Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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10202564 1524 None 18 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
3217 1524 None 18 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
CHEMBL362628 1524 None 18 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
10202564 1524 None 18 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
3217 1524 None 18 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
CHEMBL362628 1524 None 18 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
6918836 60561 None 10 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
CHEMBL175835 60561 None 10 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
6918836 60561 None 10 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
CHEMBL175835 60561 None 10 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
16718917 181788 None 0 Human Functional pEC50 = 9.5 9.5 2290 3
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL477650 181788 None 0 Human Functional pEC50 = 9.5 9.5 2290 3
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
16718920 189786 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
CHEMBL515307 189786 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
71459954 79213 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
CHEMBL2113386 79213 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
71459954 79213 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
CHEMBL2113386 79213 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
11234629 204670 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
CHEMBL609741 204670 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
16112801 181197 None 0 Human Functional pEC50 = 9.1 9.1 1258 2
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
CHEMBL476006 181197 None 0 Human Functional pEC50 = 9.1 9.1 1258 2
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
11463428 204209 None 0 Human Functional pEC50 = 9 9.0 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
CHEMBL606639 204209 None 0 Human Functional pEC50 = 9 9.0 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
10131112 1552 None 18 Human Functional pEC50 = 9 9.0 28 7
Partial agonist activity at 5-HT6 receptor (unknown origin)Partial agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1021/acs.jmedchem.3c02148
8428 1552 None 18 Human Functional pEC50 = 9 9.0 28 7
Partial agonist activity at 5-HT6 receptor (unknown origin)Partial agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1021/acs.jmedchem.3c02148
CHEMBL364005 1552 None 18 Human Functional pEC50 = 9 9.0 28 7
Partial agonist activity at 5-HT6 receptor (unknown origin)Partial agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1021/acs.jmedchem.3c02148
11200511 204187 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
CHEMBL606547 204187 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
11280663 204701 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
CHEMBL609995 204701 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
11223004 204671 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
CHEMBL609742 204671 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
11749539 204698 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
CHEMBL609992 204698 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
11451904 204752 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL610254 204752 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11210467 204666 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
CHEMBL609737 204666 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
11384146 204190 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606556 204190 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
44403084 71768 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196622 71768 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
23655289 88723 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
CHEMBL235986 88723 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
45484384 201323 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584049 201323 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
3245407 48119 None 21 Human Functional pEC50 = 6.0 6.0 1 5
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL1550957 48119 None 21 Human Functional pEC50 = 6.0 6.0 1 5
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
45484333 199272 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565724 199272 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
46880707 8540 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1094370 8540 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
11333554 96714 None 18 Human Functional pEC50 = 6.9 6.9 -64 3
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL26379 96714 None 18 Human Functional pEC50 = 6.9 6.9 -64 3
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
25208878 181169 None 0 Human Functional pEC50 = 7.9 7.9 77 2
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL475969 181169 None 0 Human Functional pEC50 = 7.9 7.9 77 2
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1 10.1021/jm8009469
23655287 88722 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
CHEMBL235985 88722 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
10067306 201322 None 0 Human Functional pEC50 = 7.8 7.8 8 4
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584046 201322 None 0 Human Functional pEC50 = 7.8 7.8 8 4
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
45484307 199285 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565753 199285 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
44403055 69869 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL193824 69869 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435607 89171 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236576 89171 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
22028185 201496 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585931 201496 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435608 89174 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236577 89174 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435643 147687 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393107 147687 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
23655462 90257 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL238277 90257 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
10017687 67302 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL188182 67302 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
10472158 199281 None 0 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565745 199281 None 0 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
11775364 204244 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606816 204244 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
23655468 89425 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236989 89425 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
14571158 149169 None 1 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
CHEMBL394303 149169 None 1 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
11211722 204192 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606558 204192 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
73354882 89727 None 0 Human Functional pEC50 = 8.6 8.6 14 6
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376482 89727 None 0 Human Functional pEC50 = 8.6 8.6 14 6
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11363934 204700 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
CHEMBL609994 204700 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
11453792 204188 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606548 204188 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
45484381 200945 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
CHEMBL577687 200945 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
46880531 6301 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081793 6301 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
44435614 154540 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL399013 154540 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
73356442 89730 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376485 89730 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44435616 147942 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393312 147942 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9902533 133671 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
CHEMBL371292 133671 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
45484297 199752 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568672 199752 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
9902533 133671 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133671 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44433197 88809 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236313 88809 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11709684 201073 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
CHEMBL578826 201073 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
11709684 201073 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL578826 201073 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44403064 133641 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371132 133641 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10380133 200792 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL576315 200792 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435635 89236 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236772 89236 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435604 154951 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL400627 154951 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484398 199323 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565977 199323 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435646 145648 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL391517 145648 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
16718827 175513 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
CHEMBL457570 175513 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
11385064 204191 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606557 204191 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
44435629 148782 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393997 148782 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484352 201092 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL579063 201092 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435641 147685 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393106 147685 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9999118 6171 None 3 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081094 6171 None 3 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
45484299 199673 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568249 199673 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
45484322 201261 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL583389 201261 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
73351903 89729 None 0 Human Functional pEC50 = 7.5 7.5 -1 4
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376484 89729 None 0 Human Functional pEC50 = 7.5 7.5 -1 4
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73347307 89732 None 0 Human Functional pEC50 = 7.5 7.5 32 4
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376487 89732 None 0 Human Functional pEC50 = 7.5 7.5 32 4
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44433198 147201 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392746 147201 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44403072 70433 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194568 70433 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435610 88829 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236404 88829 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484399 201420 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585098 201420 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
9902533 133671 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133671 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
12147013 65603 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL183203 65603 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
46880657 6381 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1082198 6381 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
44435647 88543 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235117 88543 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46880655 5554 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1076684 5554 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
11316594 204699 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
CHEMBL609993 204699 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
46227395 202585 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL596199 202585 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
11351089 204193 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606559 204193 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
11440676 204672 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
CHEMBL609743 204672 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
44435637 89398 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236976 89398 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
5 139 None 45 Human Functional pEC50 = 7.4 7.4 -181 26
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
5202 139 None 45 Human Functional pEC50 = 7.4 7.4 -181 26
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
CHEMBL39 139 None 45 Human Functional pEC50 = 7.4 7.4 -181 26
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
DB08839 139 None 45 Human Functional pEC50 = 7.4 7.4 -181 26
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
5 139 None 45 Human Functional pEC50 = 7.4 7.4 -181 26
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
5202 139 None 45 Human Functional pEC50 = 7.4 7.4 -181 26
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
CHEMBL39 139 None 45 Human Functional pEC50 = 7.4 7.4 -181 26
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
DB08839 139 None 45 Human Functional pEC50 = 7.4 7.4 -181 26
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
44435627 88534 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235070 88534 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484382 199273 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
CHEMBL565730 199273 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
44435638 155018 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL401018 155018 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11200157 204220 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
CHEMBL606705 204220 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
73347306 89728 None 0 Human Functional pEC50 = 8.3 8.3 15 5
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376483 89728 None 0 Human Functional pEC50 = 8.3 8.3 15 5
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11452988 204697 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
CHEMBL609991 204697 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
44435653 147488 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392976 147488 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435628 148590 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393830 148590 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10407367 199249 None 0 Human Functional pEC50 = 7.3 7.3 10 5
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565552 199249 None 0 Human Functional pEC50 = 7.3 7.3 10 5
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
44403059 124440 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363827 124440 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435613 154492 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398809 154492 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
23655469 89426 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236990 89426 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
46880486 6172 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081095 6172 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10199819 133677 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371318 133677 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
46880607 5976 None 1 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1079977 5976 None 1 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
10150497 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
3240 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
CHEMBL392760 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
10150497 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
3240 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
CHEMBL392760 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
10150497 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
3240 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
CHEMBL392760 4074 None 40 Human Functional pEC50 = 8.2 8.2 457 15
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
73350387 89731 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL2376486 89731 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
9840311 5552 None 3 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076665 5552 None 3 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
44435642 88671 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235734 88671 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11725505 201495 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585930 201495 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
44433196 88756 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236104 88756 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10177537 124443 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363843 124443 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435649 145913 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL391713 145913 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
23625764 147393 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL392899 147393 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880608 6022 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080316 6022 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10337743 4076 None 15 Human Functional pEC50 = 8.1 8.1 47 4
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
8429 4076 None 15 Human Functional pEC50 = 8.1 8.1 47 4
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
CHEMBL571858 4076 None 15 Human Functional pEC50 = 8.1 8.1 47 4
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
10337743 4076 None 15 Human Functional pEC50 = 8.1 8.1 47 4
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
8429 4076 None 15 Human Functional pEC50 = 8.1 8.1 47 4
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
CHEMBL571858 4076 None 15 Human Functional pEC50 = 8.1 8.1 47 4
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
44435652 89288 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236812 89288 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435639 88582 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235306 88582 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880529 6173 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
CHEMBL1081110 6173 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
21071574 124150 None 1 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
CHEMBL363275 124150 None 1 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
44433193 88755 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236103 88755 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10042892 5534 None 3 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076583 5534 None 3 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
45484383 199274 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565731 199274 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
44403096 72152 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
CHEMBL197845 72152 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
23655465 89422 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL236987 89422 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
44435650 88544 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235118 88544 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
11361090 64326 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL181066 64326 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
11624561 70311 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL187865 70311 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL194307 70311 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44389001 63822 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180221 63822 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
11396708 204668 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
CHEMBL609739 204668 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
11524473 134908 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL371886 134908 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
11739679 169955 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL444015 169955 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
44403044 161805 None 0 Human Functional pIC50 = 9 9.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL413525 161805 None 0 Human Functional pIC50 = 9 9.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
11282884 204754 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
CHEMBL610256 204754 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
44389081 62673 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178385 62673 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
49836923 18770 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277918 18770 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44554395 18730 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 18730 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
11201726 204757 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
CHEMBL610259 204757 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
49836825 18729 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
CHEMBL1277564 18729 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
49836826 18739 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277656 18739 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44389004 123193 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL361180 123193 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
49836827 18748 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277751 18748 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
49836828 18756 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277836 18756 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44554394 18740 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277657 18740 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44433195 146973 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392541 146973 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25263302 192093 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 192093 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
46189984 68912 None 1 Human Functional pIC50 = 8 8.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1922635 68912 None 1 Human Functional pIC50 = 8 8.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
11316095 204245 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
CHEMBL606817 204245 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
162676953 183628 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4799851 183628 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
24784575 176819 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
CHEMBL459989 176819 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
21071390 1987 None 42 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
8689 1987 None 42 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
CHEMBL3286580 1987 None 42 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
DB11957 1987 None 42 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
18590409 10657 None 8 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
CHEMBL1170463 10657 None 8 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
46224917 201927 None 4 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 306 2 0 2 4.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL591570 201927 None 4 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 306 2 0 2 4.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
49836615 18795 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1278091 18795 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
52918031 57683 None 4 Human Functional pIC50 = 7 7.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668587 57683 None 4 Human Functional pIC50 = 7 7.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
24763349 62650 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783608 62650 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
16070169 60115 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642850 60115 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739214 60115 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53320775 60149 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642878 60149 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739546 60149 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
58357671 129104 None 3 Human Functional pIC50 = 6.0 6.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 365 4 1 7 2.7 CNc1nn2c(-c3cccnc3)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670291 129104 None 3 Human Functional pIC50 = 6.0 6.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 365 4 1 7 2.7 CNc1nn2c(-c3cccnc3)ccnc2c1S(=O)(=O)c1ccccc1 nan
54582939 62741 None 5 Human Functional pIC50 = 6.0 6.0 -8 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783957 62741 None 5 Human Functional pIC50 = 6.0 6.0 -8 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
20901255 10959 None 6 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 3 0 9 2.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCOCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173281 10959 None 6 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 3 0 9 2.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCOCC1)c1sccc12 10.1016/j.bmc.2010.05.051
24783809 176818 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459988 176818 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
16019451 10993 None 4 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 7 1 8 4.4 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173570 10993 None 4 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 7 1 8 4.4 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
44126270 201607 None 5 Human Functional pIC50 = 6.0 6.0 -10 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589389 201607 None 5 Human Functional pIC50 = 6.0 6.0 -10 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
54585846 62747 None 4 Human Functional pIC50 = 5.0 5.0 -38 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
CHEMBL1783963 62747 None 4 Human Functional pIC50 = 5.0 5.0 -38 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
46880606 5975 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1079976 5975 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
46880756 6029 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080380 6029 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10136185 127246 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365753 127246 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
20901273 10644 None 5 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 509 4 1 8 5.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170291 10644 None 5 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 509 4 1 8 5.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
24763430 62639 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
CHEMBL1783582 62639 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
49836617 18811 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278180 18811 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
18560541 10939 None 9 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.2 CC(Cc1ccccc1)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173061 10939 None 9 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.2 CC(Cc1ccccc1)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
118512797 142943 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 403 7 1 4 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc(Cl)c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3893286 142943 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 403 7 1 4 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc(Cl)c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
44435625 149086 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL394233 149086 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
25263297 184443 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
CHEMBL484345 184443 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
4106 2502 None 21 Human Functional pIC50 = 8.0 8.0 -29 7
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
5358812 2502 None 21 Human Functional pIC50 = 8.0 8.0 -29 7
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
89 2502 None 21 Human Functional pIC50 = 8.0 8.0 -29 7
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
CHEMBL93240 2502 None 21 Human Functional pIC50 = 8.0 8.0 -29 7
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
44403048 132773 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL369910 132773 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
44388950 122670 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL360234 122670 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
46189932 68907 None 4 Human Functional pIC50 = 8.0 8.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922630 68907 None 4 Human Functional pIC50 = 8.0 8.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
53259021 69769 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935594 69769 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
16019576 10901 None 5 Human Functional pIC50 = 7.0 7.0 1995 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172726 10901 None 5 Human Functional pIC50 = 7.0 7.0 1995 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
18591269 10971 None 1 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173362 10971 None 1 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
10115005 71708 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196466 71708 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10117854 127492 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL366012 127492 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
18560059 10913 None 8 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 0 8 4.8 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172791 10913 None 8 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 0 8 4.8 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
18559283 10658 None 8 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170464 10658 None 8 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
53324933 57639 None 2 Human Functional pIC50 = 6.0 6.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668502 57639 None 2 Human Functional pIC50 = 6.0 6.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
49836621 18662 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276926 18662 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
44403047 168531 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL434932 168531 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
16019286 10952 None 5 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
CHEMBL1173206 10952 None 5 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
46225001 201572 None 4 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 326 3 0 2 4.2 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589149 201572 None 4 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 326 3 0 2 4.2 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
18560559 10685 None 11 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170682 10685 None 11 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16804502 10689 None 12 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 471 5 1 9 4.6 COc1ccccc1Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170686 10689 None 12 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 471 5 1 9 4.6 COc1ccccc1Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
18560180 10638 None 10 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170276 10638 None 10 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
197033 201608 None 42 Human Functional pIC50 = 5.9 5.9 -1 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 201608 None 42 Human Functional pIC50 = 5.9 5.9 -1 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
24783550 176837 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460194 176837 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
16019548 10886 None 9 Human Functional pIC50 = 5.9 5.9 23 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(Cl)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172597 10886 None 9 Human Functional pIC50 = 5.9 5.9 23 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(Cl)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
44156502 61004 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762569 61004 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 nan
16117278 60169 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642884 60169 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739659 60169 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
18590273 10781 None 8 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171632 10781 None 8 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16117151 60107 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642882 60107 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739102 60107 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
56655504 68891 None 3 Human Functional pIC50 = 7.9 7.9 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922614 68891 None 3 Human Functional pIC50 = 7.9 7.9 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
56849579 68896 None 3 Human Functional pIC50 = 7.9 7.9 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922619 68896 None 3 Human Functional pIC50 = 7.9 7.9 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357768 129106 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 395 5 1 8 2.7 CNc1nn2c(OC)cc(-c3cccnc3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670293 129106 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 395 5 1 8 2.7 CNc1nn2c(OC)cc(-c3cccnc3)nc2c1S(=O)(=O)c1ccccc1 nan
25123014 202887 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598229 202887 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
44435624 89137 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236541 89137 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24784573 176292 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL459348 176292 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
49798859 10570 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccc(Cl)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169724 10570 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccc(Cl)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
7185128 10979 None 1 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173433 10979 None 1 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901271 10662 None 7 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170472 10662 None 7 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)cc1 10.1016/j.bmc.2010.05.051
20901291 10766 None 5 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 7 1 8 4.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1171486 10766 None 5 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 7 1 8 4.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
16019607 10932 None 2 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 0 8 3.7 CCN(CC)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173005 10932 None 2 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 0 8 3.7 CCN(CC)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901207 10988 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173508 10988 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
10202995 70577 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194786 70577 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
16117281 60164 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642880 60164 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739648 60164 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16019305 10584 None 7 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 5 1 10 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc4c(c2)OCO4)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169898 10584 None 7 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 5 1 10 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc4c(c2)OCO4)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
49799667 10917 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172795 10917 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
16117282 60158 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642888 60158 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739615 60158 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
4106 2502 None 21 Human Functional pIC50 = 6.9 6.9 -29 7
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
5358812 2502 None 21 Human Functional pIC50 = 6.9 6.9 -29 7
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
89 2502 None 21 Human Functional pIC50 = 6.9 6.9 -29 7
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
CHEMBL93240 2502 None 21 Human Functional pIC50 = 6.9 6.9 -29 7
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
20901220 10922 None 3 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172868 10922 None 3 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16071727 60122 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642848 60122 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739253 60122 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
10430623 18682 None 22 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1277105 18682 None 22 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
9950402 170557 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL444878 170557 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44435623 149085 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394232 149085 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
49836509 18778 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277999 18778 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
57402070 71587 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949761 71587 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1963096 71587 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
18560325 10962 None 11 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173284 10962 None 11 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
49799664 11005 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(C2CCN(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173774 11005 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(C2CCN(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
44435612 88830 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236405 88830 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
57396850 71548 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949762 71548 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962863 71548 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
24965679 84069 None 21 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207386 84069 None 21 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
18590416 10692 None 8 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170689 10692 None 8 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
57393365 71574 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71574 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71574 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
53325577 60178 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642874 60178 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739700 60178 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
18560539 10884 None 10 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172595 10884 None 10 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
18560202 10636 None 10 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170274 10636 None 10 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16117279 60156 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 60156 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 60156 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
11316536 204236 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606765 204236 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
44388951 62549 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL178234 62549 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
563919 99332 None 2 Human Functional pIC50 = 7.8 7.8 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL281937 99332 None 2 Human Functional pIC50 = 7.8 7.8 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
20901117 10680 None 2 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170672 10680 None 2 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019610 10868 None 9 Human Functional pIC50 = 6.9 6.9 50 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 4 1 8 5.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172404 10868 None 9 Human Functional pIC50 = 6.9 6.9 50 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 4 1 8 5.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
71769424 91989 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 551 6 0 7 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c(N(C)C)cccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414704 91989 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 551 6 0 7 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c(N(C)C)cccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
118727447 117502 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 459 8 0 9 2.7 COc1ccc(OC)c(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)c1 10.1016/j.bmc.2015.01.032
CHEMBL3398395 117502 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 459 8 0 9 2.7 COc1ccc(OC)c(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)c1 10.1016/j.bmc.2015.01.032
44435619 88817 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236335 88817 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
118512792 145209 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 420 7 1 5 4.1 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3911908 145209 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 420 7 1 5 4.1 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
18591074 10898 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2ccc(Cl)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1172723 10898 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2ccc(Cl)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
46224941 201605 None 2 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589386 201605 None 2 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
18560060 10912 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172790 10912 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
7184895 10654 None 5 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 6 1 9 2.5 COCCNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170439 10654 None 5 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 6 1 9 2.5 COCCNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16118795 60116 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642851 60116 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739215 60116 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
86302554 110896 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260795 110896 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
45484298 199753 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568673 199753 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
45113400 14236 None 2 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1099284 14236 None 2 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199172 14236 None 2 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
10291754 70458 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL194590 70458 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
25067564 203757 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 203757 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
20901261 10682 None 7 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170679 10682 None 7 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
20901266 10915 None 7 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172793 10915 None 7 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
20901268 11006 None 4 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 437 7 1 9 3.3 COCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173777 11006 None 4 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 437 7 1 9 3.3 COCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224944 202033 None 3 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 336 3 0 3 4.4 COc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL592516 202033 None 3 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 336 3 0 3 4.4 COc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
16019510 11003 None 4 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 3 0 8 3.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173706 11003 None 4 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 3 0 8 3.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
23652787 56704 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642419 56704 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
20901258 10953 None 2 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173207 10953 None 2 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
56849580 68897 None 4 Human Functional pIC50 = 5.8 5.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922620 68897 None 4 Human Functional pIC50 = 5.8 5.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
53318111 60108 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642862 60108 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739117 60108 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53318268 57678 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668582 57678 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
25117680 203091 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599466 203091 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
7184976 10739 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171092 10739 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
54586812 62737 None 4 Human Functional pIC50 = 4.8 4.8 -12 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783953 62737 None 4 Human Functional pIC50 = 4.8 4.8 -12 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
42631003 202074 None 10 Human Functional pIC50 = 6.8 6.8 -2 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 202074 None 10 Human Functional pIC50 = 6.8 6.8 -2 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
16718922 200676 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
CHEMBL575310 200676 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
54582940 62742 None 4 Human Functional pIC50 = 5.8 5.8 -1 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783958 62742 None 4 Human Functional pIC50 = 5.8 5.8 -1 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
16117153 60159 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642889 60159 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739616 60159 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
53324896 57681 None 4 Human Functional pIC50 = 7.8 7.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668585 57681 None 4 Human Functional pIC50 = 7.8 7.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
25123013 202914 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598443 202914 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
44155109 8176 None 4 Human Functional pIC50 = 7.8 7.8 21 2
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091919 8176 None 4 Human Functional pIC50 = 7.8 7.8 21 2
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
46227396 204097 None 0 Human Functional pIC50 = 5.8 5.8 -1 3
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
CHEMBL605938 204097 None 0 Human Functional pIC50 = 5.8 5.8 -1 3
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
16019453 10944 None 4 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 5 1 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173127 10944 None 4 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 5 1 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
24894055 183274 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMPAntagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMP
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL479548 183274 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMPAntagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMP
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
18590411 10927 None 10 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 493 5 1 9 3.5 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172938 10927 None 10 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 493 5 1 9 3.5 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
71813838 91625 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 430 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(Cl)c4C)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407545 91625 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 430 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(Cl)c4C)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
46224880 203327 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 2 0 2 4.3 Cc1ccc2c(c1)C1CN(C)CCC1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL601304 203327 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 2 0 2 4.3 Cc1ccc2c(c1)C1CN(C)CCC1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
71695200 129830 None 5 Human Functional pIC50 = 5.8 5.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675191 129830 None 5 Human Functional pIC50 = 5.8 5.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
44388970 64877 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182099 64877 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
46880708 7448 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1086719 7448 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
49836823 18717 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
CHEMBL1277466 18717 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
23655467 89424 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
CHEMBL236988 89424 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
25117677 202708 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL597009 202708 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
126720440 163121 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4175829 163121 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
24771124 184440 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484333 184440 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
16019580 10566 None 1 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169707 10566 None 1 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16019288 10695 None 6 Human Functional pIC50 = 6.8 6.8 234 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 433 4 1 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170696 10695 None 6 Human Functional pIC50 = 6.8 6.8 234 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 433 4 1 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019550 10711 None 12 Human Functional pIC50 = 6.8 6.8 131 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.3 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170886 10711 None 12 Human Functional pIC50 = 6.8 6.8 131 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.3 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
20901217 10911 None 3 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172789 10911 None 3 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
56849581 68898 None 1 Human Functional pIC50 = 6.8 6.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922621 68898 None 1 Human Functional pIC50 = 6.8 6.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
56849715 68901 None 2 Human Functional pIC50 = 6.8 6.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922624 68901 None 2 Human Functional pIC50 = 6.8 6.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
16118796 60118 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642853 60118 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739217 60118 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
18559973 10640 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170280 10640 None 8 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
46224918 201949 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 2 0 2 4.1 CN1CCC2C(C1)c1cc(F)ccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL591801 201949 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 2 0 2 4.1 CN1CCC2C(C1)c1cc(F)ccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
45483622 200547 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574403 200547 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
52918030 57665 None 4 Human Functional pIC50 = 6.8 6.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668569 57665 None 4 Human Functional pIC50 = 6.8 6.8 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
129103318 167410 None 0 Human Functional pIC50 = 6.8 6.8 -19 6
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 167410 None 0 Human Functional pIC50 = 6.8 6.8 -19 6
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
118512804 157756 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 438 7 1 5 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccc(F)cc1 10.1016/j.bmcl.2017.07.031
CHEMBL4081529 157756 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 438 7 1 5 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccc(F)cc1 10.1016/j.bmcl.2017.07.031
23653062 56709 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642424 56709 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
57396848 71560 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949760 71560 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962943 71560 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
46880532 6302 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081794 6302 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
16019609 10615 None 10 Human Functional pIC50 = 6.8 6.8 223 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170098 10615 None 10 Human Functional pIC50 = 6.8 6.8 223 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
46224914 202002 None 2 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592271 202002 None 2 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
71769065 91992 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 458 5 0 6 4.1 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414711 91992 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 458 5 0 6 4.1 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
20901172 10586 None 5 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 497 6 1 8 5.6 CC(C)c1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169900 10586 None 5 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 497 6 1 8 5.6 CC(C)c1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
118727442 117497 None 0 Human Functional pIC50 = 5.7 5.7 -5 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 399 6 0 7 2.7 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccccc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398389 117497 None 0 Human Functional pIC50 = 5.7 5.7 -5 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 399 6 0 7 2.7 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccccc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
56849581 68898 None 1 Human Functional pIC50 = 5.7 5.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922621 68898 None 1 Human Functional pIC50 = 5.7 5.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44435615 89175 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236578 89175 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
53319627 57677 None 1 Human Functional pIC50 = 6.7 6.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668581 57677 None 1 Human Functional pIC50 = 6.7 6.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
53323599 57671 None 4 Human Functional pIC50 = 5.7 5.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668575 57671 None 4 Human Functional pIC50 = 5.7 5.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
53320009 56679 None 0 Human Functional pIC50 = 6.7 6.7 2 7
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 56679 None 0 Human Functional pIC50 = 6.7 6.7 2 7
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
53323402 60162 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642864 60162 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739646 60162 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16117283 60168 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1642883 60168 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1739658 60168 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
3232 3509 None 17 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
3248571 3509 None 17 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
CHEMBL60264 3509 None 17 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
53326177 57684 None 4 Human Functional pIC50 = 7.7 7.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668588 57684 None 4 Human Functional pIC50 = 7.7 7.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
44388931 64135 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180826 64135 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
7185122 10611 None 1 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 389 6 1 9 2.2 COCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170093 10611 None 1 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 389 6 1 9 2.2 COCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901254 10914 None 7 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172792 10914 None 7 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
7470702 10655 None 9 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 0 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(N(CC)CC)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170442 10655 None 9 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 0 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(N(CC)CC)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
16019490 11004 None 4 Human Functional pIC50 = 5.7 5.7 8 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 3 0 9 2.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCOCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173709 11004 None 4 Human Functional pIC50 = 5.7 5.7 8 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 3 0 9 2.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCOCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
18590413 10986 None 10 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 0 8 4.6 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173503 10986 None 10 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 0 8 4.6 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16222547 82069 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165541 82069 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
45487150 200176 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL571413 200176 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
56849714 68900 None 2 Human Functional pIC50 = 6.7 6.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922623 68900 None 2 Human Functional pIC50 = 6.7 6.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
46224945 203863 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 5.0 C/C(=C/c1ccccc1)n1c2c(c3cc(C)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
CHEMBL604669 203863 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 5.0 C/C(=C/c1ccccc1)n1c2c(c3cc(C)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
49799663 10678 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 4.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCC(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170664 10678 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 4.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCC(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
20901114 10945 None 1 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 442 4 1 9 1.9 NC(=O)C1CCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
CHEMBL1173132 10945 None 1 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 442 4 1 9 1.9 NC(=O)C1CCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
131999484 182709 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4746584 182709 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4788250 182709 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
49836924 18780 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
CHEMBL1278000 18780 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
44156626 57686 None 4 Human Functional pIC50 = 8.7 8.7 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668590 57686 None 4 Human Functional pIC50 = 8.7 8.7 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
44554228 18749 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277752 18749 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44389016 63941 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180606 63941 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
11256720 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
9444 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
CHEMBL1083390 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
DB12680 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
11256720 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
9444 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL1083390 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
DB12680 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
11256720 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
9444 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL1083390 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
DB12680 2055 None 52 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
49836824 18718 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277467 18718 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44554227 18757 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277837 18757 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
135398737 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
135398737.0 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
38 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
722 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
CHEMBL42 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
DB00363 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
135398737 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
135398737.0 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
38 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
722 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
CHEMBL42 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
DB00363 958 None 57 Human Functional pIC50 = 7.7 7.7 -7 43
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
7185123 10681 None 5 Human Functional pIC50 = 6.7 6.7 851 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170673 10681 None 5 Human Functional pIC50 = 6.7 6.7 851 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
20901267 10951 None 5 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
CHEMBL1173205 10951 None 5 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
16019602 10691 None 5 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170688 10691 None 5 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
25117681 203012 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599023 203012 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
20901132 10847 None 2 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172207 10847 None 2 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
18560542 10910 None 6 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 3 0 8 3.4 CC1CCCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
CHEMBL1172788 10910 None 6 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 3 0 8 3.4 CC1CCCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
71770944 91999 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2013.05.051
CHEMBL2414732 91999 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2013.05.051
71770944 91999 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2015.01.032
CHEMBL2414732 91999 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2015.01.032
16222549 82051 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165524 82051 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
54583938 62753 None 0 Human Functional pIC50 = 5.7 5.7 -1 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783970 62753 None 0 Human Functional pIC50 = 5.7 5.7 -1 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
46225002 201950 None 4 Human Functional pIC50 = 4.7 4.7 -602 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL591803 201950 None 4 Human Functional pIC50 = 4.7 4.7 -602 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
16116900 60121 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642847 60121 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739252 60121 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
57398718 69767 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935592 69767 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
118173755 192443 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5206617 192443 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
10141477 140345 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380556 140345 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
11177383 204189 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606549 204189 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
46227404 202339 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL594548 202339 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
11235953 204243 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606815 204243 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
118727445 117500 None 0 Human Functional pIC50 = 5.7 5.7 -8 3
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 413 6 0 7 3.0 Cc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
CHEMBL3398392 117500 None 0 Human Functional pIC50 = 5.7 5.7 -8 3
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 413 6 0 7 3.0 Cc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
44435617 89176 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236579 89176 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
20901163 10980 None 7 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173434 10980 None 7 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
58357790 129834 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 2 7 1.5 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL3675195 129834 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 2 7 1.5 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
16019312 10902 None 1 Human Functional pIC50 = 6.7 6.7 144 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 5 1 9 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172727 10902 None 1 Human Functional pIC50 = 6.7 6.7 144 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 5 1 9 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
58357705 129098 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(C)c1 nan
CHEMBL3670284 129098 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(C)c1 nan
20901131 10571 None 6 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1169725 10571 None 6 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
49799645 10899 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 4 1 8 5.5 Cc1cc(Cl)cc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172724 10899 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 4 1 8 5.5 Cc1cc(Cl)cc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
57403833 71494 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949765 71494 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962396 71494 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
44126328 203562 None 4 Human Functional pIC50 = 5.6 5.6 -74 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL603049 203562 None 4 Human Functional pIC50 = 5.6 5.6 -74 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
68303508 129831 None 4 Human Functional pIC50 = 5.6 5.6 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675192 129831 None 4 Human Functional pIC50 = 5.6 5.6 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
53323439 60177 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642873 60177 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739699 60177 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44435621 88818 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236336 88818 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24965329 84071 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207388 84071 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
46225027 201573 None 4 Human Functional pIC50 = 5.6 5.6 -74 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589150 201573 None 4 Human Functional pIC50 = 5.6 5.6 -74 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44474625 14076 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197521 14076 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL575270 14076 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
20901145 10814 None 1 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171992 10814 None 1 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53322935 57685 None 4 Human Functional pIC50 = 7.6 7.6 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668589 57685 None 4 Human Functional pIC50 = 7.6 7.6 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
44403103 141396 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL383373 141396 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44263496 203982 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
CHEMBL605292 203982 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
71770821 91996 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 474 5 0 7 3.7 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(C)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
CHEMBL2414725 91996 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 474 5 0 7 3.7 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(C)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
118512815 151766 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3ccccc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3964100 151766 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3ccccc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
118727448 117503 None 0 Human Functional pIC50 = 5.6 5.6 -1 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 463 7 0 8 3.4 COc1ccc(Cl)cc1S(=O)(=O)n1cc(/C=N/N=C/N(C)C)c2c([N+](=O)[O-])cccc21 10.1016/j.bmc.2015.01.032
CHEMBL3398396 117503 None 0 Human Functional pIC50 = 5.6 5.6 -1 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 463 7 0 8 3.4 COc1ccc(Cl)cc1S(=O)(=O)n1cc(/C=N/N=C/N(C)C)c2c([N+](=O)[O-])cccc21 10.1016/j.bmc.2015.01.032
57403837 71497 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949772 71497 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962399 71497 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
24783810 176301 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459371 176301 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
10274389 133490 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370507 133490 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
46189987 68911 None 3 Human Functional pIC50 = 7.6 7.6 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1922634 68911 None 3 Human Functional pIC50 = 7.6 7.6 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
11775364 204244 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606816 204244 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
20901128 10954 None 2 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 5 1 9 3.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173208 10954 None 2 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 5 1 9 3.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
18591272 10663 None 8 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 459 4 1 8 4.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170473 10663 None 8 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 459 4 1 8 4.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
16750338 62649 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783607 62649 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
118727450 117505 None 0 Human Functional pIC50 = 5.6 5.6 -5 3
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc3ccccc3c2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398398 117505 None 0 Human Functional pIC50 = 5.6 5.6 -5 3
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc3ccccc3c2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
46224878 201925 None 0 Human Functional pIC50 = 5.6 5.6 -2 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL591568 201925 None 0 Human Functional pIC50 = 5.6 5.6 -2 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
44433194 146690 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392318 146690 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11545169 147739 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393158 147739 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25263299 192227 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL520343 192227 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
21071390 1987 None 42 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
8689 1987 None 42 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
CHEMBL3286580 1987 None 42 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
DB11957 1987 None 42 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
46190034 68913 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922636 68913 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
25122652 203118 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
CHEMBL599663 203118 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
25263301 184725 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484927 184725 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
16019601 10567 None 1 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169708 10567 None 1 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901120 10637 None 1 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 7 1 9 2.6 COCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170275 10637 None 1 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 7 1 9 2.6 COCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
49799683 10946 None 2 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 422 5 1 9 3.2 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173135 10946 None 2 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 422 5 1 9 3.2 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
45113275 9109 None 5 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 293 2 1 3 1.4 CN1CCc2[nH]c3ccc(S(=O)(=O)N(C)C)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1099282 9109 None 5 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 293 2 1 3 1.4 CN1CCc2[nH]c3ccc(S(=O)(=O)N(C)C)cc3c2C1 10.1016/j.ejmech.2009.10.035
16117280 60157 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642887 60157 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739614 60157 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
57393363 71588 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949764 71588 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963097 71588 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
44156863 8080 None 0 Human Functional pIC50 = 7.6 7.6 21 2
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
CHEMBL1091206 8080 None 0 Human Functional pIC50 = 7.6 7.6 21 2
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
16019372 10684 None 8 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170681 10684 None 8 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
44126269 203941 None 4 Human Functional pIC50 = 6.6 6.6 -2 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 203941 None 4 Human Functional pIC50 = 6.6 6.6 -2 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44435631 89711 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237594 89711 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25122651 202705 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL597002 202705 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
18560562 10616 None 9 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170099 10616 None 9 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
45113535 14245 None 1 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
CHEMBL1097614 14245 None 1 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
CHEMBL1199305 14245 None 1 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
57403835 71495 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949767 71495 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962397 71495 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
46224915 202031 None 2 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 370 2 0 2 5.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592514 202031 None 2 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 370 2 0 2 5.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
18591268 10903 None 1 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172728 10903 None 1 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
118173772 190484 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5177311 190484 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
20901118 10565 None 7 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 10 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1169706 10565 None 7 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 10 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
18560182 10867 None 7 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172403 10867 None 7 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
71769190 91994 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 476 5 0 6 4.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414713 91994 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 476 5 0 6 4.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
23624297 56698 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642413 56698 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
45487139 199796 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL568935 199796 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
46224942 203862 None 2 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 324 2 0 2 4.5 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL604668 203862 None 2 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 324 2 0 2 4.5 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
118727449 117504 None 0 Human Functional pIC50 = 5.5 5.5 -5 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2cccc3ccccc23)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398397 117504 None 0 Human Functional pIC50 = 5.5 5.5 -5 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2cccc3ccccc23)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
54579956 62740 None 4 Human Functional pIC50 = 5.5 5.5 -3 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783956 62740 None 4 Human Functional pIC50 = 5.5 5.5 -3 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
53326176 57682 None 4 Human Functional pIC50 = 8.5 8.5 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668586 57682 None 4 Human Functional pIC50 = 8.5 8.5 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
10405986 18796 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1278092 18796 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
57396970 69765 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935590 69765 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
118181460 190002 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5169546 190002 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
44327759 210371 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL96745 210371 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
16071847 60165 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642865 60165 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739655 60165 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
44389002 63585 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180066 63585 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
53318109 60123 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642849 60123 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739254 60123 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
18560186 10585 None 9 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 0 8 4.5 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169899 10585 None 9 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 0 8 4.5 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
10356663 112006 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL328816 112006 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
58357851 129094 None 5 Human Functional pIC50 = 6.5 6.5 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670280 129094 None 5 Human Functional pIC50 = 6.5 6.5 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357730 129100 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 412 5 0 8 3.4 COc1cc(-c2ccccn2)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 nan
CHEMBL3670286 129100 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 412 5 0 8 3.4 COc1cc(-c2ccccn2)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 nan
57398615 71573 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71573 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71573 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
44389074 123379 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL361572 123379 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
71814157 91629 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2013.05.100
CHEMBL2407553 91629 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2013.05.100
71814318 91630 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3ccc4ccccc4c3)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2017.07.031
CHEMBL2407554 91630 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3ccc4ccccc4c3)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2017.07.031
23653135 56697 None 3 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642412 56697 None 3 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
25117679 203060 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599263 203060 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
57400392 69775 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935600 69775 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
18560181 10715 None 9 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1Cl)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170892 10715 None 9 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1Cl)c1sccc12 10.1016/j.bmc.2010.05.051
44155109 8176 None 4 Human Functional pIC50 = 7.5 7.5 21 2
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091919 8176 None 4 Human Functional pIC50 = 7.5 7.5 21 2
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
10356663 112006 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL328816 112006 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
53322548 56703 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642418 56703 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
54580942 62751 None 7 Human Functional pIC50 = 5.5 5.5 -13 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783967 62751 None 7 Human Functional pIC50 = 5.5 5.5 -13 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
71813833 91623 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 450 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(C(F)(F)F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407540 91623 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 450 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(C(F)(F)F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
57391618 71493 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71493 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71493 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
25122654 202984 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
CHEMBL598851 202984 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
44388944 63038 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178767 63038 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
118512805 147652 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2ccc3ccccc3c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3930881 147652 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2ccc3ccccc3c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
49836715 18669 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277010 18669 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
44435633 89575 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237389 89575 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
57391729 69768 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935593 69768 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
16019553 10710 None 5 Human Functional pIC50 = 7.5 7.5 912 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170871 10710 None 5 Human Functional pIC50 = 7.5 7.5 912 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
44435609 154491 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398808 154491 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45113404 14227 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1095273 14227 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199078 14227 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
58357665 129105 None 2 Human Functional pIC50 = 6.5 6.5 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(-c3cccnc3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670292 129105 None 2 Human Functional pIC50 = 6.5 6.5 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(-c3cccnc3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
164622805 185969 None 0 Human Functional pIC50 = 6.5 6.5 -30 6
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4867978 185969 None 0 Human Functional pIC50 = 6.5 6.5 -30 6
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
44155107 8081 None 4 Human Functional pIC50 = 7.5 7.5 60 2
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091207 8081 None 4 Human Functional pIC50 = 7.5 7.5 60 2
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
16019339 10607 None 5 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170087 10607 None 5 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
16019508 10916 None 8 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172794 10916 None 8 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
57395082 71568 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949766 71568 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963006 71568 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57520121 73292 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2012.02.020
CHEMBL2012637 73292 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2012.02.020
57520121 73292 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2015.01.032
CHEMBL2012637 73292 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2015.01.032
73347610 91990 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 462 5 0 8 2.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3nccn3C)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414705 91990 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 462 5 0 8 2.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3nccn3C)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
60141574 73293 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 394 5 1 5 4.0 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc12 10.1016/j.bmc.2012.02.020
CHEMBL2012639 73293 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 394 5 1 5 4.0 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc12 10.1016/j.bmc.2012.02.020
18560538 10606 None 9 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.3 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170086 10606 None 9 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.3 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
621659 62749 None 8 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783965 62749 None 8 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
7184886 10609 None 1 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170091 10609 None 1 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224973 202073 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.8 C/C(=C/c1ccccc1)n1c2c(c3cc(F)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
CHEMBL592751 202073 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.8 C/C(=C/c1ccccc1)n1c2c(c3cc(F)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
49836620 18661 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276925 18661 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
45378935 201961 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591939 201961 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
73349123 91991 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 516 5 0 8 3.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c3OCCO4)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414707 91991 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 516 5 0 8 3.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c3OCCO4)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
18590836 10569 None 8 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 4 1 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(F)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169722 10569 None 8 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 4 1 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(F)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
45487129 200262 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL572092 200262 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
25117676 202915 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598444 202915 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
135339817 181590 None 0 Human Functional pIC50 = 7.4 7.4 -6 5
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
CHEMBL4764679 181590 None 0 Human Functional pIC50 = 7.4 7.4 -6 5
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
45113401 9111 None 1 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 435 5 2 3 4.7 O=S(=O)(Nc1cccc(F)c1)c1ccc2[nH]c3c(c2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2009.10.035
CHEMBL1099285 9111 None 1 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 435 5 2 3 4.7 O=S(=O)(Nc1cccc(F)c1)c1ccc2[nH]c3c(c2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2009.10.035
118727451 117506 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3ccc(NS(=O)(=O)c4cccc5ccccc45)cc3s2)CC1 10.1016/j.bmc.2015.01.032
CHEMBL3398399 117506 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3ccc(NS(=O)(=O)c4cccc5ccccc45)cc3s2)CC1 10.1016/j.bmc.2015.01.032
10286610 120928 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assayAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assay
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL355905 120928 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assayAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assay
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
52918032 57660 None 4 Human Functional pIC50 = 8.4 8.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668564 57660 None 4 Human Functional pIC50 = 8.4 8.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 nan
53322258 57661 None 4 Human Functional pIC50 = 8.4 8.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668565 57661 None 4 Human Functional pIC50 = 8.4 8.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357784 129103 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(C)cc(-c3ccncc3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670290 129103 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(C)cc(-c3ccncc3)nc2c1S(=O)(=O)c1ccccc1 nan
53326178 57692 None 4 Human Functional pIC50 = 8.4 8.4 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668596 57692 None 4 Human Functional pIC50 = 8.4 8.4 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
44389023 62535 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
CHEMBL178193 62535 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
44554393 18554 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1275630 18554 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
4106 2502 None 21 Human Functional pIC50 = 8.3 8.3 -29 7
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
5358812 2502 None 21 Human Functional pIC50 = 8.3 8.3 -29 7
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
89 2502 None 21 Human Functional pIC50 = 8.3 8.3 -29 7
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
CHEMBL93240 2502 None 21 Human Functional pIC50 = 8.3 8.3 -29 7
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
4106 2502 None 21 Human Functional pIC50 = 8.3 8.3 -29 7
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
5358812 2502 None 21 Human Functional pIC50 = 8.3 8.3 -29 7
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
89 2502 None 21 Human Functional pIC50 = 8.3 8.3 -29 7
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
CHEMBL93240 2502 None 21 Human Functional pIC50 = 8.3 8.3 -29 7
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
57400234 71564 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71564 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71564 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
49836716 18670 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1277011 18670 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
7184883 10900 None 2 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172725 10900 None 2 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
118512841 156547 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 417 7 1 4 4.5 Cc1c(Cl)cccc1S(=O)(=O)NCc1cc(CC(C)C)n(-c2ccccc2)n1 10.1016/j.bmcl.2017.07.031
CHEMBL4067243 156547 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 417 7 1 4 4.5 Cc1c(Cl)cccc1S(=O)(=O)NCc1cc(CC(C)C)n(-c2ccccc2)n1 10.1016/j.bmcl.2017.07.031
44126327 204110 None 4 Human Functional pIC50 = 5.4 5.4 -41 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 372 3 0 2 5.2 Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL606036 204110 None 4 Human Functional pIC50 = 5.4 5.4 -41 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 372 3 0 2 5.2 Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
45487128 200243 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL571878 200243 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
18560556 10921 None 10 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172867 10921 None 10 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
53320926 57663 None 4 Human Functional pIC50 = 6.4 6.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1668567 57663 None 4 Human Functional pIC50 = 6.4 6.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 nan
9929294 64101 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180765 64101 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44388999 63401 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179592 63401 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
10115854 69621 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193450 69621 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
54581998 62755 None 2 Human Functional pIC50 = 4.4 4.4 -5 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 368 4 0 4 4.3 CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783972 62755 None 2 Human Functional pIC50 = 4.4 4.4 -5 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 368 4 0 4 4.3 CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
45378936 201962 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591940 201962 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
54581997 62750 None 5 Human Functional pIC50 = 5.4 5.4 -11 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783966 62750 None 5 Human Functional pIC50 = 5.4 5.4 -11 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
16117152 60106 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642885 60106 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739101 60106 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
44126330 62744 None 4 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783960 62744 None 4 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
57520122 73294 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 410 5 1 5 4.5 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1016/j.bmc.2012.02.020
CHEMBL2012643 73294 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 410 5 1 5 4.5 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1016/j.bmc.2012.02.020
45378934 204103 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL605971 204103 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
57396813 71569 None 0 Human Functional pIC50 = 7.4 7.4 39 4
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71569 None 0 Human Functional pIC50 = 7.4 7.4 39 4
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71569 None 0 Human Functional pIC50 = 7.4 7.4 39 4
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
53323601 57689 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668593 57689 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
46189980 68916 None 3 Human Functional pIC50 = 7.4 7.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922639 68916 None 3 Human Functional pIC50 = 7.4 7.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
21254909 57638 None 2 Human Functional pIC50 = 6.4 6.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668501 57638 None 2 Human Functional pIC50 = 6.4 6.4 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
53318142 60110 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642867 60110 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739135 60110 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
16049388 82054 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165527 82054 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
20901141 10712 None 5 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170887 10712 None 5 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
10068007 18794 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278090 18794 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
44474631 14087 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197618 14087 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL578631 14087 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
7246142 10926 None 7 Human Functional pIC50 = 6.3 6.3 85 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172934 10926 None 7 Human Functional pIC50 = 6.3 6.3 85 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901139 10960 None 5 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173282 10960 None 5 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53320927 57666 None 4 Human Functional pIC50 = 6.3 6.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668570 57666 None 4 Human Functional pIC50 = 6.3 6.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
71770822 91997 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 414 4 0 6 2.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2013.05.051
CHEMBL2414726 91997 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 414 4 0 6 2.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2013.05.051
46884709 8082 None 4 Human Functional pIC50 = 6.3 6.3 - 1
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091208 8082 None 4 Human Functional pIC50 = 6.3 6.3 - 1
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
16116898 60148 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1642877 60148 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1739545 60148 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
18591271 10660 None 11 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 473 5 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170466 10660 None 11 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 473 5 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901160 10920 None 6 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172866 10920 None 6 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
44403097 72470 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198827 72470 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44435644 89163 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236571 89163 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
118727443 117498 None 0 Human Functional pIC50 = 5.3 5.3 -7 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 417 6 0 7 2.8 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(F)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398390 117498 None 0 Human Functional pIC50 = 5.3 5.3 -7 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 417 6 0 7 2.8 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(F)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
44516817 57680 None 4 Human Functional pIC50 = 8.3 8.3 1023 2
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668584 57680 None 4 Human Functional pIC50 = 8.3 8.3 1023 2
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44156624 57687 None 4 Human Functional pIC50 = 8.3 8.3 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1668591 57687 None 4 Human Functional pIC50 = 8.3 8.3 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
162646407 179729 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4742804 179729 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
45484340 199282 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565746 199282 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
162656068 180922 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4756814 180922 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
44435603 91784 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL240922 91784 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435640 155019 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL401019 155019 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
49799684 10947 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 436 5 0 9 3.2 CN(Cc1cccnc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173136 10947 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 436 5 0 9 3.2 CN(Cc1cccnc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901125 10981 None 5 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 5 1 9 3.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173435 10981 None 5 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 5 1 9 3.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
6625986 10608 None 9 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170088 10608 None 9 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
25123012 204166 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
CHEMBL606401 204166 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
126720394 162408 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164541 162408 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
58357663 129097 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 426 5 0 8 4.1 CSc1nn2c(C)c(Oc3cccnc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670283 129097 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 426 5 0 8 4.1 CSc1nn2c(C)c(Oc3cccnc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357754 129101 None 4 Human Functional pIC50 = 7.3 7.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670288 129101 None 4 Human Functional pIC50 = 7.3 7.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
9924959 69486 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193358 69486 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
16019364 10961 None 5 Human Functional pIC50 = 6.3 6.3 53 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 467 5 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173283 10961 None 5 Human Functional pIC50 = 6.3 6.3 53 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 467 5 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
53318300 57636 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668499 57636 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
71813685 91631 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 400 4 2 4 2.9 Cc1ccc(N2CCc3c(NS(=O)(=O)c4ccc(F)cc4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407562 91631 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 400 4 2 4 2.9 Cc1ccc(N2CCc3c(NS(=O)(=O)c4ccc(F)cc4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
18559939 10635 None 11 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170273 10635 None 11 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
24794436 14074 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL1197511 14074 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL574856 14074 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
25263300 184724 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484926 184724 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
10136837 166058 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
CHEMBL425196 166058 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
10136837 166058 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL425196 166058 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
44474797 14069 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL1197505 14069 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574625 14069 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
49836508 18777 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
CHEMBL1277998 18777 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
57402187 69772 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935597 69772 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
20901263 10683 None 5 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170680 10683 None 5 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16956087 10985 None 10 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 1 8 5.1 CC(Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1173502 10985 None 10 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 1 8 5.1 CC(Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
49836619 18651 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276839 18651 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
46224916 201926 None 2 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 332 3 0 3 4.6 COc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL591569 201926 None 2 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 332 3 0 3 4.6 COc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
46224943 202032 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 374 2 0 2 5.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592515 202032 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 374 2 0 2 5.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
53319441 60119 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642845 60119 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739231 60119 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
44435622 89134 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236540 89134 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44403099 133078 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370215 133078 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
126720425 162208 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4161308 162208 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
58357826 129835 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 377 5 1 7 2.1 CNc1nn2c(C)cc(CN(C)C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL3675196 129835 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 377 5 1 7 2.1 CNc1nn2c(C)cc(CN(C)C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
118512827 146519 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 437 7 1 4 4.9 CC(C)Cc1cc(CNS(=O)(=O)c2c(Cl)cccc2Cl)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3921947 146519 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 437 7 1 4 4.9 CC(C)Cc1cc(CNS(=O)(=O)c2c(Cl)cccc2Cl)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
49836618 18650 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276838 18650 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
18560564 10617 None 8 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170100 10617 None 8 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224877 203157 None 4 Human Functional pIC50 = 5.2 5.2 -74 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL599913 203157 None 4 Human Functional pIC50 = 5.2 5.2 -74 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
23725134 14059 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL1197475 14059 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL573521 14059 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
71813986 91626 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 416 5 2 5 2.6 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407547 91626 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 416 5 2 5 2.6 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
20901126 10568 None 6 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169709 10568 None 6 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16956089 10897 None 9 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 527 6 0 8 5.0 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172722 10897 None 9 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 527 6 0 8 5.0 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
7184892 10941 None 8 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 1 8 3.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173063 10941 None 8 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 1 8 3.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
49799656 10978 None 2 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173432 10978 None 2 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL3216262 10978 None 2 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
54584885 62746 None 4 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783962 62746 None 4 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
44474470 14066 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL1197489 14066 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL573981 14066 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
16019546 10714 None 5 Human Functional pIC50 = 7.2 7.2 676 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170891 10714 None 5 Human Functional pIC50 = 7.2 7.2 676 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901133 10639 None 5 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 4 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170279 10639 None 5 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 4 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901186 10641 None 5 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.3 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170281 10641 None 5 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.3 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16019514 10870 None 5 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.1 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172406 10870 None 5 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.1 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
44224259 62743 None 4 Human Functional pIC50 = 5.2 5.2 -30 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783959 62743 None 4 Human Functional pIC50 = 5.2 5.2 -30 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
44155109 8176 None 4 Human Functional pIC50 = 8.2 8.2 21 2
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1091919 8176 None 4 Human Functional pIC50 = 8.2 8.2 21 2
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
57400234 71564 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71564 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71564 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
44156863 8080 None 0 Human Functional pIC50 = 8.2 8.2 21 2
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091206 8080 None 0 Human Functional pIC50 = 8.2 8.2 21 2
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
44156622 57688 None 4 Human Functional pIC50 = 8.2 8.2 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668592 57688 None 4 Human Functional pIC50 = 8.2 8.2 - 1
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
10449488 199322 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565976 199322 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
118181414 191304 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5189271 191304 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
126720397 181201 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4760105 181201 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
162644347 181865 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4777550 181865 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
57393468 69774 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935599 69774 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
46880757 6030 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080381 6030 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
20901264 10969 None 7 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 6 1 8 4.0 CCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173360 10969 None 7 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 6 1 8 4.0 CCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901122 10589 None 5 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 4 1 8 4.1 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1169903 10589 None 5 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 4 1 8 4.1 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
18560317 10919 None 9 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 5 1 8 5.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1172862 10919 None 9 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 5 1 8 5.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
68261572 129832 None 4 Human Functional pIC50 = 5.2 5.2 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675193 129832 None 4 Human Functional pIC50 = 5.2 5.2 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
10140915 140442 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380772 140442 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
20901229 10987 None 1 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 409 2 1 8 2.5 Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173506 10987 None 1 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 409 2 1 8 2.5 Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
11595209 94894 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253708 94894 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
49836616 18810 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278179 18810 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
45113534 14233 None 1 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1097613 14233 None 1 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199141 14233 None 1 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
45113399 9110 None 4 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 348 2 1 4 1.1 CN1CCN(S(=O)(=O)c2ccc3[nH]c4c(c3c2)CN(C)CC4)CC1 10.1016/j.ejmech.2009.10.035
CHEMBL1099283 9110 None 4 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 348 2 1 4 1.1 CN1CCN(S(=O)(=O)c2ccc3[nH]c4c(c3c2)CN(C)CC4)CC1 10.1016/j.ejmech.2009.10.035
57391567 71561 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71561 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71561 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
20901115 10968 None 5 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173359 10968 None 5 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
118727444 117499 None 0 Human Functional pIC50 = 5.2 5.2 -25 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 525 6 0 7 3.3 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(I)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398391 117499 None 0 Human Functional pIC50 = 5.2 5.2 -25 2
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 525 6 0 7 3.3 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(I)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
54585847 62752 None 5 Human Functional pIC50 = 5.2 5.2 -29 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783968 62752 None 5 Human Functional pIC50 = 5.2 5.2 -29 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
44435626 154948 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
CHEMBL400608 154948 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
16019397 10963 None 10 Human Functional pIC50 = 6.2 6.2 54 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173286 10963 None 10 Human Functional pIC50 = 6.2 6.2 54 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
71769315 91995 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 508 5 0 6 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414722 91995 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 508 5 0 6 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
44126325 201570 None 4 Human Functional pIC50 = 6.2 6.2 -10 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 334 4 0 3 4.2 COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589147 201570 None 4 Human Functional pIC50 = 6.2 6.2 -10 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 334 4 0 3 4.2 COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
57396813 71569 None 0 Human Functional pIC50 = 7.2 7.2 39 4
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71569 None 0 Human Functional pIC50 = 7.2 7.2 39 4
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71569 None 0 Human Functional pIC50 = 7.2 7.2 39 4
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
20901210 10923 None 3 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 1 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172869 10923 None 3 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 1 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
71813835 91624 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 412 5 2 5 2.7 COc1cccc(S(=O)(=O)Nc2n[nH]c3c2CCN(c2ccc(C)cc2)C3=O)c1 10.1016/j.bmcl.2013.05.100
CHEMBL2407542 91624 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 412 5 2 5 2.7 COc1cccc(S(=O)(=O)Nc2n[nH]c3c2CCN(c2ccc(C)cc2)C3=O)c1 10.1016/j.bmcl.2013.05.100
20901259 10970 None 5 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 4.3 CC(C)CCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173361 10970 None 5 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 4.3 CC(C)CCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
57393467 69770 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935595 69770 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
18560324 10713 None 8 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170890 10713 None 8 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
44435630 89710 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL237593 89710 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
7185121 10610 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 387 6 1 8 3.4 CCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170092 10610 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 387 6 1 8 3.4 CCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901265 10738 None 6 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1171041 10738 None 6 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
126720403 162705 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4169236 162705 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
16019574 10885 None 10 Human Functional pIC50 = 6.2 6.2 14 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172596 10885 None 10 Human Functional pIC50 = 6.2 6.2 14 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901253 10925 None 1 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 365 2 1 8 2.4 Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172933 10925 None 1 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 365 2 1 8 2.4 Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46225000 201571 None 4 Human Functional pIC50 = 6.2 6.2 -9 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589148 201571 None 4 Human Functional pIC50 = 6.2 6.2 -9 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
118181454 190070 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5170650 190070 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
9969402 70571 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194750 70571 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44403104 72504 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198941 72504 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44155107 8081 None 4 Human Functional pIC50 = 8.1 8.1 60 2
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091207 8081 None 4 Human Functional pIC50 = 8.1 8.1 60 2
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
44537940 18781 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1278001 18781 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
44403065 166407 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL427184 166407 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
46830134 8219 None 0 Human Functional pIC50 = 8.1 8.1 37 2
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1092241 8219 None 0 Human Functional pIC50 = 8.1 8.1 37 2
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
46830134 8219 None 0 Human Functional pIC50 = 8.1 8.1 37 2
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1092241 8219 None 0 Human Functional pIC50 = 8.1 8.1 37 2
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44435632 89503 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237179 89503 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25122653 202983 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL598850 202983 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
71813988 91627 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 428 6 2 6 2.4 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(OC)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407549 91627 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 428 6 2 6 2.4 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(OC)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
16019519 10972 None 4 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173364 10972 None 4 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
58357699 129102 None 4 Human Functional pIC50 = 6.1 6.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 442 5 1 8 3.7 CNc1nn2c(-c3ccccn3)cc(-c3ccccn3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670289 129102 None 4 Human Functional pIC50 = 6.1 6.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 442 5 1 8 3.7 CNc1nn2c(-c3ccccn3)cc(-c3ccccn3)nc2c1S(=O)(=O)c1ccccc1 nan
53316984 57664 None 4 Human Functional pIC50 = 7.1 7.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668568 57664 None 4 Human Functional pIC50 = 7.1 7.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
16019303 10603 None 5 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170069 10603 None 5 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901275 10664 None 6 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170474 10664 None 6 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16019310 10763 None 10 Human Functional pIC50 = 6.1 6.1 47 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 453 5 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1171436 10763 None 10 Human Functional pIC50 = 6.1 6.1 47 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 453 5 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
71815503 117501 None 0 Human Functional pIC50 = 6.1 6.1 -3 3
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 429 7 0 8 2.7 COc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
CHEMBL3398394 117501 None 0 Human Functional pIC50 = 6.1 6.1 -3 3
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 429 7 0 8 2.7 COc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
71769066 91993 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 536 6 0 7 5.1 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(-c2ccccc2)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
CHEMBL2414712 91993 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 536 6 0 7 5.1 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(-c2ccccc2)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
54585848 62754 None 5 Human Functional pIC50 = 5.1 5.1 -5 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 316 3 0 4 3.1 CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783971 62754 None 5 Human Functional pIC50 = 5.1 5.1 -5 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 316 3 0 4 3.1 CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
20901142 10767 None 1 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1171500 10767 None 1 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
24763352 62643 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783601 62643 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
46880759 6134 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080899 6134 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
53319628 57679 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668583 57679 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
44403089 133698 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL371469 133698 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
24783294 176817 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
CHEMBL459987 176817 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
71814155 91628 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 425 4 3 5 2.1 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1C1CCNCC1 10.1016/j.bmcl.2013.05.100
CHEMBL2407551 91628 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 425 4 3 5 2.1 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1C1CCNCC1 10.1016/j.bmcl.2013.05.100
20901136 10973 None 5 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 9 4.0 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173365 10973 None 5 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 9 4.0 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
45113530 14228 None 3 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1095274 14228 None 3 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199079 14228 None 3 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
46189982 129833 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 6 2 7 2.1 CNc1nn2c(C)c(CCCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675194 129833 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 6 2 7 2.1 CNc1nn2c(C)c(CCCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
18591267 10642 None 10 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170282 10642 None 10 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
49799656 10978 None 2 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173432 10978 None 2 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL3216262 10978 None 2 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
57391567 71561 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71561 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71561 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
18560184 10866 None 8 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172398 10866 None 8 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
86302554 110896 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260795 110896 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
44433199 88810 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236314 88810 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24771120 184206 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
CHEMBL482562 184206 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
9978683 18681 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
CHEMBL1277104 18681 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
16118923 60166 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642866 60166 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739656 60166 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
44403093 71462 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196094 71462 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
9950255 199271 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565723 199271 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
57398803 69764 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935589 69764 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1949758 69764 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
44388956 63107 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178870 63107 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
10383646 18769 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277917 18769 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
44389003 123903 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL362487 123903 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
46880709 7449 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
CHEMBL1086720 7449 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
20901169 10690 None 5 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(Cl)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
CHEMBL1170687 10690 None 5 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(Cl)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
11723168 209953 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
CHEMBL94422 209953 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
44397689 71464 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196102 71464 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL373107 71464 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
46880758 6097 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080729 6097 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
16019343 10583 None 4 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1169894 10583 None 4 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
20901124 10634 None 5 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 475 4 1 8 4.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170271 10634 None 5 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 475 4 1 8 4.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
18591266 10931 None 10 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 6 1 8 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173004 10931 None 10 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 6 1 8 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
45487140 201289 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL583677 201289 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
54582938 62739 None 5 Human Functional pIC50 = 5.1 5.1 -1 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783955 62739 None 5 Human Functional pIC50 = 5.1 5.1 -1 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
58357860 129095 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670281 129095 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
45113403 9070 None 1 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 344 2 1 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1098894 9070 None 1 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 344 2 1 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
9842551 127290 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365774 127290 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
44126329 62738 None 5 Human Functional pIC50 = 6.1 6.1 2 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783954 62738 None 5 Human Functional pIC50 = 6.1 6.1 2 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
18560255 10719 None 8 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 9 4.5 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170897 10719 None 8 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 9 4.5 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
18559286 10994 None 8 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173575 10994 None 8 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
7183407 10995 None 11 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173576 10995 None 11 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
162647425 179683 None 1 Human Functional pIC50 = 6.1 6.1 - 1
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4741978 179683 None 1 Human Functional pIC50 = 6.1 6.1 - 1
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
16116896 60160 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642861 60160 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739644 60160 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
53320746 60170 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642854 60170 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739685 60170 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
46224879 204004 None 3 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 204004 None 3 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
49799629 10940 None 1 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 416 6 0 9 2.2 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173062 10940 None 1 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 416 6 0 9 2.2 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
118512807 150480 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 425 7 1 4 4.8 CC(C)Cc1cc(CNS(=O)(=O)c2ccc(C(C)(C)C)cc2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3953555 150480 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 425 7 1 4 4.8 CC(C)Cc1cc(CNS(=O)(=O)c2ccc(C(C)(C)C)cc2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
16116899 60120 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642846 60120 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739232 60120 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
25123011 203650 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
CHEMBL603483 203650 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
11723168 209953 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL94422 209953 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
197033 201608 None 42 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL589390 201608 None 42 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
18559285 10928 None 6 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 443 5 1 9 3.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172939 10928 None 6 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 443 5 1 9 3.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
197033 201608 None 42 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 201608 None 42 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
54579957 62748 None 4 Human Functional pIC50 = 5.1 5.1 -36 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783964 62748 None 4 Human Functional pIC50 = 5.1 5.1 -36 2
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
56849578 68895 None 4 Human Functional pIC50 = 8.1 8.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922618 68895 None 4 Human Functional pIC50 = 8.1 8.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189935 68910 None 3 Human Functional pIC50 = 8.1 8.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922633 68910 None 3 Human Functional pIC50 = 8.1 8.1 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
44389099 64858 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182000 64858 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
44389015 122396 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL359876 122396 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44435538 90640 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
CHEMBL238770 90640 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
44388943 63310 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL179277 63310 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
53327611 69776 None 0 Human Functional pIC50 = 8.0 8.0 154 2
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69776 None 0 Human Functional pIC50 = 8.0 8.0 154 2
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
53323436 60152 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642870 60152 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739585 60152 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
16019366 10679 None 3 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170671 10679 None 3 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
18559353 10643 None 10 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 5.0 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170288 10643 None 10 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 5.0 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
53326022 60161 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642863 60161 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739645 60161 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
44435618 88816 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236334 88816 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46224881 203420 None 4 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 4.9 Cc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL601902 203420 None 4 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 4.9 Cc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
53323600 57675 None 2 Human Functional pIC50 = 6.0 6.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668579 57675 None 2 Human Functional pIC50 = 6.0 6.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
20901270 10659 None 5 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170465 10659 None 5 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
16019292 10997 None 6 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173578 10997 None 6 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53319443 60174 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642858 60174 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739696 60174 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
16956204 10984 None 5 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 529 6 1 9 4.6 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173501 10984 None 5 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 529 6 1 9 4.6 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16117154 60167 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642881 60167 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739657 60167 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
46880658 6382 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1082199 6382 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
16118797 60117 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642852 60117 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739216 60117 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
44435620 149082 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394231 149082 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44474629 14084 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL1197581 14084 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL577570 14084 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
57393365 71574 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71574 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71574 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
23624309 176838 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460195 176838 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
44403092 70658 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL195018 70658 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10272325 71765 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL196619 71765 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
16019394 10869 None 7 Human Functional pIC50 = 6.0 6.0 37 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172405 10869 None 7 Human Functional pIC50 = 6.0 6.0 37 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019604 10977 None 2 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173431 10977 None 2 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
3241 3521 None 18 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
6918649 3521 None 18 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
CHEMBL1210710 3521 None 18 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
11256720 2055 None 52 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
9444 2055 None 52 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
CHEMBL1083390 2055 None 52 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
DB12680 2055 None 52 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
44126272 201606 None 4 Human Functional pIC50 = 6.0 6.0 -14 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 358 3 0 2 4.9 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589388 201606 None 4 Human Functional pIC50 = 6.0 6.0 -14 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 358 3 0 2 4.9 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
44126326 202075 None 6 Human Functional pIC50 = 6.0 6.0 -32 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592753 202075 None 6 Human Functional pIC50 = 6.0 6.0 -32 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
46884709 8082 None 4 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091208 8082 None 4 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
58357740 129099 None 0 Human Functional pIC50 = 6 6.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL3670285 129099 None 0 Human Functional pIC50 = 6 6.0 - 1
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
58158749 139082 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785512 139082 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
54752954 139037 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785100 139037 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
46189932 68907 None 4 Human Functional pKd = 9.4 9.4 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922630 68907 None 4 Human Functional pKd = 9.4 9.4 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56655504 68891 None 3 Human Functional pKd = 9.3 9.3 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922614 68891 None 3 Human Functional pKd = 9.3 9.3 - 1
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44216882 139202 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786752 139202 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
58158721 139079 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785453 139079 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595671 65699 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834333 65699 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
6918542 207382 None 20 Human Functional pKd = 8.9 8.9 - 0
Antagonistic activity towards 5-hydroxytryptamine 6 receptorAntagonistic activity towards 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL76237 207382 None 20 Human Functional pKd = 8.9 8.9 - 0
Antagonistic activity towards 5-hydroxytryptamine 6 receptorAntagonistic activity towards 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
44240860 139269 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787525 139269 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
56593934 65716 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
CHEMBL1834350 65716 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
56595402 65658 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65658 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595531 65667 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
CHEMBL1834235 65667 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
56593797 65708 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834341 65708 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
56593933 65715 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
CHEMBL1834349 65715 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
58158719 139078 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785431 139078 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
59339383 139223 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787014 139223 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595670 65698 None 0 Human Functional pKd = 7 7.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834332 65698 None 0 Human Functional pKd = 7 7.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
56593643 65701 None 0 Human Functional pKd = 7 7.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834335 65701 None 0 Human Functional pKd = 7 7.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
56593803 65712 None 0 Human Functional pKd = 7 7.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
CHEMBL1834346 65712 None 0 Human Functional pKd = 7 7.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
58158748 139180 None 0 Human Functional pKd = 7 7.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786563 139180 None 0 Human Functional pKd = 7 7.0 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
10356663 112006 None 0 Human Functional pKd = 7 7.0 - 1
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL328816 112006 None 0 Human Functional pKd = 7 7.0 - 1
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
56595667 65672 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834241 65672 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158707 139135 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786087 139135 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595533 65668 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
CHEMBL1834237 65668 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
56593799 65710 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834343 65710 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
127033666 139058 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785278 139058 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595280 65657 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834225 65657 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
25056080 65711 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834345 65711 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
56595280 65657 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834225 65657 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
25056080 65711 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834345 65711 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
56593644 65702 None 0 Human Functional pKd = 6.8 6.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834336 65702 None 0 Human Functional pKd = 6.8 6.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
127031618 139256 None 0 Human Functional pKd = 5.8 5.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 405 4 2 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(N)cc1 10.1016/j.bmcl.2016.02.001
CHEMBL3787388 139256 None 0 Human Functional pKd = 5.8 5.8 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 405 4 2 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(N)cc1 10.1016/j.bmcl.2016.02.001
56595529 65666 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
CHEMBL1834234 65666 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
56595529 65666 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
CHEMBL1834234 65666 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
56593646 65704 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834338 65704 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
58158738 139049 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785231 139049 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
56593642 65700 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834334 65700 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158668 139115 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785864 139115 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
56593798 65709 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834342 65709 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
58158739 139244 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787201 139244 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56593932 65714 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
CHEMBL1834348 65714 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
59339335 139093 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785626 139093 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
53310757 139221 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786973 139221 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56849719 68904 None 3 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922627 68904 None 3 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56595402 65658 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65658 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595668 65673 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834242 65673 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595405 65661 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
70878688 65661 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
CHEMBL1834229 65661 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
56595535 65670 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
CHEMBL1834239 65670 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
56595402 65658 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65658 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595402 65658 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834226 65658 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
44240753 139197 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786693 139197 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
44240802 139268 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787508 139268 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595403 65659 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834227 65659 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
24855787 65655 None 1 Human Functional pKd = 8.2 8.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834221 65655 None 1 Human Functional pKd = 8.2 8.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
56595404 65660 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
CHEMBL1834228 65660 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
56595666 65671 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834240 65671 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
56593931 65713 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
CHEMBL1834347 65713 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
56593936 65718 None 0 Human Functional pKd = 7.2 7.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834352 65718 None 0 Human Functional pKd = 7.2 7.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
56593936 65718 None 0 Human Functional pKd = 7.2 7.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834352 65718 None 0 Human Functional pKd = 7.2 7.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
127032424 139198 None 0 Human Functional pKd = 7.2 7.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786703 139198 None 0 Human Functional pKd = 7.2 7.2 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595406 65663 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
CHEMBL1834230 65663 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
56595534 65669 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
CHEMBL1834238 65669 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
56593645 65703 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834337 65703 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
56593647 65705 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834339 65705 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
56665086 65707 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834340 65707 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
58158682 139054 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785259 139054 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595407 65664 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
CHEMBL1834231 65664 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
56595669 65674 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834243 65674 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158709 139246 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787246 139246 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595408 65665 None 0 Human Functional pKd = 6.1 6.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
CHEMBL1834232 65665 None 0 Human Functional pKd = 6.1 6.1 - 0
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
56849576 68893 None 4 Human Functional pKi = 9.9 9.9 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922616 68893 None 4 Human Functional pKi = 9.9 9.9 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849576 68893 None 4 Human Functional pKi = 9.9 9.9 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922616 68893 None 4 Human Functional pKi = 9.9 9.9 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
10131620 102533 None 1 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413990 102533 None 1 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040186 102533 None 1 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44156626 57686 None 4 Human Functional pKi = 9.7 9.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668590 57686 None 4 Human Functional pKi = 9.7 9.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
56655571 68909 None 37 Human Functional pKi = 9.7 9.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 4 1 7 2.3 CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922632 68909 None 37 Human Functional pKi = 9.7 9.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 4 1 7 2.3 CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849575 68892 None 4 Human Functional pKi = 9.7 9.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922615 68892 None 4 Human Functional pKi = 9.7 9.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53326176 57682 None 4 Human Functional pKi = 9.6 9.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668586 57682 None 4 Human Functional pKi = 9.6 9.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44516817 57680 None 4 Human Functional pKi = 9.6 9.6 1023 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668584 57680 None 4 Human Functional pKi = 9.6 9.6 1023 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44156754 6512 None 4 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082763 6512 None 4 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
44516817 57680 None 4 Human Functional pKi = 9.6 9.6 1023 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57680 None 4 Human Functional pKi = 9.6 9.6 1023 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
44516817 57680 None 4 Human Functional pKi = 9.6 9.6 1023 2
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1668584 57680 None 4 Human Functional pKi = 9.6 9.6 1023 2
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44516817 57680 None 4 Human Functional pKi = 9.6 9.6 1023 2
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1668584 57680 None 4 Human Functional pKi = 9.6 9.6 1023 2
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
52918032 57660 None 4 Human Functional pKi = 9.6 9.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668564 57660 None 4 Human Functional pKi = 9.6 9.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
53322258 57661 None 4 Human Functional pKi = 9.6 9.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668565 57661 None 4 Human Functional pKi = 9.6 9.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56655504 68891 None 3 Human Functional pKi = 9.5 9.5 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922614 68891 None 3 Human Functional pKi = 9.5 9.5 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3509 None 17 Mouse Functional pKi = 9.5 9.5 - 1
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3509 None 17 Mouse Functional pKi = 9.5 9.5 - 1
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3509 None 17 Mouse Functional pKi = 9.5 9.5 - 1
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
56849579 68896 None 3 Human Functional pKi = 9.5 9.5 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922619 68896 None 3 Human Functional pKi = 9.5 9.5 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44156628 6716 None 4 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083654 6716 None 4 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
44156622 57688 None 4 Human Functional pKi = 9.4 9.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668592 57688 None 4 Human Functional pKi = 9.4 9.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
44156752 6582 None 4 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083075 6582 None 4 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
46190037 68915 None 2 Human Functional pKi = 9.4 9.4 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 407 5 1 7 2.9 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922638 68915 None 2 Human Functional pKi = 9.4 9.4 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 407 5 1 7 2.9 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53326177 57684 None 4 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668588 57684 None 4 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44156624 57687 None 4 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668591 57687 None 4 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
46189932 68907 None 4 Human Functional pKi = 9.3 9.3 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922630 68907 None 4 Human Functional pKi = 9.3 9.3 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
46867519 6510 None 4 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082761 6510 None 4 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
46189984 68912 None 1 Human Functional pKi = 9.3 9.3 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922635 68912 None 1 Human Functional pKi = 9.3 9.3 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53316984 57664 None 4 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668568 57664 None 4 Human Functional pKi = 9.3 9.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56849578 68895 None 4 Human Functional pKi = 9.2 9.2 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922618 68895 None 4 Human Functional pKi = 9.2 9.2 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53326178 57692 None 4 Human Functional pKi = 9.2 9.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668596 57692 None 4 Human Functional pKi = 9.2 9.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
46189935 68910 None 3 Human Functional pKi = 9.2 9.2 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922633 68910 None 3 Human Functional pKi = 9.2 9.2 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
46190034 68913 None 0 Human Functional pKi = 9.2 9.2 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922636 68913 None 0 Human Functional pKi = 9.2 9.2 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3509 None 17 Mouse Functional pKi = 9.1 9.1 - 1
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3509 None 17 Mouse Functional pKi = 9.1 9.1 - 1
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3509 None 17 Mouse Functional pKi = 9.1 9.1 - 1
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
44155994 57667 None 4 Human Functional pKi = 9.1 9.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668571 57667 None 4 Human Functional pKi = 9.1 9.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
6918479 56677 None 0 Human Functional pKi = 9.1 9.1 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm201079g
CHEMBL1642114 56677 None 0 Human Functional pKi = 9.1 9.1 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm201079g
56849857 68914 None 3 Human Functional pKi = 9.1 9.1 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 391 5 1 7 2.4 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922637 68914 None 3 Human Functional pKi = 9.1 9.1 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 391 5 1 7 2.4 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
56655505 68906 None 3 Human Functional pKi = 9.0 9.0 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922629 68906 None 3 Human Functional pKi = 9.0 9.0 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44155992 57668 None 4 Human Functional pKi = 9.0 9.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668572 57668 None 4 Human Functional pKi = 9.0 9.0 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
53322935 57685 None 4 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668589 57685 None 4 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
44155874 57637 None 19 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668500 57637 None 19 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
44155874 57637 None 19 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668500 57637 None 19 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579181 191061 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 374 2 0 4 3.6 CN1CCc2cc3ccn(S(=O)(=O)c4cccc(Cl)c4)c3cc2CC1 10.1016/j.bmcl.2008.08.010
CHEMBL518591 191061 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 374 2 0 4 3.6 CN1CCc2cc3ccn(S(=O)(=O)c4cccc(Cl)c4)c3cc2CC1 10.1016/j.bmcl.2008.08.010
46890885 6903 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1084315 6903 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46189980 68916 None 3 Human Functional pKi = 8.9 8.9 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922639 68916 None 3 Human Functional pKi = 8.9 8.9 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
6918629 68940 None 0 Human Functional pKi = 8.9 8.9 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922716 68940 None 0 Human Functional pKi = 8.9 8.9 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
46189987 68911 None 3 Human Functional pKi = 8.9 8.9 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922634 68911 None 3 Human Functional pKi = 8.9 8.9 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
53324896 57681 None 4 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668585 57681 None 4 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
25110702 171380 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL446054 171380 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579085 190549 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL517828 190549 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
9944808 102525 None 4 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413989 102525 None 4 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040139 102525 None 4 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44476436 82379 None 8 Human Functional pKi = 8.7 8.7 7413 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172186 82379 None 8 Human Functional pKi = 8.7 8.7 7413 2
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
56849717 68903 None 3 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 1 7 2.0 CNc1nn2c(CN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922626 68903 None 3 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 1 7 2.0 CNc1nn2c(CN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849716 68902 None 2 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(CN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922625 68902 None 2 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(CN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44476434 82378 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172185 82378 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 10.1016/j.bmcl.2012.05.036
44155875 61003 None 0 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1762568 61003 None 0 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
10286330 182906 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccc2c(c1)CCNCC2)c1ccccc1 10.1016/j.bmcl.2008.08.010
CHEMBL479067 182906 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccc2c(c1)CCNCC2)c1ccccc1 10.1016/j.bmcl.2008.08.010
44579131 181730 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2ccc3cc4c(cc32)CCNCC4)c1 10.1016/j.bmcl.2008.08.010
CHEMBL477386 181730 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2ccc3cc4c(cc32)CCNCC4)c1 10.1016/j.bmcl.2008.08.010
44579182 182747 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 340 2 1 4 2.7 Cn1cc(S(=O)(=O)c2ccccc2)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478871 182747 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 340 2 1 4 2.7 Cn1cc(S(=O)(=O)c2ccccc2)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
53320929 57690 None 4 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 3 2 7 1.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668594 57690 None 4 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 3 2 7 1.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
5113605 79754 None 1 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1016/j.bmc.2013.05.040
CHEMBL211577 79754 None 1 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1016/j.bmc.2013.05.040
44579132 181731 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 327 2 1 5 2.0 O=S(=O)(c1ccccn1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL477387 181731 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 327 2 1 5 2.0 O=S(=O)(c1ccccn1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
46891114 6627 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 5 0 5 3.2 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
CHEMBL1083298 6627 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 5 0 5 3.2 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
46891174 6886 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 485 5 0 5 3.5 COc1cc(C)c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
CHEMBL1084214 6886 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 485 5 0 5 3.5 COc1cc(C)c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
53323601 57689 None 4 Human Functional pKi = 7.9 7.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668593 57689 None 4 Human Functional pKi = 7.9 7.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
56849713 68899 None 2 Human Functional pKi = 7.0 7.0 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922622 68899 None 2 Human Functional pKi = 7.0 7.0 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849713 68899 None 2 Human Functional pKi = 7.0 7.0 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922622 68899 None 2 Human Functional pKi = 7.0 7.0 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3509 None 17 Mouse Functional pKi = 6.9 6.9 - 1
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3509 None 17 Mouse Functional pKi = 6.9 6.9 - 1
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3509 None 17 Mouse Functional pKi = 6.9 6.9 - 1
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
53318300 57636 None 0 Human Functional pKi = 6.9 6.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668499 57636 None 0 Human Functional pKi = 6.9 6.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44476804 82382 None 2 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 392 3 0 7 2.4 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccc(F)cc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172190 82382 None 2 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 392 3 0 7 2.4 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccc(F)cc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
9822810 69524 None 0 Rat Functional pKi = 7.9 7.9 - 0
Binding affinity against 5-hydroxytryptamine 6 receptor of rat striatumBinding affinity against 5-hydroxytryptamine 6 receptor of rat striatum
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193400 69524 None 0 Rat Functional pKi = 7.9 7.9 - 0
Binding affinity against 5-hydroxytryptamine 6 receptor of rat striatumBinding affinity against 5-hydroxytryptamine 6 receptor of rat striatum
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
46882521 5713 None 0 Human Functional pKi = 6.9 6.9 - 2
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078207 5713 None 0 Human Functional pKi = 6.9 6.9 - 2
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
46891053 6513 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 7 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4nsnc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082764 6513 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 7 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4nsnc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891175 6945 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(-c4ccccc4)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1084482 6945 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(-c4ccccc4)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
53323599 57671 None 4 Human Functional pKi = 6.9 6.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668575 57671 None 4 Human Functional pKi = 6.9 6.9 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
52915983 61009 None 4 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 371 3 1 7 1.6 Cc1cc(C)n2nc(N3CCNCC3)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762574 61009 None 4 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 371 3 1 7 1.6 Cc1cc(C)n2nc(N3CCNCC3)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
44476607 82384 None 3 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172192 82384 None 3 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
44156502 61004 None 0 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762569 61004 None 0 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
58149665 82376 None 3 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172183 82376 None 3 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
45488151 199366 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
CHEMBL566213 199366 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
53320927 57666 None 4 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668570 57666 None 4 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
46882583 5758 None 0 Human Functional pKi = 7.8 7.8 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 453 5 2 6 2.6 CN1CCOc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc21 10.1016/j.bmcl.2009.09.027
CHEMBL1078491 5758 None 0 Human Functional pKi = 7.8 7.8 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 453 5 2 6 2.6 CN1CCOc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc21 10.1016/j.bmcl.2009.09.027
68014793 91962 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 323 4 1 3 4.2 CNc1cc(-c2ccccc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413987 91962 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 323 4 1 3 4.2 CNc1cc(-c2ccccc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
53324895 57662 None 4 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 10.1016/j.bmc.2010.12.055
CHEMBL1668566 57662 None 4 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 10.1016/j.bmc.2010.12.055
45102707 5759 None 0 Human Functional pKi = 6.8 6.8 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 465 6 2 6 3.9 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2009.09.027
CHEMBL1078492 5759 None 0 Human Functional pKi = 6.8 6.8 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 465 6 2 6 3.9 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2009.09.027
46890103 7151 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 437 4 1 5 2.3 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(N)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085361 7151 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 437 4 1 5 2.3 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(N)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
31386 96659 None 58 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 218 2 0 2 2.5 O=S(=O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL263327 96659 None 58 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 218 2 0 2 2.5 O=S(=O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.05.040
45488139 199403 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
CHEMBL566410 199403 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
45488143 200222 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
CHEMBL571762 200222 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
21254909 57638 None 2 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668501 57638 None 2 Human Functional pKi = 7.8 7.8 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56849714 68900 None 2 Human Functional pKi = 7.8 7.8 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922623 68900 None 2 Human Functional pKi = 7.8 7.8 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
45488166 199368 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
CHEMBL566219 199368 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
46867655 6658 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 411 3 1 7 2.2 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCCC2 10.1021/jm100350r
CHEMBL1083389 6658 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 411 3 1 7 2.2 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCCC2 10.1021/jm100350r
56849577 68894 None 4 Human Functional pKi = 7.7 7.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 385 3 2 7 2.8 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922617 68894 None 4 Human Functional pKi = 7.7 7.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 385 3 2 7 2.8 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
10934 1320 None 69 Human Functional pKi = 6.7 6.7 - 1
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
2955 1320 None 69 Human Functional pKi = 6.7 6.7 - 1
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
782 1320 None 69 Human Functional pKi = 6.7 6.7 - 1
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
CHEMBL1043 1320 None 69 Human Functional pKi = 6.7 6.7 - 1
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
DB00250 1320 None 69 Human Functional pKi = 6.7 6.7 - 1
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
46890886 6904 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 9 1 5 3.6 CCN(CC)CCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
CHEMBL1084316 6904 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 9 1 5 3.6 CCN(CC)CCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
46891112 7272 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 5 0 5 3.4 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085965 7272 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 5 0 5 3.4 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46882522 5714 None 0 Human Functional pKi = 6.7 6.7 - 2
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078208 5714 None 0 Human Functional pKi = 6.7 6.7 - 2
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
46190041 68917 None 0 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 6 1 7 2.3 CNc1nn2c(C)c(CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922640 68917 None 0 Human Functional pKi = 8.7 8.7 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 6 1 7 2.3 CNc1nn2c(C)c(CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44476611 82383 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCNC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172191 82383 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCNC3 10.1016/j.bmcl.2012.05.036
52918030 57665 None 4 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668569 57665 None 4 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
25110703 189829 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL515624 189829 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
9924293 68918 None 0 Human Functional pKi = 8.6 8.6 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922641 68918 None 0 Human Functional pKi = 8.6 8.6 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1021/jm201079g
54238415 91958 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 261 3 0 3 2.6 CN(C)c1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413983 91958 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 261 3 0 3 2.6 CN(C)c1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
56849581 68898 None 1 Human Functional pKi = 7.7 7.7 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922621 68898 None 1 Human Functional pKi = 7.7 7.7 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53324933 57639 None 2 Human Functional pKi = 7.6 7.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668502 57639 None 2 Human Functional pKi = 7.6 7.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
52915982 61010 None 2 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 374 6 0 7 2.1 Cc1cc(C)n2nc(OCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762575 61010 None 2 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 374 6 0 7 2.1 Cc1cc(C)n2nc(OCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
10658135 91960 None 2 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 247 3 1 3 2.6 CNc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413985 91960 None 2 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 247 3 1 3 2.6 CNc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
46891113 6626 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1083297 6626 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891111 6805 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1083909 6805 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891004 7147 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085351 7147 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890058 7251 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 479 5 1 5 3.4 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085835 7251 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 479 5 1 5 3.4 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46867524 6585 None 4 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 356 3 0 6 2.4 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N(C)C)nn2c2c1CCC2 10.1021/jm100350r
CHEMBL1083078 6585 None 4 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 356 3 0 6 2.4 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N(C)C)nn2c2c1CCC2 10.1021/jm100350r
52915869 61011 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 373 6 1 7 2.2 Cc1cc(C)n2nc(NCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762576 61011 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 373 6 1 7 2.2 Cc1cc(C)n2nc(NCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
45488165 199367 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL566218 199367 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
46867523 6584 None 4 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 0 6 2.1 CN(C)c1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083077 6584 None 4 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 0 6 2.1 CN(C)c1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
44155871 61006 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762571 61006 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
52915984 61012 None 4 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 349 3 0 6 1.9 Cc1cc(C)n2nc([S+](C)[O-])c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762577 61012 None 4 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 349 3 0 6 1.9 Cc1cc(C)n2nc([S+](C)[O-])c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
56849719 68904 None 3 Human Functional pKi = 8.5 8.5 - 0
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922627 68904 None 3 Human Functional pKi = 8.5 8.5 - 0
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53322259 57669 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668573 57669 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2010.12.055
53320926 57663 None 4 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.bmc.2010.12.055
CHEMBL1668567 57663 None 4 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.bmc.2010.12.055
53326175 57676 None 4 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668580 57676 None 4 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
53319628 57679 None 0 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668583 57679 None 0 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579180 182746 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 394 2 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478870 182746 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 394 2 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
53325519 57672 None 4 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 3 1 7 2.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668576 57672 None 4 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 3 1 7 2.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
10132329 102531 None 1 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413988 102531 None 1 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040182 102531 None 1 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
45488131 201037 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
CHEMBL578411 201037 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
46890949 6449 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082485 6449 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890056 6454 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 505 5 1 5 3.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CC4CCC(C3)N4C)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082494 6454 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 505 5 1 5 3.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CC4CCC(C3)N4C)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890946 6600 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 509 8 1 6 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCN3CCOCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1083122 6600 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 509 8 1 6 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCN3CCOCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46891176 6946 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(-c4ccccc4)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1084483 6946 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(-c4ccccc4)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891005 7148 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 457 4 0 5 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)C3=CC4CCOC4C=C3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085352 7148 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 457 4 0 5 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)C3=CC4CCOC4C=C3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891055 6515 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 419 4 0 5 2.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082766 6515 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 419 4 0 5 2.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891056 6516 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 413 4 0 4 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082767 6516 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 413 4 0 4 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891007 7150 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 478 4 0 5 3.4 Cc1cnc2c(S(=O)(=O)N3CC(C(=O)N(C)C4CCN(C)CC4)c4ccccc43)cccc2c1 10.1016/j.bmcl.2010.04.085
CHEMBL1085354 7150 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 478 4 0 5 3.4 Cc1cnc2c(S(=O)(=O)N3CC(C(=O)N(C)C4CCN(C)CC4)c4ccccc43)cccc2c1 10.1016/j.bmcl.2010.04.085
56849720 68905 None 3 Human Functional pKi = 7.5 7.5 - 0
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 6 1 7 2.0 CNc1nn2c(CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922628 68905 None 3 Human Functional pKi = 7.5 7.5 - 0
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 6 1 7 2.0 CNc1nn2c(CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
45488152 201385 None 0 Mouse Functional pKi = 7.5 7.5 - 0
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 201385 None 0 Mouse Functional pKi = 7.5 7.5 - 0
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
53318267 57673 None 1 Human Functional pKi = 7.4 7.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668577 57673 None 1 Human Functional pKi = 7.4 7.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 10.1016/j.bmc.2010.12.055
53320928 57674 None 4 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 376 4 0 7 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(N(C)C)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668578 57674 None 4 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 376 4 0 7 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(N(C)C)cc1 10.1016/j.bmc.2010.12.055
44579183 182749 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 342 2 1 3 2.5 O=S(=O)(c1ccccc1)N1CCCc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478872 182749 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 342 2 1 3 2.5 O=S(=O)(c1ccccc1)N1CCCc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
56849715 68901 None 2 Human Functional pKi = 8.4 8.4 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922624 68901 None 2 Human Functional pKi = 8.4 8.4 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849856 68908 None 5 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 4 2 7 2.2 CNc1nn2c(C)c(NC(C)=O)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922631 68908 None 5 Human Functional pKi = 8.3 8.3 - 0
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 4 2 7 2.2 CNc1nn2c(C)c(NC(C)=O)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53323600 57675 None 2 Human Functional pKi = 7.4 7.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668579 57675 None 2 Human Functional pKi = 7.4 7.4 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
68014784 91961 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 324 4 1 4 3.6 CNc1cc(-c2cccnc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413986 91961 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 324 4 1 4 3.6 CNc1cc(-c2cccnc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
52915980 61007 None 2 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 6 0 7 2.2 Cc1cc(C)n2nc(N(C)CCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762572 61007 None 2 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 6 0 7 2.2 Cc1cc(C)n2nc(N(C)CCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
77956 73044 None 47 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 233 2 1 3 2.1 Nc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2009408 73044 None 47 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 233 2 1 3 2.1 Nc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44476801 82381 None 3 Human Functional pKi = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172189 82381 None 3 Human Functional pKi = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
45488152 201385 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 201385 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
45488152 201385 None 0 Mouse Functional pKi = 8.3 8.3 - 0
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 201385 None 0 Mouse Functional pKi = 8.3 8.3 - 0
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
46890948 6448 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 4 0 4 4.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4c(Cl)cccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082484 6448 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 4 0 4 4.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4c(Cl)cccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891006 7149 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 6 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4c(c3)OCCO4)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085353 7149 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 6 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4c(c3)OCCO4)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890059 7252 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 555 7 1 5 4.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(Cc4ccccc4)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085836 7252 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 555 7 1 5 4.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(Cc4ccccc4)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
3232 3509 None 17 Mouse Functional pKi = 7.3 7.3 - 1
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3509 None 17 Mouse Functional pKi = 7.3 7.3 - 1
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3509 None 17 Mouse Functional pKi = 7.3 7.3 - 1
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
1472656 34637 None 21 Human Functional pKi = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1429795 34637 None 21 Human Functional pKi = 6.3 6.3 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
460659 51421 None 3 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 263 2 3 5 1.3 Nc1ccc(S(=O)(=O)c2ccc(N)c(N)c2)cc1 10.1016/j.bmc.2013.05.040
CHEMBL1581846 51421 None 3 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 263 2 3 5 1.3 Nc1ccc(S(=O)(=O)c2ccc(N)c(N)c2)cc1 10.1016/j.bmc.2013.05.040
46882520 5858 None 0 Human Functional pKi = 8.2 8.2 - 2
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
CHEMBL1079311 5858 None 0 Human Functional pKi = 8.2 8.2 - 2
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
44155876 57670 None 2 Human Functional pKi = 8.2 8.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668574 57670 None 2 Human Functional pKi = 8.2 8.2 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
46891054 6514 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 517 4 0 5 4.7 Cc1c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082765 6514 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 517 4 0 5 4.7 Cc1c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.04.085
46890106 6981 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 557 6 0 6 4.5 COc1cccc(N2CCN(C(=O)C3CN(S(=O)(=O)c4ccc(OC)c5ccccc45)c4ccccc43)CC2)c1 10.1016/j.bmcl.2010.04.085
CHEMBL1084614 6981 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 557 6 0 6 4.5 COc1cccc(N2CCN(C(=O)C3CN(S(=O)(=O)c4ccc(OC)c5ccccc45)c4ccccc43)CC2)c1 10.1016/j.bmcl.2010.04.085
45102708 5772 None 0 Human Functional pKi = 6.2 6.2 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 468 6 2 7 2.0 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(N2CCOCC2)nc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078595 5772 None 0 Human Functional pKi = 6.2 6.2 - 1
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 468 6 2 7 2.0 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(N2CCOCC2)nc1 10.1016/j.bmcl.2009.09.027
56849580 68897 None 4 Human Functional pKi = 7.2 7.2 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922620 68897 None 4 Human Functional pKi = 7.2 7.2 - 1
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
52918031 57683 None 4 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668587 57683 None 4 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579130 181729 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL477385 181729 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579129 182243 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478223 182243 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579133 190347 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 332 2 1 5 2.6 O=S(=O)(c1ccsc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL517503 190347 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 332 2 1 5 2.6 O=S(=O)(c1ccsc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
46890057 6529 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 493 5 0 5 3.7 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082818 6529 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 493 5 0 5 3.7 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890105 7199 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 4 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085608 7199 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 4 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
53319627 57677 None 1 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668581 57677 None 1 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
9822810 69524 None 0 Human Functional pKi = 8.1 8.1 - 0
Binding affinity against 5-hydroxytryptamine 6 receptor of human caudateBinding affinity against 5-hydroxytryptamine 6 receptor of human caudate
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193400 69524 None 0 Human Functional pKi = 8.1 8.1 - 0
Binding affinity against 5-hydroxytryptamine 6 receptor of human caudateBinding affinity against 5-hydroxytryptamine 6 receptor of human caudate
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
52915979 61008 None 4 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 7 1 7 2.5 Cc1cc(C)n2nc(NCCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762573 61008 None 4 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 7 1 7 2.5 Cc1cc(C)n2nc(NCCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
46890947 6447 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 490 8 1 6 3.5 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCn3ccnc3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082483 6447 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 490 8 1 6 3.5 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCn3ccnc3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890887 6905 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 495 10 1 5 4.0 CCN(CC)CCCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
CHEMBL1084317 6905 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 495 10 1 5 4.0 CCN(CC)CCCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
46890104 7152 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 5 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(CN)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085362 7152 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 5 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(CN)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
9925009 102532 None 2 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413991 102532 None 2 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040183 102532 None 2 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
640912 91959 None 5 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 3 0 3 2.5 COc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413984 91959 None 5 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 3 0 3 2.5 COc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
46867654 6657 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 397 3 1 7 1.8 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCC2 10.1021/jm100350r
CHEMBL1083388 6657 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 397 3 1 7 1.8 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCC2 10.1021/jm100350r
52915868 61005 None 5 Human Functional pKi = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762570 61005 None 5 Human Functional pKi = 7.1 7.1 - 1
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
53319629 57691 None 4 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 4 1 7 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668595 57691 None 4 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 4 1 7 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 10.1016/j.bmc.2010.12.055
4223 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314.0 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
10131112 1552 None 18 Human Functional pIC50 = 8.1 8.1 28 7
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331
8428 1552 None 18 Human Functional pIC50 = 8.1 8.1 28 7
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331
CHEMBL364005 1552 None 18 Human Functional pIC50 = 8.1 8.1 28 7
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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2585 803 None 59 Human Binding pAC50 = 5.9 5.9 -131 22
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2585.0 803 None 59 Human Binding pAC50 = 5.9 5.9 -131 22
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 803 None 59 Human Binding pAC50 = 5.9 5.9 -131 22
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 803 None 59 Human Binding pAC50 = 5.9 5.9 -131 22
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 803 None 59 Human Binding pAC50 = 5.9 5.9 -131 22
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 803 None 59 Human Binding pAC50 = 5.9 5.9 -131 22
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2726 919 None 48 Human Binding pAC50 = 7.9 7.9 -10 72
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2726.0 919 None 48 Human Binding pAC50 = 7.9 7.9 -10 72
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 None 48 Human Binding pAC50 = 7.9 7.9 -10 72
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 None 48 Human Binding pAC50 = 7.9 7.9 -10 72
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 None 48 Human Binding pAC50 = 7.9 7.9 -10 72
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 None 48 Human Binding pAC50 = 7.9 7.9 -10 72
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
135398745 2914 None 65 Human Binding pAC50 = 7.8 7.8 -4 65
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
135398745.0 2914 None 65 Human Binding pAC50 = 7.8 7.8 -4 65
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 None 65 Human Binding pAC50 = 7.8 7.8 -4 65
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 None 65 Human Binding pAC50 = 7.8 7.8 -4 65
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 None 65 Human Binding pAC50 = 7.8 7.8 -4 65
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
1209 1658 None 52 Human Binding pAC50 = 5.8 5.8 -12 31
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1658 None 52 Human Binding pAC50 = 5.8 5.8 -12 31
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1658 None 52 Human Binding pAC50 = 5.8 5.8 -12 31
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1658 None 52 Human Binding pAC50 = 5.8 5.8 -12 31
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1658 None 52 Human Binding pAC50 = 5.8 5.8 -12 31
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
135398737 958 None 57 Human Binding pAC50 = 7.8 7.8 -4 91
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 57 Human Binding pAC50 = 7.8 7.8 -4 91
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 57 Human Binding pAC50 = 7.8 7.8 -4 91
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 57 Human Binding pAC50 = 7.8 7.8 -4 91
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 57 Human Binding pAC50 = 7.8 7.8 -4 91
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 57 Human Binding pAC50 = 7.8 7.8 -4 91
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135409453 3773 None 26 Human Binding pAC50 = 6.7 6.7 -72 19
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 None 26 Human Binding pAC50 = 6.7 6.7 -72 19
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 None 26 Human Binding pAC50 = 6.7 6.7 -72 19
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
2162 41527 None 58 Human Binding pAC50 = 5.7 5.7 -2 6
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41527 None 58 Human Binding pAC50 = 5.7 5.7 -2 6
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Binding pAC50 = 6.7 6.7 -851 20
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Binding pAC50 = 6.7 6.7 -851 20
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Binding pAC50 = 6.7 6.7 -851 20
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Binding pAC50 = 6.7 6.7 -851 20
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
1400 1957 None 46 Human Binding pAC50 = 5.7 5.7 - 3
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1957 None 46 Human Binding pAC50 = 5.7 5.7 - 3
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658.0 1957 None 46 Human Binding pAC50 = 5.7 5.7 - 3
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1957 None 46 Human Binding pAC50 = 5.7 5.7 - 3
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1957 None 46 Human Binding pAC50 = 5.7 5.7 - 3
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1957 None 46 Human Binding pAC50 = 5.7 5.7 - 3
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1957 None 46 Human Binding pAC50 = 5.7 5.7 - 3
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
191 403 None 60 Human Binding pAC50 = 7.6 7.6 -20 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 None 60 Human Binding pAC50 = 7.6 7.6 -20 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 None 60 Human Binding pAC50 = 7.6 7.6 -20 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170.0 403 None 60 Human Binding pAC50 = 7.6 7.6 -20 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 None 60 Human Binding pAC50 = 7.6 7.6 -20 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 None 60 Human Binding pAC50 = 7.6 7.6 -20 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
5329102 194838 None 50 Human Binding pAC50 = 5.6 5.6 - 0
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194838 None 50 Human Binding pAC50 = 5.6 5.6 - 0
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
2284 3182 None 26 Human Binding pAC50 = 6.6 6.6 -12 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 None 26 Human Binding pAC50 = 6.6 6.6 -12 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 None 26 Human Binding pAC50 = 6.6 6.6 -12 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 None 26 Human Binding pAC50 = 6.6 6.6 -12 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 None 26 Human Binding pAC50 = 6.6 6.6 -12 28
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
6918638 158079 None 53 Human Binding pAC50 = 5.6 5.6 - 0
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 5 3 4 2.0 O=C(/C=C/c1cccc(S(=O)(=O)Nc2ccccc2)c1)NO 10.1038/s41467-023-40064-9
CHEMBL408513 158079 None 53 Human Binding pAC50 = 5.6 5.6 - 0
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 5 3 4 2.0 O=C(/C=C/c1cccc(S(=O)(=O)Nc2ccccc2)c1)NO 10.1038/s41467-023-40064-9
1971 2866 None 32 Human Binding pAC50 = 6.6 6.6 -10 29
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 None 32 Human Binding pAC50 = 6.6 6.6 -10 29
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 None 32 Human Binding pAC50 = 6.6 6.6 -10 29
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543.0 2866 None 32 Human Binding pAC50 = 6.6 6.6 -10 29
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 None 32 Human Binding pAC50 = 6.6 6.6 -10 29
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 None 32 Human Binding pAC50 = 6.6 6.6 -10 29
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
3294 2006 None 61 Human Binding pAC50 = 6.6 6.6 -87 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 2006 None 61 Human Binding pAC50 = 6.6 6.6 -87 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360.0 2006 None 61 Human Binding pAC50 = 6.6 6.6 -87 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 2006 None 61 Human Binding pAC50 = 6.6 6.6 -87 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 2006 None 61 Human Binding pAC50 = 6.6 6.6 -87 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 2006 None 61 Human Binding pAC50 = 6.6 6.6 -87 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
2247 505 None 55 Human Binding pAC50 = 5.5 5.5 -53 41
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 55 Human Binding pAC50 = 5.5 5.5 -53 41
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 55 Human Binding pAC50 = 5.5 5.5 -53 41
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 55 Human Binding pAC50 = 5.5 5.5 -53 41
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 55 Human Binding pAC50 = 5.5 5.5 -53 41
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
1427 2013 None 42 Human Binding pAC50 = 6.5 6.5 - 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 None 42 Human Binding pAC50 = 6.5 6.5 - 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 None 42 Human Binding pAC50 = 6.5 6.5 - 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 None 42 Human Binding pAC50 = 6.5 6.5 - 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 None 42 Human Binding pAC50 = 6.5 6.5 - 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
21722 17999 None 26 Human Binding pAC50 = 5.5 5.5 - 5
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17999 None 26 Human Binding pAC50 = 5.5 5.5 - 5
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
212 3806 None 35 Human Binding pAC50 = 6.3 6.3 -6 25
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3806 None 35 Human Binding pAC50 = 6.3 6.3 -6 25
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3806 None 35 Human Binding pAC50 = 6.3 6.3 -6 25
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651.0 3806 None 35 Human Binding pAC50 = 6.3 6.3 -6 25
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3806 None 35 Human Binding pAC50 = 6.3 6.3 -6 25
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3806 None 35 Human Binding pAC50 = 6.3 6.3 -6 25
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
1224 1432 None 51 Human Binding pAC50 = 5.3 5.3 - 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1432 None 51 Human Binding pAC50 = 5.3 5.3 - 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100.0 1432 None 51 Human Binding pAC50 = 5.3 5.3 - 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1432 None 51 Human Binding pAC50 = 5.3 5.3 - 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1432 None 51 Human Binding pAC50 = 5.3 5.3 - 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1432 None 51 Human Binding pAC50 = 5.3 5.3 - 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1432 None 51 Human Binding pAC50 = 5.3 5.3 - 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
2337 3256 None 51 Human Binding pAC50 = 5.3 5.3 -54 62
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 None 51 Human Binding pAC50 = 5.3 5.3 -54 62
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 None 51 Human Binding pAC50 = 5.3 5.3 -54 62
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002.0 3256 None 51 Human Binding pAC50 = 5.3 5.3 -54 62
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 None 51 Human Binding pAC50 = 5.3 5.3 -54 62
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 None 51 Human Binding pAC50 = 5.3 5.3 -54 62
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
1613 2348 None 42 Human Binding pAC50 = 7.2 7.2 -4 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 None 42 Human Binding pAC50 = 7.2 7.2 -4 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 None 42 Human Binding pAC50 = 7.2 7.2 -4 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964.0 2348 None 42 Human Binding pAC50 = 7.2 7.2 -4 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 None 42 Human Binding pAC50 = 7.2 7.2 -4 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 None 42 Human Binding pAC50 = 7.2 7.2 -4 44
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2389 3331 None 72 Human Binding pAC50 = 5.2 5.2 -2511 67
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3331 None 72 Human Binding pAC50 = 5.2 5.2 -2511 67
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073.0 3331 None 72 Human Binding pAC50 = 5.2 5.2 -2511 67
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3331 None 72 Human Binding pAC50 = 5.2 5.2 -2511 67
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3331 None 72 Human Binding pAC50 = 5.2 5.2 -2511 67
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3331 None 72 Human Binding pAC50 = 5.2 5.2 -2511 67
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
135 2532 None 33 Human Binding pAC50 = 7.2 7.2 -21 57
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 None 33 Human Binding pAC50 = 7.2 7.2 -21 57
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 None 33 Human Binding pAC50 = 7.2 7.2 -21 57
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184.0 2532 None 33 Human Binding pAC50 = 7.2 7.2 -21 57
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 None 33 Human Binding pAC50 = 7.2 7.2 -21 57
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 None 33 Human Binding pAC50 = 7.2 7.2 -21 57
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
102 4127 None 36 Human Binding pAC50 = 6.2 6.2 -1737 50
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 4127 None 36 Human Binding pAC50 = 6.2 6.2 -1737 50
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 4127 None 36 Human Binding pAC50 = 6.2 6.2 -1737 50
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969.0 4127 None 36 Human Binding pAC50 = 6.2 6.2 -1737 50
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 4127 None 36 Human Binding pAC50 = 6.2 6.2 -1737 50
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 4127 None 36 Human Binding pAC50 = 6.2 6.2 -1737 50
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
2600 3779 None 53 Human Binding pAC50 = 5.1 5.1 -5 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 None 53 Human Binding pAC50 = 5.1 5.1 -5 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 None 53 Human Binding pAC50 = 5.1 5.1 -5 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 None 53 Human Binding pAC50 = 5.1 5.1 -5 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 None 53 Human Binding pAC50 = 5.1 5.1 -5 13
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
1890 2759 None 31 Human Binding pAC50 = 6.1 6.1 -141 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2759 None 31 Human Binding pAC50 = 6.1 6.1 -141 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2759 None 31 Human Binding pAC50 = 6.1 6.1 -141 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2759 None 31 Human Binding pAC50 = 6.1 6.1 -141 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2759 None 31 Human Binding pAC50 = 6.1 6.1 -141 26
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
9921064 127245 None 23 Human Binding pEC50 = 7.4 7.4 - 3
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
CHEMBL365751 127245 None 23 Human Binding pEC50 = 7.4 7.4 - 3
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
10337743 4076 None 15 Human Binding pEC50 = 8.1 8.1 - 1
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
8429 4076 None 15 Human Binding pEC50 = 8.1 8.1 - 1
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
CHEMBL571858 4076 None 15 Human Binding pEC50 = 8.1 8.1 - 1
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
91971999 138918 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 517 7 1 5 3.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781299 138918 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 517 7 1 5 3.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
46189984 68912 None 1 Human Binding pIC50 = 9.6 9.6 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1922635 68912 None 1 Human Binding pIC50 = 9.6 9.6 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
118465011 138920 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781323 138920 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
56655504 68891 None 3 Human Binding pIC50 = 9.5 9.5 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922614 68891 None 3 Human Binding pIC50 = 9.5 9.5 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465045 138855 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 545 7 1 5 4.6 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780579 138855 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 545 7 1 5 4.6 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
52918031 57683 None 4 Human Binding pIC50 = 9.5 9.5 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668587 57683 None 4 Human Binding pIC50 = 9.5 9.5 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465023 138926 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781452 138926 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
118464996 138804 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3779904 138804 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
46189935 68910 None 3 Human Binding pIC50 = 9.3 9.3 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922633 68910 None 3 Human Binding pIC50 = 9.3 9.3 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189980 68916 None 3 Human Binding pIC50 = 9.2 9.2 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922639 68916 None 3 Human Binding pIC50 = 9.2 9.2 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189932 68907 None 4 Human Binding pIC50 = 9.2 9.2 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922630 68907 None 4 Human Binding pIC50 = 9.2 9.2 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465171 138832 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780274 138832 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
10383682 120453 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition against human 5-hydroxytryptamine 6 receptorInhibition against human 5-hydroxytryptamine 6 receptor
ChEMBL 356 5 1 1 5.1 CN(C)CCCc1c(-c2cccc(Br)c2)[nH]c2ccccc12 10.1021/jm0309452
CHEMBL353389 120453 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition against human 5-hydroxytryptamine 6 receptorInhibition against human 5-hydroxytryptamine 6 receptor
ChEMBL 356 5 1 1 5.1 CN(C)CCCc1c(-c2cccc(Br)c2)[nH]c2ccccc12 10.1021/jm0309452
53326176 57682 None 4 Human Binding pIC50 = 9.1 9.1 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668586 57682 None 4 Human Binding pIC50 = 9.1 9.1 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
44476436 82379 None 8 Human Binding pIC50 = 9.1 9.1 - 1
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172186 82379 None 8 Human Binding pIC50 = 9.1 9.1 - 1
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
53326177 57684 None 4 Human Binding pIC50 = 9.1 9.1 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668588 57684 None 4 Human Binding pIC50 = 9.1 9.1 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
118464995 138905 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 439 7 1 5 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781179 138905 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 439 7 1 5 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
44155109 8176 None 4 Human Binding pIC50 = 9.0 9.0 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091919 8176 None 4 Human Binding pIC50 = 9.0 9.0 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44156863 8080 None 0 Human Binding pIC50 = 9.0 9.0 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
CHEMBL1091206 8080 None 0 Human Binding pIC50 = 9.0 9.0 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
118464998 138954 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3781801 138954 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
118465054 138915 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 8 2 6 3.5 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3781263 138915 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 8 2 6 3.5 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
44155107 8081 None 4 Human Binding pIC50 = 8.9 8.9 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091207 8081 None 4 Human Binding pIC50 = 8.9 8.9 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
118465064 138810 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 529 7 2 5 4.0 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(Br)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3779974 138810 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 529 7 2 5 4.0 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(Br)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
68303363 129828 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 430 7 1 8 3.1 CCOC(=O)Cc1c(C)nc2c(S(=O)(=O)c3ccccc3)c(NC(C)C)nn2c1C nan
CHEMBL3675189 129828 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 430 7 1 8 3.1 CCOC(=O)Cc1c(C)nc2c(S(=O)(=O)c3ccccc3)c(NC(C)C)nn2c1C nan
118465035 138818 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 453 7 2 5 3.5 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780141 138818 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 453 7 2 5 3.5 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
118464997 138911 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781239 138911 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
10427672 105050 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2ccc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113554 105050 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2ccc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
118465048 138812 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 497 8 1 6 3.9 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3780011 138812 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 497 8 1 6 3.9 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
70245924 82385 None 0 Human Binding pIC50 = 8.9 8.9 - 1
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172193 82385 None 0 Human Binding pIC50 = 8.9 8.9 - 1
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
46830134 8219 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1092241 8219 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44476514 82380 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172187 82380 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
118465025 138924 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781399 138924 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
196129 67820 None 12 Human Binding pIC50 = 8.8 8.8 1 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67820 None 12 Human Binding pIC50 = 8.8 8.8 1 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
118465050 138882 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 531 7 2 5 4.3 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780861 138882 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 531 7 2 5 4.3 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
15619875 69482 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 1 1 1 3.8 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(C)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL193351 69482 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 1 1 1 3.8 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(C)CC1 10.1016/j.bmcl.2005.06.067
73354882 89727 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376482 89727 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73347307 89732 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376487 89732 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
5 139 None 45 Human Binding pIC50 = 7 7.0 -169 54
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 None 45 Human Binding pIC50 = 7 7.0 -169 54
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 None 45 Human Binding pIC50 = 7 7.0 -169 54
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 None 45 Human Binding pIC50 = 7 7.0 -169 54
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
44403367 71099 None 1 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.3 CC(C)c1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL195239 71099 None 1 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.3 CC(C)c1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
73351904 89734 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 270 3 2 2 3.6 Cc1[nH]c2ccc(OC(C)C)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376489 89734 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 270 3 2 2 3.6 Cc1[nH]c2ccc(OC(C)C)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73353367 89738 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 274 2 1 2 4.0 CCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
CHEMBL2376493 89738 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 274 2 1 2 4.0 CCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
73351905 89736 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376491 89736 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
141 1427 None 18 Human Binding pIC50 = 6.0 6.0 -3 28
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pIC50 = 6.0 6.0 -3 28
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pIC50 = 6.0 6.0 -3 28
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pIC50 = 6.0 6.0 -3 28
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
4189 209380 None 58 Human Binding pIC50 = 5.0 5.0 -31 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 209380 None 58 Human Binding pIC50 = 5.0 5.0 -31 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 209380 None 58 Human Binding pIC50 = 5.0 5.0 -31 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
3198 207971 None 50 Human Binding pIC50 = 5.0 5.0 -32 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 207971 None 50 Human Binding pIC50 = 5.0 5.0 -32 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 207971 None 50 Human Binding pIC50 = 5.0 5.0 -32 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
135398737 958 None 57 Human Binding pIC50 = 8.0 8.0 -4 91
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
135398737.0 958 None 57 Human Binding pIC50 = 8.0 8.0 -4 91
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 None 57 Human Binding pIC50 = 8.0 8.0 -4 91
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 None 57 Human Binding pIC50 = 8.0 8.0 -4 91
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 None 57 Human Binding pIC50 = 8.0 8.0 -4 91
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 None 57 Human Binding pIC50 = 8.0 8.0 -4 91
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
118465024 138914 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781260 138914 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
118465038 138960 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 471 7 2 5 3.7 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781948 138960 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 471 7 2 5 3.7 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
53322638 56691 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)C(C)CC2=O 10.1016/j.bmcl.2010.12.007
CHEMBL1642128 56691 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)C(C)CC2=O 10.1016/j.bmcl.2010.12.007
10451504 105013 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmc.2014.01.003
CHEMBL3113350 105013 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmc.2014.01.003
20901117 10680 None 2 Human Binding pIC50 = 7.9 7.9 - 1
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170672 10680 None 2 Human Binding pIC50 = 7.9 7.9 - 1
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
6761 67821 None 11 Human Binding pIC50 = 7.0 7.0 -9 18
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67821 None 11 Human Binding pIC50 = 7.0 7.0 -9 18
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
44155876 57670 None 2 Human Binding pIC50 = 7.0 7.0 - 1
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668574 57670 None 2 Human Binding pIC50 = 7.0 7.0 - 1
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
4601 209205 None 27 Human Binding pIC50 = 6.0 6.0 -2 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
4601.0 209205 None 27 Human Binding pIC50 = 6.0 6.0 -2 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 209205 None 27 Human Binding pIC50 = 6.0 6.0 -2 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 209205 None 27 Human Binding pIC50 = 6.0 6.0 -2 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
DB01173 209205 None 27 Human Binding pIC50 = 6.0 6.0 -2 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
1530 2182 None 36 Human Binding pIC50 = 5.9 5.9 -144 24
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 None 36 Human Binding pIC50 = 5.9 5.9 -144 24
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827.0 2182 None 36 Human Binding pIC50 = 5.9 5.9 -144 24
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 None 36 Human Binding pIC50 = 5.9 5.9 -144 24
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 None 36 Human Binding pIC50 = 5.9 5.9 -144 24
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 None 36 Human Binding pIC50 = 5.9 5.9 -144 24
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
49864601 15670 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 4 0 2 5.0 CC(C)N(c1cccc(I)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222137 15670 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 4 0 2 5.0 CC(C)N(c1cccc(I)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
1588 2325 None 21 Human Binding pIC50 = 7.9 7.9 -21 43
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2325 None 21 Human Binding pIC50 = 7.9 7.9 -21 43
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864.0 2325 None 21 Human Binding pIC50 = 7.9 7.9 -21 43
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2325 None 21 Human Binding pIC50 = 7.9 7.9 -21 43
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2325 None 21 Human Binding pIC50 = 7.9 7.9 -21 43
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2325 None 21 Human Binding pIC50 = 7.9 7.9 -21 43
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
11724112 105023 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 329 4 1 6 2.0 CCOc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113360 105023 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 329 4 1 6 2.0 CCOc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
9979748 105057 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(C)cc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113561 105057 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(C)cc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
10472756 105018 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 0 6 2.4 C/N=c1/c(S(=O)(=O)c2ccccc2)c(SC)nc2ccccn12 10.1016/j.bmc.2014.01.003
CHEMBL3113355 105018 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 0 6 2.4 C/N=c1/c(S(=O)(=O)c2ccccc2)c(SC)nc2ccccn12 10.1016/j.bmc.2014.01.003
5 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5202 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
CHEMBL39 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
DB08839 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5202 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
CHEMBL39 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
DB08839 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
141 1427 None 18 Human Binding pIC50 = 5.9 5.9 -3 28
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pIC50 = 5.9 5.9 -3 28
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pIC50 = 5.9 5.9 -3 28
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pIC50 = 5.9 5.9 -3 28
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
2812 4781 None 63 Human Binding pIC50 = 4.9 4.9 -36 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4781 None 63 Human Binding pIC50 = 4.9 4.9 -36 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
11743064 35962 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL144265 35962 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
448537 160344 None 54 Human Binding pIC50 = 4.9 4.9 -35 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160344 None 54 Human Binding pIC50 = 4.9 4.9 -35 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
53319229 56587 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 3 0 5 2.5 Cc1ccc(S(=O)(=O)N2CCC(=O)c3c(N4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2010.12.007
CHEMBL1641610 56587 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 3 0 5 2.5 Cc1ccc(S(=O)(=O)N2CCC(=O)c3c(N4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2010.12.007
44476704 82375 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172182 82375 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
135398745 2914 None 65 Human Binding pIC50 = 7.9 7.9 -4 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
135398745.0 2914 None 65 Human Binding pIC50 = 7.9 7.9 -4 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 None 65 Human Binding pIC50 = 7.9 7.9 -4 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 None 65 Human Binding pIC50 = 7.9 7.9 -4 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 None 65 Human Binding pIC50 = 7.9 7.9 -4 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
18180076 15609 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221497 15609 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
5 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 None 45 Human Binding pIC50 = 6.9 6.9 -169 54
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
2600 3779 None 53 Human Binding pIC50 = 5.9 5.9 -5 13
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3779 None 53 Human Binding pIC50 = 5.9 5.9 -5 13
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3779 None 53 Human Binding pIC50 = 5.9 5.9 -5 13
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3779 None 53 Human Binding pIC50 = 5.9 5.9 -5 13
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3779 None 53 Human Binding pIC50 = 5.9 5.9 -5 13
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5323 205246 None 67 Human Binding pIC50 = 5.9 5.9 - 1
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
CHEMBL62193 205246 None 67 Human Binding pIC50 = 5.9 5.9 - 1
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
11236269 129373 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
CHEMBL367088 129373 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
11113605 10510 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 10510 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
54576142 66516 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852341 66516 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216098 66516 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
180 401 None 38 Human Binding pIC50 = 6.9 6.9 -99 39
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 None 38 Human Binding pIC50 = 6.9 6.9 -99 39
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 None 38 Human Binding pIC50 = 6.9 6.9 -99 39
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160.0 401 None 38 Human Binding pIC50 = 6.9 6.9 -99 39
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 None 38 Human Binding pIC50 = 6.9 6.9 -99 39
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 None 38 Human Binding pIC50 = 6.9 6.9 -99 39
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
156018181 177912 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 430 5 1 6 4.0 CC(C)c1ccc(S(=O)(=O)Nc2ccc3nc(N4CCN(C)CC4)sc3c2)cc1 10.1016/j.ejmech.2018.11.017
CHEMBL4643549 177912 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 430 5 1 6 4.0 CC(C)c1ccc(S(=O)(=O)Nc2ccc3nc(N4CCN(C)CC4)sc3c2)cc1 10.1016/j.ejmech.2018.11.017
4211 57839 None 58 Human Binding pIC50 = 5.9 5.9 1 4
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57839 None 58 Human Binding pIC50 = 5.9 5.9 1 4
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
45109862 7436 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
CHEMBL1086626 7436 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
52915868 61005 None 5 Human Binding pIC50 = 6.8 6.8 - 1
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762570 61005 None 5 Human Binding pIC50 = 6.8 6.8 - 1
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
73453 29624 None 14 Human Binding pIC50 = 7.8 7.8 -10 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29624 None 14 Human Binding pIC50 = 7.8 7.8 -10 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
53318694 56690 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1ccc2c(c1N1CCN(C)CC1)C(=O)CC(C)N2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642127 56690 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1ccc2c(c1N1CCN(C)CC1)C(=O)CC(C)N2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
68262106 129829 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 401 5 1 7 1.9 CNc1nn2c(C)c(CC(=O)N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675190 129829 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 401 5 1 7 1.9 CNc1nn2c(C)c(CC(=O)N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
2585 803 None 59 Human Binding pIC50 = 5.8 5.8 -131 22
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
2585.0 803 None 59 Human Binding pIC50 = 5.8 5.8 -131 22
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 803 None 59 Human Binding pIC50 = 5.8 5.8 -131 22
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 803 None 59 Human Binding pIC50 = 5.8 5.8 -131 22
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 803 None 59 Human Binding pIC50 = 5.8 5.8 -131 22
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 803 None 59 Human Binding pIC50 = 5.8 5.8 -131 22
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
1548953 210138 None 21 Human Binding pIC50 = 5.8 5.8 -3 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 210138 None 21 Human Binding pIC50 = 5.8 5.8 -3 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
11071079 110656 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 110656 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
134551 358 None 18 Human Binding pIC50 = 7.8 7.8 -6 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 358 None 18 Human Binding pIC50 = 7.8 7.8 -6 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 358 None 18 Human Binding pIC50 = 7.8 7.8 -6 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 358 None 18 Human Binding pIC50 = 7.8 7.8 -6 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
118465034 138831 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780270 138831 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
46866711 15677 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2010.06.150
CHEMBL1222234 15677 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2010.06.150
169713 80192 None 12 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
CHEMBL21343 80192 None 12 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
6918647 100800 None 0 Human Binding pIC50 = 7.8 7.8 50 14
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
CHEMBL292759 100800 None 0 Human Binding pIC50 = 7.8 7.8 50 14
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
58149663 127489 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659969 127489 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
3117 210300 None 60 Human Binding pIC50 = 4.8 4.8 -5 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 210300 None 60 Human Binding pIC50 = 4.8 4.8 -5 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
134 2514 None 19 Human Binding pIC50 = 6.8 6.8 -63 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2514 None 19 Human Binding pIC50 = 6.8 6.8 -63 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2514 None 19 Human Binding pIC50 = 6.8 6.8 -63 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681.0 2514 None 19 Human Binding pIC50 = 6.8 6.8 -63 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2514 None 19 Human Binding pIC50 = 6.8 6.8 -63 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2514 None 19 Human Binding pIC50 = 6.8 6.8 -63 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
53321318 56684 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 6 3.4 COc1cc2c(cc1N1CCN(C)CC1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
CHEMBL1642121 56684 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 6 3.4 COc1cc2c(cc1N1CCN(C)CC1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
1209 1658 None 52 Human Binding pIC50 = 5.8 5.8 -12 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1658 None 52 Human Binding pIC50 = 5.8 5.8 -12 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1658 None 52 Human Binding pIC50 = 5.8 5.8 -12 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1658 None 52 Human Binding pIC50 = 5.8 5.8 -12 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1658 None 52 Human Binding pIC50 = 5.8 5.8 -12 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
124 2981 None 32 Human Binding pIC50 = 5.8 5.8 -100 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2981 None 32 Human Binding pIC50 = 5.8 5.8 -100 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2981 None 32 Human Binding pIC50 = 5.8 5.8 -100 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636.0 2981 None 32 Human Binding pIC50 = 5.8 5.8 -100 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2981 None 32 Human Binding pIC50 = 5.8 5.8 -100 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2981 None 32 Human Binding pIC50 = 5.8 5.8 -100 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
54577891 66596 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852516 66596 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216758 66596 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
102 4127 None 36 Human Binding pIC50 = 5.8 5.8 -1737 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4127 None 36 Human Binding pIC50 = 5.8 5.8 -1737 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4127 None 36 Human Binding pIC50 = 5.8 5.8 -1737 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969.0 4127 None 36 Human Binding pIC50 = 5.8 5.8 -1737 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4127 None 36 Human Binding pIC50 = 5.8 5.8 -1737 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4127 None 36 Human Binding pIC50 = 5.8 5.8 -1737 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
53323972 56683 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642120 56683 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
135398737 958 None 57 Human Binding pIC50 = 7.8 7.8 -4 91
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
135398737.0 958 None 57 Human Binding pIC50 = 7.8 7.8 -4 91
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
38 958 None 57 Human Binding pIC50 = 7.8 7.8 -4 91
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
722 958 None 57 Human Binding pIC50 = 7.8 7.8 -4 91
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
CHEMBL42 958 None 57 Human Binding pIC50 = 7.8 7.8 -4 91
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
DB00363 958 None 57 Human Binding pIC50 = 7.8 7.8 -4 91
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
46884709 8082 None 4 Human Binding pIC50 = 7.8 7.8 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091208 8082 None 4 Human Binding pIC50 = 7.8 7.8 - 1
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
20901115 10968 None 5 Human Binding pIC50 = 7.8 7.8 - 1
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173359 10968 None 5 Human Binding pIC50 = 7.8 7.8 - 1
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
126720440 163121 None 0 Human Binding pIC50 = 7.8 7.8 72 5
Partial inverse agonist activity at 5HT6R (unknown origin)Partial inverse agonist activity at 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4175829 163121 None 0 Human Binding pIC50 = 7.8 7.8 72 5
Partial inverse agonist activity at 5HT6R (unknown origin)Partial inverse agonist activity at 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
71695200 129830 None 5 Human Binding pIC50 = 6.8 6.8 - 0
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675191 129830 None 5 Human Binding pIC50 = 6.8 6.8 - 0
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
3397 207946 None 70 Human Binding pIC50 = 4.8 4.8 -37 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
CHEMBL806 207946 None 70 Human Binding pIC50 = 4.8 4.8 -37 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
53323601 57689 None 4 Human Binding pIC50 = 7.8 7.8 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668593 57689 None 4 Human Binding pIC50 = 7.8 7.8 - 1
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
11741686 105014 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 399 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2014.01.003
CHEMBL3113351 105014 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 399 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2014.01.003
5 139 None 45 Human Binding pIC50 = 6.8 6.8 -169 54
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
5202 139 None 45 Human Binding pIC50 = 6.8 6.8 -169 54
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
CHEMBL39 139 None 45 Human Binding pIC50 = 6.8 6.8 -169 54
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
DB08839 139 None 45 Human Binding pIC50 = 6.8 6.8 -169 54
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
25070582 61474 None 27 Human Binding pIC50 = 5.8 5.8 - 1
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61474 None 27 Human Binding pIC50 = 5.8 5.8 - 1
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
6075 150196 None 34 Human Binding pIC50 = 5.7 5.7 -13 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150196 None 34 Human Binding pIC50 = 5.7 5.7 -13 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
2291 3184 None 43 Human Binding pIC50 = 5.7 5.7 -12 12
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3184 None 43 Human Binding pIC50 = 5.7 5.7 -12 12
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3184 None 43 Human Binding pIC50 = 5.7 5.7 -12 12
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932.0 3184 None 43 Human Binding pIC50 = 5.7 5.7 -12 12
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3184 None 43 Human Binding pIC50 = 5.7 5.7 -12 12
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3184 None 43 Human Binding pIC50 = 5.7 5.7 -12 12
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
7185124 10957 None 1 Human Binding pIC50 = 6.7 6.7 - 1
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173210 10957 None 1 Human Binding pIC50 = 6.7 6.7 - 1
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
45278882 7454 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086756 7454 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
176 398 None 47 Human Binding pIC50 = 4.7 4.7 -5 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 47 Human Binding pIC50 = 4.7 4.7 -5 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157.0 398 None 47 Human Binding pIC50 = 4.7 4.7 -5 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 47 Human Binding pIC50 = 4.7 4.7 -5 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 47 Human Binding pIC50 = 4.7 4.7 -5 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 47 Human Binding pIC50 = 4.7 4.7 -5 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
42635204 187865 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495678 187865 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
10826203 161939 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.2 C1=C(c2c(-c3ccccc3)[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2005.06.067
CHEMBL414668 161939 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.2 C1=C(c2c(-c3ccccc3)[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2005.06.067
118465009 138964 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 465 7 1 5 3.6 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3782008 138964 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 465 7 1 5 3.6 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
73356447 89740 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 386 3 1 4 4.2 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2013.03.006
CHEMBL2376561 89740 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 386 3 1 4 4.2 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2013.03.006
11724023 105025 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 328 4 2 6 2.1 CCNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113362 105025 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 328 4 2 6 2.1 CCNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
276 3513 None 37 Human Binding pIC50 = 8.7 8.7 81 20
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
5312149 3513 None 37 Human Binding pIC50 = 8.7 8.7 81 20
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
CHEMBL431298 3513 None 37 Human Binding pIC50 = 8.7 8.7 81 20
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
1043 1582 None 6 Human Binding pIC50 = 8.7 8.7 -23 27
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1582 None 6 Human Binding pIC50 = 8.7 8.7 -23 27
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1582 None 6 Human Binding pIC50 = 8.7 8.7 -23 27
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223.0 1582 None 6 Human Binding pIC50 = 8.7 8.7 -23 27
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1582 None 6 Human Binding pIC50 = 8.7 8.7 -23 27
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1582 None 6 Human Binding pIC50 = 8.7 8.7 -23 27
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
118465087 138807 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 503 7 2 5 3.5 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3779933 138807 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 503 7 2 5 3.5 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
118465051 138967 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 495 8 1 6 3.6 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCN(C)CC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3782049 138967 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 495 8 1 6 3.6 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCN(C)CC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
118465065 138937 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(F)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781574 138937 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(F)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
4106 2502 None 21 Human Binding pIC50 = 8.6 8.6 -2 33
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
5358812 2502 None 21 Human Binding pIC50 = 8.6 8.6 -2 33
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
89 2502 None 21 Human Binding pIC50 = 8.6 8.6 -2 33
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
CHEMBL93240 2502 None 21 Human Binding pIC50 = 8.6 8.6 -2 33
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
10470893 105024 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 314 3 2 6 1.7 CNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113361 105024 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 314 3 2 6 1.7 CNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
150 2509 None 14 Human Binding pIC50 = 8.6 8.6 -2 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2509 None 14 Human Binding pIC50 = 8.6 8.6 -2 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2509 None 14 Human Binding pIC50 = 8.6 8.6 -2 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226.0 2509 None 14 Human Binding pIC50 = 8.6 8.6 -2 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2509 None 14 Human Binding pIC50 = 8.6 8.6 -2 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2509 None 14 Human Binding pIC50 = 8.6 8.6 -2 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
118465026 138888 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780950 138888 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
9924293 68918 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL1922641 68918 None 0 Human Binding pIC50 = 8.6 8.6 - 1
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
118456745 138837 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 425 7 2 5 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780359 138837 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 425 7 2 5 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
73350387 89731 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL2376486 89731 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
11333554 96714 None 18 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL26379 96714 None 18 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
44155994 57667 None 4 Human Binding pIC50 = 7.7 7.7 - 1
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668571 57667 None 4 Human Binding pIC50 = 7.7 7.7 - 1
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
3245407 48119 None 21 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL1550957 48119 None 21 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
5 139 None 45 Human Binding pIC50 = 6.7 6.7 -169 54
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 None 45 Human Binding pIC50 = 6.7 6.7 -169 54
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 None 45 Human Binding pIC50 = 6.7 6.7 -169 54
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 None 45 Human Binding pIC50 = 6.7 6.7 -169 54
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
22504458 105022 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 315 3 1 6 1.7 COc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113359 105022 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 315 3 1 6 1.7 COc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
72197486 102558 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393245 102558 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040361 102558 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
124087 1389 None 72 Human Binding pIC50 = 5.7 5.7 -28 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
124087.0 1389 None 72 Human Binding pIC50 = 5.7 5.7 -28 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 None 72 Human Binding pIC50 = 5.7 5.7 -28 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 None 72 Human Binding pIC50 = 5.7 5.7 -28 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 None 72 Human Binding pIC50 = 5.7 5.7 -28 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 None 72 Human Binding pIC50 = 5.7 5.7 -28 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
49864530 15663 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccccc1N1CCN(C)CC1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222028 15663 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccccc1N1CCN(C)CC1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
3191 102913 None 65 Human Binding pIC50 = 5.7 5.7 -15 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
3191.0 102913 None 65 Human Binding pIC50 = 5.7 5.7 -15 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102913 None 65 Human Binding pIC50 = 5.7 5.7 -15 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
DB11742 102913 None 65 Human Binding pIC50 = 5.7 5.7 -15 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
31101 729 None 28 Human Binding pIC50 = 7.7 7.7 -23 35
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
31101.0 729 None 28 Human Binding pIC50 = 7.7 7.7 -23 35
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 729 None 28 Human Binding pIC50 = 7.7 7.7 -23 35
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 729 None 28 Human Binding pIC50 = 7.7 7.7 -23 35
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 729 None 28 Human Binding pIC50 = 7.7 7.7 -23 35
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 729 None 28 Human Binding pIC50 = 7.7 7.7 -23 35
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
10427896 105012 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2014.01.003
CHEMBL3113349 105012 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2014.01.003
72197485 102544 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393244 102544 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040288 102544 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
49799703 10996 None 4 Human Binding pIC50 = 6.7 6.7 - 1
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173577 10996 None 4 Human Binding pIC50 = 6.7 6.7 - 1
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
10885636 111079 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 111079 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
44395664 66781 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
CHEMBL185850 66781 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
58149664 127490 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
CHEMBL3659970 127490 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
53322259 57669 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 nan
CHEMBL1668573 57669 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 nan
9931929 63483 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
CHEMBL179814 63483 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
2286 3183 None 36 Human Binding pIC50 = 5.6 5.6 -36 29
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3183 None 36 Human Binding pIC50 = 5.6 5.6 -36 29
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927.0 3183 None 36 Human Binding pIC50 = 5.6 5.6 -36 29
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3183 None 36 Human Binding pIC50 = 5.6 5.6 -36 29
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3183 None 36 Human Binding pIC50 = 5.6 5.6 -36 29
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3183 None 36 Human Binding pIC50 = 5.6 5.6 -36 29
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
2398 954 None 43 Human Binding pIC50 = 6.6 6.6 -5 28
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 954 None 43 Human Binding pIC50 = 6.6 6.6 -5 28
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801.0 954 None 43 Human Binding pIC50 = 6.6 6.6 -5 28
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 954 None 43 Human Binding pIC50 = 6.6 6.6 -5 28
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 954 None 43 Human Binding pIC50 = 6.6 6.6 -5 28
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 954 None 43 Human Binding pIC50 = 6.6 6.6 -5 28
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
44155992 57668 None 4 Human Binding pIC50 = 7.6 7.6 - 1
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1668572 57668 None 4 Human Binding pIC50 = 7.6 7.6 - 1
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
11725253 105021 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 347 3 1 6 1.4 C[S+]([O-])c1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113358 105021 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 347 3 1 6 1.4 C[S+]([O-])c1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
72548703 161661 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161661 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
53320009 56679 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 56679 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
274 3339 None 32 Human Binding pIC50 = 7.6 7.6 -1 3
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
5312145 3339 None 32 Human Binding pIC50 = 7.6 7.6 -1 3
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
CHEMBL433461 3339 None 32 Human Binding pIC50 = 7.6 7.6 -1 3
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
5 139 None 45 Human Binding pIC50 = 6.6 6.6 -169 54
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 139 None 45 Human Binding pIC50 = 6.6 6.6 -169 54
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 139 None 45 Human Binding pIC50 = 6.6 6.6 -169 54
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 139 None 45 Human Binding pIC50 = 6.6 6.6 -169 54
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
42388639 188160 None 0 Human Binding pIC50 = 5.6 5.6 - 6
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2008.04.023
CHEMBL497749 188160 None 0 Human Binding pIC50 = 5.6 5.6 - 6
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2008.04.023
2274 3173 None 38 Human Binding pIC50 = 6.6 6.6 -23 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 None 38 Human Binding pIC50 = 6.6 6.6 -23 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917.0 3173 None 38 Human Binding pIC50 = 6.6 6.6 -23 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 None 38 Human Binding pIC50 = 6.6 6.6 -23 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 None 38 Human Binding pIC50 = 6.6 6.6 -23 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 None 38 Human Binding pIC50 = 6.6 6.6 -23 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
1016 3747 None 45 Human Binding pIC50 = 5.6 5.6 -38 35
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan