2)cc(NC(C)C)n1 10.1016/j.bmcl.2015.11.090
134130316 141778 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3885468 141778 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
134131399 141771 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1ccccc1-c1cccc2cc(CNCCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885401 141771 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1ccccc1-c1cccc2cc(CNCCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
134130548 141645 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 6.7 O=C(O)c1ccc(CNCc2cc3c(-c4ccc5ccccc5c4)cccc3s2)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3884011 141645 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 6.7 O=C(O)c1ccc(CNCc2cc3c(-c4ccc5ccccc5c4)cccc3s2)cc1 10.1016/j.bmcl.2016.11.050
124171447 136893 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 425 6 1 7 3.5 Cc1nc(CC(C)C)cc(-c2nc(-c3ccc(O[C@@H]4CCC(=O)NC4)c(F)c3)no2)n1 10.1016/j.bmcl.2015.11.090
CHEMBL3753479 136893 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 425 6 1 7 3.5 Cc1nc(CC(C)C)cc(-c2nc(-c3ccc(O[C@@H]4CCC(=O)NC4)c(F)c3)no2)n1 10.1016/j.bmcl.2015.11.090
44398058 11646 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181660 11646 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL187712 11646 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
124221654 1100 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 OC(=O)CCCNCc1cc2c(s1)c(ccc2)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2016.11.050
9495 1100 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 OC(=O)CCCNCc1cc2c(s1)c(ccc2)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2016.11.050
CHEMBL3884038 1100 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 OC(=O)CCCNCc1cc2c(s1)c(ccc2)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2016.11.050
44394289 12288 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 3.7 CCCCCCCCc1ccc2[nH]c(C(C)(N)COP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL1185803 12288 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 3.7 CCCCCCCCc1ccc2[nH]c(C(C)(N)COP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL433593 12288 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 3.7 CCCCCCCCc1ccc2[nH]c(C(C)(N)COP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
44394521 11641 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL1181640 11641 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL186815 11641 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
134131209 141774 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2cc(CNc3cccc(CC(=O)O)c3)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885415 141774 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2cc(CNc3cccc(CC(=O)O)c3)sc12 10.1016/j.bmcl.2016.11.050
2924 1602 37 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2005.05.097
44398069 1602 37 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2005.05.097
9908268 1602 37 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2005.05.097
CHEMBL114606 1602 37 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2005.05.097
134131067 141641 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1ccc(NCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3883991 141641 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1ccc(NCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)cc1 10.1016/j.bmcl.2016.11.050
10023913 12012 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 400 14 4 4 3.7 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1184130 12012 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 400 14 4 4 3.7 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL334038 12012 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 400 14 4 4 3.7 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
67249162 115839 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359520 115839 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
134129983 141604 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883555 141604 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
134130146 141581 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 353 7 2 3 4.9 CCc1ccccc1-c1cccc2cc(CNCC(C)C(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3883401 141581 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 353 7 2 3 4.9 CCc1ccccc1-c1cccc2cc(CNCC(C)C(=O)O)sc12 10.1016/j.bmcl.2016.11.050
44342219 11291 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL115344 11291 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1180152 11291 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
10883396 3579 39 None - 4 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
5283560 3579 39 None - 4 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
911 3579 39 None - 4 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
CHEMBL225155 3579 39 None - 4 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
134130183 141624 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 6.7 O=C(O)c1ccc(CNCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3883805 141624 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 6.7 O=C(O)c1ccc(CNCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)cc1 10.1016/j.bmcl.2016.11.050
134131169 141719 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 381 7 2 3 5.8 CC(C)(C)c1ccc(-c2cccc3cc(CNCCCC(=O)O)sc23)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3884888 141719 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 381 7 2 3 5.8 CC(C)(C)c1ccc(-c2cccc3cc(CNCCCC(=O)O)sc23)cc1 10.1016/j.bmcl.2016.11.050
67250226 115841 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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 115841 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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
134131475 141643 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2sc(CNc3ccc(CC(=O)O)cc3)cc12 10.1016/j.bmcl.2016.11.050
CHEMBL3883998 141643 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2sc(CNc3ccc(CC(=O)O)cc3)cc12 10.1016/j.bmcl.2016.11.050
134130066 141709 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 8 2 3 6.2 O=C(O)CCCNCc1cc2cccc(-c3cccc(-c4ccccc4)c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884809 141709 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 8 2 3 6.2 O=C(O)CCCNCc1cc2cccc(-c3cccc(-c4ccccc4)c3)c2s1 10.1016/j.bmcl.2016.11.050
49839234 117435 1 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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 117435 1 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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
134131291 141607 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3cccc(-c4ccc5ccccc5c4)c3s2)C1 10.1016/j.bmcl.2016.11.050
CHEMBL3883579 141607 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3cccc(-c4ccc5ccccc5c4)c3s2)C1 10.1016/j.bmcl.2016.11.050
134130695 141592 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883447 141592 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
44398012 12143 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 12 4 4 4.4 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1184707 12143 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 12 4 4 4.4 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL364950 12143 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 12 4 4 4.4 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
44342175 85081 0 None - 2 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL227371 85081 0 None - 2 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL422074 85081 0 None - 2 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
44342339 11286 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL114031 11286 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1180115 11286 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
134131363 141706 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 393 7 2 3 5.5 O=C(O)CCCNCc1cc2cccc(-c3ccc(C(F)(F)F)cc3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884795 141706 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 393 7 2 3 5.5 O=C(O)CCCNCc1cc2cccc(-c3ccc(C(F)(F)F)cc3)c2s1 10.1016/j.bmcl.2016.11.050
44394497 66346 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 497 11 4 6 4.3 CCCCCCCCc1ccc2[nH]c([C@@H](N)COP(=O)(O)O)nc2c1.COC(=O)C(F)(F)F 10.1016/j.bmcl.2004.07.030
CHEMBL185491 66346 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 497 11 4 6 4.3 CCCCCCCCc1ccc2[nH]c([C@@H](N)COP(=O)(O)O)nc2c1.COC(=O)C(F)(F)F 10.1016/j.bmcl.2004.07.030
134131381 141765 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3885331 141765 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
44342221 11972 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determinedIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determined
ChEMBL 352 15 4 4 2.5 CCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL1183918 11972 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determinedIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determined
ChEMBL 352 15 4 4 2.5 CCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL324358 11972 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determinedIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determined
ChEMBL 352 15 4 4 2.5 CCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
134130947 141685 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 8 2 3 6.2 O=C(O)CCCNCc1cc2cccc(-c3ccc(-c4ccccc4)cc3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884580 141685 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 8 2 3 6.2 O=C(O)CCCNCc1cc2cccc(-c3ccc(-c4ccccc4)cc3)c2s1 10.1016/j.bmcl.2016.11.050
134131043 141734 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.1 CCc1ccccc1-c1cccc2sc(CNCc3ccc(C(=O)O)cc3)cc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885068 141734 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.1 CCc1ccccc1-c1cccc2sc(CNCc3ccc(C(=O)O)cc3)cc12 10.1016/j.bmcl.2016.11.050
44398074 12762 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 345 11 4 4 3.1 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1188885 12762 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 345 11 4 4 3.1 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL537632 12762 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 345 11 4 4 3.1 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
134131297 141613 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883621 141613 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
134130023 141667 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3884173 141667 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
66829311 139266 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at S1PR5 (unknown origin)Agonist activity at S1PR5 (unknown origin)
ChEMBL 530 13 3 9 3.6 CCc1cc(-c2noc(-c3cc(C)c(CN(C)CC(C)C)s3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.048
CHEMBL3798837 139266 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at S1PR5 (unknown origin)Agonist activity at S1PR5 (unknown origin)
ChEMBL 530 13 3 9 3.6 CCc1cc(-c2noc(-c3cc(C)c(CN(C)CC(C)C)s3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.048
134131316 141655 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3cc(-c4ccc5ccccc5c4)ccc3s2)c1 10.1016/j.bmcl.2016.11.050
CHEMBL3884077 141655 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3cc(-c4ccc5ccccc5c4)ccc3s2)c1 10.1016/j.bmcl.2016.11.050
44394327 11632 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 4.0 CCCCCCCCc1ccc2[nH]c([C@@H](N)[C@@H](C)OP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL1181601 11632 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 4.0 CCCCCCCCc1ccc2[nH]c([C@@H](N)[C@@H](C)OP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL183894 11632 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 4.0 CCCCCCCCc1ccc2[nH]c([C@@H](N)[C@@H](C)OP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
44394459 123107 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 497 11 4 6 4.3 CCCCCCCCc1ccc2[nH]c([C@H](N)COP(=O)(O)O)nc2c1.COC(=O)C(F)(F)F 10.1016/j.bmcl.2004.07.030
CHEMBL361915 123107 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 497 11 4 6 4.3 CCCCCCCCc1ccc2[nH]c([C@H](N)COP(=O)(O)O)nc2c1.COC(=O)C(F)(F)F 10.1016/j.bmcl.2004.07.030
46174905 115775 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment 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 115775 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
44398172 11659 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 315 10 3 3 4.0 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181739 11659 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 315 10 3 3 4.0 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL190529 11659 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 315 10 3 3 4.0 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
134130192 141660 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 6 2 3 5.5 CC(CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3884134 141660 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 6 2 3 5.5 CC(CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
10883396 3579 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding 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.2005.05.097
5283560 3579 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding 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.2005.05.097
911 3579 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding 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.2005.05.097
CHEMBL225155 3579 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding 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.2005.05.097
10883396 3579 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
5283560 3579 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
911 3579 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
CHEMBL225155 3579 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
67249162 115839 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359520 115839 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
11743459 140247 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 431 7 1 5 4.4 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL381872 140247 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 431 7 1 5 4.4 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1 10.1021/jm0503244
11575787 70273 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 439 6 1 5 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL195014 70273 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 439 6 1 5 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1021/jm0503244
11604577 71966 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 439 6 1 5 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc([C@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL198415 71966 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 439 6 1 5 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc([C@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1021/jm0503244
10408874 72130 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 403 6 1 5 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCCC5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL198976 72130 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 403 6 1 5 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCCC5)cc4)n3)cc2)C1 10.1021/jm0503244
10883396 3579 39 None - 4 Human 9.3 pIC50 = 9.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm0492507
5283560 3579 39 None - 4 Human 9.3 pIC50 = 9.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm0492507
911 3579 39 None - 4 Human 9.3 pIC50 = 9.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm0492507
CHEMBL225155 3579 39 None - 4 Human 9.3 pIC50 = 9.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm0492507
44394191 65962 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 381 12 3 2 5.3 CCCCCCCCCc1ccc(C2CCC(CCP(=O)(O)O)N2)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL184879 65962 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 381 12 3 2 5.3 CCCCCCCCCc1ccc(C2CCC(CCP(=O)(O)O)N2)cc1 10.1016/j.bmcl.2004.07.049
44394191 65962 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 381 12 3 2 5.3 CCCCCCCCCc1ccc(C2CCC(CCP(=O)(O)O)N2)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL184879 65962 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 381 12 3 2 5.3 CCCCCCCCCc1ccc(C2CCC(CCP(=O)(O)O)N2)cc1 10.1016/j.bmcl.2004.07.049
2924 1602 37 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
44398069 1602 37 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
9908268 1602 37 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
CHEMBL114606 1602 37 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
46905530 10180 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 14 5 6 2.6 CCCCCCCCc1ccc(CCC(N)(CO)CO[PH](O)(O)O)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL1161691 10180 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 14 5 6 2.6 CCCCCCCCc1ccc(CCC(N)(CO)CO[PH](O)(O)O)cc1 10.1016/j.bmcl.2004.07.049
9979368 71347 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 417 6 1 5 5.0 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL196534 71347 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 417 6 1 5 5.0 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)C1 10.1021/jm0503244
10430549 1029 33 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1021/jm0503244
2929 1029 33 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1021/jm0503244
CHEMBL194419 1029 33 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1021/jm0503244
10045980 69482 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 8 1 5 4.3 CCCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL193789 69482 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 8 1 5 4.3 CCCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
49830722 71395 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 379 6 1 3 4.1 Cc1cc(OCc2cccc(C(F)(F)F)c2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1966501 71395 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 379 6 1 3 4.1 Cc1cc(OCc2cccc(C(F)(F)F)c2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
49830919 71632 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 363 6 1 2 4.0 O=C(O)C1CN(Cc2ccc(CCc3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1973936 71632 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 363 6 1 2 4.0 O=C(O)C1CN(Cc2ccc(CCc3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
46872619 72142 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 379 6 1 3 4.4 Cc1cc(OCc2ccc(Cl)c(Cl)c2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1990223 72142 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 379 6 1 3 4.4 Cc1cc(OCc2ccc(Cl)c(Cl)c2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
127037695 136039 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 333 12 1 3 4.3 CCCCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739440 136039 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 333 12 1 3 4.3 CCCCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451793 136226 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 399 6 1 3 4.5 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)c(Cl)c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741092 136226 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 399 6 1 3 4.5 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)c(Cl)c2)C1 10.1021/acs.jmedchem.5b00928
10430549 1029 33 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1016/j.bmcl.2006.03.090
2929 1029 33 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1016/j.bmcl.2006.03.090
CHEMBL194419 1029 33 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1016/j.bmcl.2006.03.090
10883396 3579 39 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2008.11.072
5283560 3579 39 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2008.11.072
911 3579 39 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2008.11.072
CHEMBL225155 3579 39 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2008.11.072
44591266 178710 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 443 13 4 5 4.2 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1F 10.1016/j.bmcl.2008.11.072
CHEMBL473269 178710 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 443 13 4 5 4.2 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1F 10.1016/j.bmcl.2008.11.072
44394273 64232 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 395 12 3 2 5.6 CCCCCCCCCc1ccc(CN[C@H]2CCC[C@H](P(=O)(O)O)C2)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL181597 64232 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 395 12 3 2 5.6 CCCCCCCCCc1ccc(CN[C@H]2CCC[C@H](P(=O)(O)O)C2)cc1 10.1016/j.bmcl.2004.07.049
44591265 179391 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 425 13 4 5 4.1 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2008.11.072
CHEMBL474689 179391 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 425 13 4 5 4.1 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2008.11.072
10317453 70060 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 377 7 1 5 3.9 CCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL194578 70060 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 377 7 1 5 3.9 CCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
10363915 134657 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 405 7 1 5 4.6 CCC(C)(C)c1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL372066 134657 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 405 7 1 5 4.6 CCC(C)(C)c1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
59451812 136353 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 331 6 1 3 3.4 O=C(O)C1CN(Cc2ccc(OCc3cccc(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3742245 136353 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 331 6 1 3 3.4 O=C(O)C1CN(Cc2ccc(OCc3cccc(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
59451770 136363 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 277 8 1 3 2.8 CCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3742304 136363 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 277 8 1 3 2.8 CCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
10127776 10935 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 465 15 3 4 4.9 CCCCCCCCOc1c(Br)cc(CNCCCP(=O)(O)O)cc1OC 10.1021/jm0492507
CHEMBL117723 10935 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 465 15 3 4 4.9 CCCCCCCCOc1c(Br)cc(CNCCCP(=O)(O)O)cc1OC 10.1021/jm0492507
11271470 137046 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 475 8 1 4 6.1 CCc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
CHEMBL375488 137046 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 475 8 1 4 6.1 CCc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
44412282 77878 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 405 7 2 5 4.9 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](CC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL210785 77878 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 405 7 2 5 4.9 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](CC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
11502026 71095 0 None - 0 Human 6.0 pIC50 = 6 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2nnc(-c3ccc(CN4CC(C(=O)O)C4)cc3)o2)cc1 10.1021/jm0503244
CHEMBL196149 71095 0 None - 0 Human 6.0 pIC50 = 6 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2nnc(-c3ccc(CN4CC(C(=O)O)C4)cc3)o2)cc1 10.1021/jm0503244
11683935 178751 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 456 9 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL473563 178751 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 456 9 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
59451878 136159 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.3 C[C@@H](Oc1ccc(CN2CC(C(=O)O)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740494 136159 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.3 C[C@@H](Oc1ccc(CN2CC(C(=O)O)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.5b00928
10251062 70278 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 411 6 1 5 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(-c5ccccc5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL195025 70278 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 411 6 1 5 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(-c5ccccc5)cc4)n3)cc2)C1 10.1021/jm0503244
44413349 77271 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 453 6 2 5 5.4 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL208838 77271 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 453 6 2 5 5.4 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
10149721 84659 4 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 317 11 1 2 4.5 CCCCCCCCCc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/jm0492507
CHEMBL224623 84659 4 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 317 11 1 2 4.5 CCCCCCCCCc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/jm0492507
44394220 66653 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 15 3 2 5.8 CCCCCCCCCCCCCCNC1CCCC(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
CHEMBL186921 66653 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 15 3 2 5.8 CCCCCCCCCCCCCCNC1CCCC(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
59451743 136241 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 361 7 1 4 3.4 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1ccccc1Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741222 136241 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 361 7 1 4 3.4 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1ccccc1Cl 10.1021/acs.jmedchem.5b00928
10249979 71287 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 393 7 1 6 3.7 CC(C)Oc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL196357 71287 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 393 7 1 6 3.7 CC(C)Oc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
11603220 134645 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 375 6 1 5 3.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CC5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL371985 134645 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 375 6 1 5 3.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CC5)cc4)n3)cc2)C1 10.1021/jm0503244
11408903 84688 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 475 7 1 4 6.1 Cc1cc(CN2CC(C(=O)O)C2)cc(C)c1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
CHEMBL224853 84688 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 475 7 1 4 6.1 Cc1cc(CN2CC(C(=O)O)C2)cc(C)c1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
44565738 189151 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 445 11 4 5 3.8 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCCCc3ccccc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
CHEMBL515917 189151 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 445 11 4 5 3.8 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCCCc3ccccc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
10195325 84682 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.9 O=C(O)C1CCN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1021/jm0492507
CHEMBL224799 84682 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.9 O=C(O)C1CCN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1021/jm0492507
46872748 136339 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC[C@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3742107 136339 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC[C@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
11540052 179975 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL475405 179975 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
59451751 136185 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC[C@@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740739 136185 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC[C@@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
44412221 76742 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 391 6 2 5 4.5 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](C(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL207580 76742 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 391 6 2 5 4.5 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](C(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
44412165 77393 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL209076 77393 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
10288527 84591 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.8 Cc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
CHEMBL224005 84591 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.8 Cc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
44344193 114401 5 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 335 17 3 2 4.8 CCCCCCCCCCCCCCNCCCP(=O)(O)O 10.1021/jm0492507
CHEMBL334213 114401 5 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 335 17 3 2 4.8 CCCCCCCCCCCCCCNCCCP(=O)(O)O 10.1021/jm0492507
44344193 114401 5 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 335 17 3 2 4.8 CCCCCCCCCCCCCCNCCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL334213 114401 5 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 335 17 3 2 4.8 CCCCCCCCCCCCCCNCCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
44413274 138169 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 447 6 2 4 5.7 O=C(O)C1CNC(c2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL377968 138169 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 447 6 2 4 5.7 O=C(O)C1CNC(c2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
44394220 66653 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 15 3 2 5.8 CCCCCCCCCCCCCCNC1CCCC(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
CHEMBL186921 66653 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 15 3 2 5.8 CCCCCCCCCCCCCCNC1CCCC(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
11503967 7924 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 482 10 4 5 3.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(C(=O)CCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2010.02.098
CHEMBL1090796 7924 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 482 10 4 5 3.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(C(=O)CCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2010.02.098
44413430 138227 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 405 7 2 5 4.7 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4C[C@@H](CC(=O)O)CN4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.090
CHEMBL378061 138227 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 405 7 2 5 4.7 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4C[C@@H](CC(=O)O)CN4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.090
4492589 30677 7 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.04.097
CHEMBL1397874 30677 7 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.04.097
11224984 8614 18 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 460 8 2 6 4.3 CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C 10.1021/jm100181s
CHEMBL1095833 8614 18 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 460 8 2 6 4.3 CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C 10.1021/jm100181s
59451867 136253 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 4.2 O=C(O)C1CN(Cc2ccc(-c3cc(Cl)cc(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741338 136253 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 4.2 O=C(O)C1CN(Cc2ccc(-c3cc(Cl)cc(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
44412165 77393 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL209076 77393 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
44394212 66819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 373 15 2 2 6.5 CCCCCCCCCCCCCC1CCCC(CCP(C)(=O)O)N1 10.1016/j.bmcl.2004.07.049
CHEMBL187692 66819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 373 15 2 2 6.5 CCCCCCCCCCCCCC1CCCC(CCP(C)(=O)O)N1 10.1016/j.bmcl.2004.07.049
44412364 77734 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL210257 77734 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
46872874 136079 2 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC(C(=O)O)CC2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739759 136079 2 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC(C(=O)O)CC2)cc1 10.1021/acs.jmedchem.5b00928
59451883 136299 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 295 6 1 2 3.0 O=C(O)C1CN(Cc2ccc(CCc3ccccc3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741743 136299 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 295 6 1 2 3.0 O=C(O)C1CN(Cc2ccc(CCc3ccccc3)cc2)C1 10.1021/acs.jmedchem.5b00928
10174255 84779 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
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 84779 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
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
44394279 66799 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 16 3 2 5.8 CCCCCCCCCCCCCC[C@H]1CC[C@H](CCP(=O)(O)O)N1 10.1016/j.bmcl.2004.07.049
CHEMBL187588 66799 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 16 3 2 5.8 CCCCCCCCCCCCCC[C@H]1CC[C@H](CCP(=O)(O)O)N1 10.1016/j.bmcl.2004.07.049
10217498 84648 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 481 7 1 4 6.2 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1 10.1021/jm0492507
CHEMBL224571 84648 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 481 7 1 4 6.2 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1 10.1021/jm0492507
44412232 165756 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 391 6 2 5 4.5 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](C(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL427221 165756 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 391 6 2 5 4.5 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](C(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
46885798 7934 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 561 10 4 5 5.7 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1 10.1016/j.bmcl.2010.02.098
CHEMBL1090829 7934 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 561 10 4 5 5.7 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1 10.1016/j.bmcl.2010.02.098
44412165 77393 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL209076 77393 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
49830724 72025 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 399 6 1 3 4.5 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2Cl)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1986265 72025 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 399 6 1 3 4.5 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2Cl)C1 10.1021/acs.jmedchem.5b00928
49830723 72372 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 3.9 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2F)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1998478 72372 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 3.9 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2F)C1 10.1021/acs.jmedchem.5b00928
59451819 136280 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 3.9 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741572 136280 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 3.9 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
10883396 3579 39 None - 4 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.098
5283560 3579 39 None - 4 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.098
911 3579 39 None - 4 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.098
CHEMBL225155 3579 39 None - 4 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.098
10287034 65837 3 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 367 11 2 2 4.7 CCCCCCCCCc1ccc(CN2CCC(P(=O)(O)O)C2)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL184349 65837 3 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 367 11 2 2 4.7 CCCCCCCCCc1ccc(CN2CCC(P(=O)(O)O)C2)cc1 10.1016/j.bmcl.2004.07.049
44565597 178697 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 436 12 4 5 3.2 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCCc2ccccc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL473156 178697 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 436 12 4 5 3.2 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCCc2ccccc2)cc1 10.1016/j.bmcl.2009.02.073
11696807 125423 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2noc(-c3ccc(CN4CC(C(=O)O)C4)cc3)n2)cc1 10.1021/jm0503244
CHEMBL364899 125423 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2noc(-c3ccc(CN4CC(C(=O)O)C4)cc3)n2)cc1 10.1021/jm0503244
44412416 77812 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 431 6 2 5 5.7 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL210520 77812 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 431 6 2 5 5.7 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
44412233 77768 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 405 7 2 5 4.9 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](CC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL210352 77768 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 405 7 2 5 4.9 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](CC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
44565716 179153 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 493 10 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
CHEMBL474418 179153 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 493 10 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
44413365 77014 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 467 6 2 5 5.8 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCC(F)(F)CC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL208648 77014 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 467 6 2 5 5.8 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCC(F)(F)CC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
11168252 84646 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 515 7 1 4 6.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(C(F)(F)F)c2)C1 10.1021/jm0492507
CHEMBL224549 84646 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 515 7 1 4 6.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(C(F)(F)F)c2)C1 10.1021/jm0492507
107970 1601 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
2407 1601 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
4167 1601 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
CHEMBL314854 1601 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
DB08868 1601 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
59451797 136366 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 4.2 O=C(O)C1CN(Cc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3742345 136366 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 4.2 O=C(O)C1CN(Cc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
10127475 165465 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL425563 165465 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
10127475 165465 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1021/jm0492507
CHEMBL425563 165465 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1021/jm0492507
44394161 66675 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 16 2 2 6.1 CCCCCCCCCCCCCC1CCCCN1CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL187061 66675 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 16 2 2 6.1 CCCCCCCCCCCCCC1CCCCN1CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
44394116 66003 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 349 17 2 2 5.2 CCCCCCCCCCCCCCN(C)CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL185100 66003 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 349 17 2 2 5.2 CCCCCCCCCCCCCCN(C)CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
46872507 136131 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.3 CC(Oc1ccc(CN2CC(C(=O)O)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740188 136131 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.3 CC(Oc1ccc(CN2CC(C(=O)O)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.5b00928
59451779 136049 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 9 1 3 3.6 CCCCCCOc1ccc(CN2CC[C@@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739509 136049 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 9 1 3 3.6 CCCCCCOc1ccc(CN2CC[C@@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
44565622 178750 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 428 11 4 5 3.6 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCC2CCCCC2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL473562 178750 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 428 11 4 5 3.6 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCC2CCCCC2)cc1 10.1016/j.bmcl.2009.02.073
44394211 66812 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 14 2 3 5.4 CCCCCCCCCCCCCCN1CCC(O)(P(C)(=O)O)CC1 10.1016/j.bmcl.2004.07.049
CHEMBL187645 66812 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 14 2 3 5.4 CCCCCCCCCCCCCCN1CCC(O)(P(C)(=O)O)CC1 10.1016/j.bmcl.2004.07.049
46872872 136106 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 333 9 1 3 4.2 CCCCCCOc1ccc(CN2CCC(C(=O)O)C(C)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739964 136106 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 333 9 1 3 4.2 CCCCCCOc1ccc(CN2CCC(C(=O)O)C(C)C2)cc1 10.1021/acs.jmedchem.5b00928
10215259 84669 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 331 11 1 2 4.9 CCCCCCCCCc1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/jm0492507
CHEMBL224703 84669 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 331 11 1 2 4.9 CCCCCCCCCc1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/jm0492507
59451870 136123 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 277 7 1 3 2.6 CC(C)CCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740090 136123 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 277 7 1 3 2.6 CC(C)CCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451813 136151 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 295 5 1 2 3.4 CCc1ccc(-c2ccc(CN3CC(C(=O)O)C3)cc2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740359 136151 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 295 5 1 2 3.4 CCc1ccc(-c2ccc(CN3CC(C(=O)O)C3)cc2)cc1 10.1021/acs.jmedchem.5b00928
10883396 3579 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counterDisplacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1039/d1md00357g
5283560 3579 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counterDisplacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1039/d1md00357g
911 3579 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counterDisplacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1039/d1md00357g
CHEMBL225155 3579 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counterDisplacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1039/d1md00357g
10883396 3579 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting methodDisplacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2017.12.010
5283560 3579 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting methodDisplacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2017.12.010
911 3579 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting methodDisplacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2017.12.010
CHEMBL225155 3579 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting methodDisplacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2017.12.010
44591264 179389 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)c(F)c1 10.1016/j.bmcl.2008.11.072
CHEMBL474688 179389 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)c(F)c1 10.1016/j.bmcl.2008.11.072
44565739 178372 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 459 12 4 5 4.2 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCCCCc3ccccc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
CHEMBL470511 178372 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 459 12 4 5 4.2 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCCCCc3ccccc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
44412294 138107 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 419 8 2 5 5.3 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](CCC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL377637 138107 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 419 8 2 5 5.3 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](CCC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
44412353 165664 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 435 6 2 5 5.5 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)c(F)c4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL426688 165664 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 435 6 2 5 5.5 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)c(F)c4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
11495139 138362 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 405 7 2 5 4.7 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4C[C@H](CC(=O)O)CN4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.090
CHEMBL378300 138362 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 405 7 2 5 4.7 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4C[C@H](CC(=O)O)CN4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.090
54582607 62115 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 375 3 2 3 5.8 Cc1cc(O)cc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.04.097
CHEMBL1779895 62115 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 375 3 2 3 5.8 Cc1cc(O)cc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.04.097
11752659 165580 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 515 7 1 4 6.8 O=C(O)C1CN(Cc2cc(Cl)c(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1 10.1021/jm0492507
CHEMBL426191 165580 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 515 7 1 4 6.8 O=C(O)C1CN(Cc2cc(Cl)c(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1 10.1021/jm0492507
44394153 65810 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 363 14 3 3 4.3 CCCCCCCCCCCCCCN1CCC(O)(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
CHEMBL184237 65810 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 363 14 3 3 4.3 CCCCCCCCCCCCCCN1CCC(O)(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
59451739 136189 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.1 Cc1ccccc1COc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740768 136189 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.1 Cc1ccccc1COc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
44413415 138148 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 2 4 6.1 O=C(O)CC1CNC(c2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL377855 138148 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 2 4 6.1 O=C(O)CC1CNC(c2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
11653967 70215 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 389 6 1 5 4.2 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCC5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL194898 70215 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 389 6 1 5 4.2 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCC5)cc4)n3)cc2)C1 10.1021/jm0503244
49830828 71456 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1968499 71456 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.5b00928
49830725 71532 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 3.8 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1971132 71532 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 3.8 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
44394149 123496 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 377 15 3 3 4.5 CCCCCCCCCCCCCCN1CCC(C(O)P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
CHEMBL363008 123496 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 377 15 3 3 4.5 CCCCCCCCCCCCCCN1CCC(C(O)P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
59451824 136337 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 3.9 O=C(O)C1CN(Cc2ccc(-c3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3742100 136337 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 3.9 O=C(O)C1CN(Cc2ccc(-c3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
59451859 136302 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 315 6 1 3 2.9 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741775 136302 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 315 6 1 3 2.9 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
11248292 142962 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 465 7 1 4 5.7 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(F)c2)C1 10.1021/jm0492507
CHEMBL389880 142962 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 465 7 1 4 5.7 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(F)c2)C1 10.1021/jm0492507
44565596 188945 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 422 11 4 5 2.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccccc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL514302 188945 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 422 11 4 5 2.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccccc2)cc1 10.1016/j.bmcl.2009.02.073
11540052 179975 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2010.02.098
CHEMBL475405 179975 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2010.02.098
11690779 189113 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 442 8 4 5 3.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(Oc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL515603 189113 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 442 8 4 5 3.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(Oc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
2926 3525 72 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 440 3 0 4 7.2 FC(c1sc(cc1c1ccccc1)c1onc(n1)c1cccc(c1)C(F)(F)F)(F)F 10.1021/jm0492507
4077460 3525 72 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 440 3 0 4 7.2 FC(c1sc(cc1c1ccccc1)c1onc(n1)c1cccc(c1)C(F)(F)F)(F)F 10.1021/jm0492507
CHEMBL224720 3525 72 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 440 3 0 4 7.2 FC(c1sc(cc1c1ccccc1)c1onc(n1)c1cccc(c1)C(F)(F)F)(F)F 10.1021/jm0492507
11501764 133863 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 379 7 1 6 3.3 CCOc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL371743 133863 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 379 7 1 6 3.3 CCOc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
127041987 136092 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 11 1 3 3.9 CCCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739878 136092 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 11 1 3 3.9 CCCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
46872620 136124 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 4.2 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3740093 136124 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 4.2 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
59451845 136219 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 410 7 1 5 4.0 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)c([N+](=O)[O-])c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741022 136219 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 410 7 1 5 4.0 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)c([N+](=O)[O-])c2)C1 10.1021/acs.jmedchem.5b00928
59451849 136249 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 4.2 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2F)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741298 136249 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 4.2 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2F)C1 10.1021/acs.jmedchem.5b00928
44413349 77271 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 453 6 2 5 5.4 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL208838 77271 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 453 6 2 5 5.4 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
10249887 70569 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL195141 70569 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
44413482 165474 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 445 7 2 5 5.0 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL425602 165474 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 445 7 2 5 5.0 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
11466640 84652 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 525 7 1 4 6.3 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Br)c2)C1 10.1021/jm0492507
CHEMBL224599 84652 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 525 7 1 4 6.3 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Br)c2)C1 10.1021/jm0492507
10312 1263 16 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 388 4 2 3 5.6 NCc1cc(C)c(c(c1)C)NC(=O)c1ccc(o1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2011.04.097
53358422 1263 16 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 388 4 2 3 5.6 NCc1cc(C)c(c(c1)C)NC(=O)c1ccc(o1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2011.04.097
CHEMBL1779732 1263 16 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 388 4 2 3 5.6 NCc1cc(C)c(c(c1)C)NC(=O)c1ccc(o1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2011.04.097
44413447 138141 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 431 6 2 5 5.6 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL377828 138141 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 431 6 2 5 5.6 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
46872626 213 18 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
9496 213 18 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741589 213 18 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
46872622 72077 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 331 6 1 3 3.4 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)cc2Cl)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1987998 72077 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 331 6 1 3 3.4 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)cc2Cl)C1 10.1021/acs.jmedchem.5b00928
10287034 65837 3 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 367 11 2 2 4.7 CCCCCCCCCc1ccc(CN2CCC(P(=O)(O)O)C2)cc1 10.1021/jm0492507
CHEMBL184349 65837 3 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 367 11 2 2 4.7 CCCCCCCCCc1ccc(CN2CCC(P(=O)(O)O)C2)cc1 10.1021/jm0492507
10409838 133648 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 419 10 1 5 5.0 CCCCCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL371670 133648 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 419 10 1 5 5.0 CCCCCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
10476387 126980 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 405 6 1 5 4.5 CC(C)(C)Cc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL366181 126980 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 405 6 1 5 4.5 CC(C)(C)Cc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
44591250 189152 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1F 10.1016/j.bmcl.2008.11.072
CHEMBL515921 189152 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1F 10.1016/j.bmcl.2008.11.072
44412428 77877 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 435 6 2 5 5.5 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)cc4F)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL210782 77877 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 435 6 2 5 5.5 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)cc4F)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
44394212 66819 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 373 15 2 2 6.5 CCCCCCCCCCCCCC1CCCC(CCP(C)(=O)O)N1 10.1016/j.bmcl.2004.07.049
CHEMBL187692 66819 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 373 15 2 2 6.5 CCCCCCCCCCCCCC1CCCC(CCP(C)(=O)O)N1 10.1016/j.bmcl.2004.07.049
44394169 66335 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 16 2 2 5.7 CCCCCCCCCCCCCCN1CCCC1CCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL185447 66335 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 16 2 2 5.7 CCCCCCCCCCCCCCN1CCCC1CCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
44413446 77932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 417 6 2 5 5.2 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL211006 77932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 417 6 2 5 5.2 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
44394117 65994 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 17 2 2 6.1 CCCCCCCCCCCCCCC1CCCN1CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL185066 65994 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 17 2 2 6.1 CCCCCCCCCCCCCCC1CCCN1CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
59451753 136371 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 281 4 1 2 3.2 Cc1ccc(-c2ccc(CN3CC(C(=O)O)C3)cc2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3742384 136371 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 281 4 1 2 3.2 Cc1ccc(-c2ccc(CN3CC(C(=O)O)C3)cc2)cc1 10.1021/acs.jmedchem.5b00928
44565714 178707 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 484 11 4 5 4.1 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL473238 178707 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 484 11 4 5 4.1 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
59451780 136266 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 9 1 3 3.6 CCCCCCOc1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3741459 136266 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 9 1 3 3.6 CCCCCCOc1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451832 136107 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 297 6 1 3 2.8 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3739977 136107 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 297 6 1 3 2.8 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)cc2)C1 10.1021/acs.jmedchem.5b00928
10310952 84683 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 477 8 1 5 5.5 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
CHEMBL224800 84683 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 477 8 1 5 5.5 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
46872625 136134 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 317 5 1 3 3.6 O=C(O)C1CN(Cc2ccc(Oc3ccc(Cl)cc3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3740219 136134 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 317 5 1 3 3.6 O=C(O)C1CN(Cc2ccc(Oc3ccc(Cl)cc3)cc2)C1 10.1021/acs.jmedchem.5b00928
59451750 136328 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.1 Cc1cc(OCc2ccccc2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3742033 136328 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.1 Cc1cc(OCc2ccccc2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
11725751 12723 5 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 355 14 3 2 4.6 CCCCCCCCCc1ccc(CNCCCP(=O)(O)O)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL118860 12723 5 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 355 14 3 2 4.6 CCCCCCCCCc1ccc(CNCCCP(=O)(O)O)cc1 10.1016/j.bmcl.2004.07.049
44591249 180044 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 402 13 4 5 3.2 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1 10.1016/j.bmcl.2008.11.072
CHEMBL475495 180044 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 402 13 4 5 3.2 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1 10.1016/j.bmcl.2008.11.072
44412415 77798 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 419 8 2 5 5.3 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](CCC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL210468 77798 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 419 8 2 5 5.3 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](CCC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
46885796 8311 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 538 10 4 5 4.8 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(C(F)(F)F)c1 10.1016/j.bmcl.2010.02.098
CHEMBL1093429 8311 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 538 10 4 5 4.8 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(C(F)(F)F)c1 10.1016/j.bmcl.2010.02.098
68489165 136073 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 315 6 1 3 2.9 O=C(O)C1CN(Cc2ccc(OCc3ccc(F)cc3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3739695 136073 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 315 6 1 3 2.9 O=C(O)C1CN(Cc2ccc(OCc3ccc(F)cc3)cc2)C1 10.1021/acs.jmedchem.5b00928
59451764 136118 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 291 9 1 3 3.2 CCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740060 136118 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 291 9 1 3 3.2 CCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
46872048 136257 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 395 7 1 4 4.1 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741364 136257 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 395 7 1 4 4.1 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.5b00928
127037696 136271 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 10 1 3 3.6 CCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3741496 136271 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 10 1 3 3.6 CCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
44565717 188929 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 479 9 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
CHEMBL514170 188929 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 479 9 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
25008420 8364 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 547 9 4 5 5.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1 10.1016/j.bmcl.2010.02.098
CHEMBL1093823 8364 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 547 9 4 5 5.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1 10.1016/j.bmcl.2010.02.098
44565717 188929 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 479 9 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2010.02.098
CHEMBL514170 188929 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 479 9 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2010.02.098
44565715 179851 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 498 12 4 5 4.5 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL475253 179851 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 498 12 4 5 4.5 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
77846754 181950 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 435 5 1 3 6.3 Cc1cc(OC2CCC3(CCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4787458 181950 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 435 5 1 3 6.3 Cc1cc(OC2CCC3(CCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
11502996 158169 36 None 1 4 Human 9.2 pKi = 9.2 Binding
Displacement of [33P]-S1P from human S1P5 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting methodDisplacement of [33P]-S1P from human S1P5 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting method
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 158169 36 None 1 4 Human 9.2 pKi = 9.2 Binding
Displacement of [33P]-S1P from human S1P5 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting methodDisplacement of [33P]-S1P from human S1P5 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting method
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
77847762 182831 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 397 7 2 3 5.7 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4798593 182831 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 397 7 2 3 5.7 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
12573 978 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
77846592 978 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
CHEMBL4748198 978 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
11363176 3088 42 None - 0 Human 6.9 pIC50 = 6.9 Binding
In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>
Guide to Pharmacology 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C 20446681
5446 3088 42 None - 0 Human 6.9 pIC50 = 6.9 Binding
In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>
Guide to Pharmacology 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C 20446681
9320 3088 42 None - 0 Human 6.9 pIC50 = 6.9 Binding
In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>
Guide to Pharmacology 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C 20446681
CHEMBL1096146 3088 42 None - 0 Human 6.9 pIC50 = 6.9 Binding
In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>
Guide to Pharmacology 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C 20446681
6992 3934 0 None 7 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 11 3 3 4.3 CCCCCCCCc1cccc(c1)C1CC(C1)(N)COP(=O)(O)O 21632869
73755254 3934 0 None 7 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 11 3 3 4.3 CCCCCCCCc1cccc(c1)C1CC(C1)(N)COP(=O)(O)O 21632869
10883396 3579 39 None 1 4 Rat 8.7 pKd None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10799507
5283560 3579 39 None 1 4 Rat 8.7 pKd None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10799507
911 3579 39 None 1 4 Rat 8.7 pKd None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10799507
CHEMBL225155 3579 39 None 1 4 Rat 8.7 pKd None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10799507