Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL362628 5ht6r_human Human Yes 10.2 EC50 = 0.1 nM Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C
CHEMBL362628 5ht6r_human Human Yes 10.2 EC50 = 0.1 nM Funct
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
423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C
CHEMBL175835 5ht6r_human Human Yes 9.5 EC50 = 0.3 nM Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12
CHEMBL175835 5ht6r_human Human Yes 9.5 EC50 = 0.3 nM Funct
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
427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12
CHEMBL477650 5ht6r_human Human No 9.5 EC50 = 0.3 nM Funct
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
412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1
CHEMBL515307 5ht6r_human Human No 9.5 EC50 = 0.3 nM Funct
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
422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21
CHEMBL2113386 5ht6r_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1
CHEMBL2113386 5ht6r_human Human No 9.4 EC50 = 0.4 nM Funct
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
495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1
CHEMBL609741 5ht6r_human Human No 9.1 EC50 = 0.8 nM Funct
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
388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1
CHEMBL476006 5ht6r_human Human No 9.1 EC50 = 0.9 nM Funct
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
436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1
CHEMBL606639 5ht6r_human Human No 9.0 EC50 = 1 nM Funct
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
389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1
CHEMBL606547 5ht6r_human Human No 9.0 EC50 = 1.1 nM Funct
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
403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12
CHEMBL609995 5ht6r_human Human No 9.0 EC50 = 1.1 nM Funct
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
387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12
CHEMBL609742 5ht6r_human Human No 8.9 EC50 = 1.3 nM Funct
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
389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl
CHEMBL609992 5ht6r_human Human No 8.9 EC50 = 1.3 nM Funct
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
387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12
CHEMBL610254 5ht6r_human Human No 8.9 EC50 = 1.3 nM Funct
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
383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1
CHEMBL609737 5ht6r_human Human No 8.9 EC50 = 1.4 nM Funct
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
355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1
CHEMBL606556 5ht6r_human Human No 8.8 EC50 = 1.6 nM Funct
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
403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12
CHEMBL196622 5ht6r_human Human No 7.0 EC50 = 102.8 nM Funct
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
438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12
CHEMBL235986 5ht6r_human Human No 7.0 EC50 = 108.5 nM Funct
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
334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12
CHEMBL584049 5ht6r_human Human No 7.0 EC50 = 110 nM Funct
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
369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21
CHEMBL1550957 5ht6r_human Human Yes 6.0 EC50 = 1100 nM Funct
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
212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1
CHEMBL565724 5ht6r_human Human No 6.9 EC50 = 120 nM Funct
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
409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21
CHEMBL1094370 5ht6r_human Human No 6.9 EC50 = 125 nM Funct
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
360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12
CHEMBL26379 5ht6r_human Human Yes 6.9 EC50 = 130 nM Funct
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
223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1
CHEMBL475969 5ht6r_human Human No 7.9 EC50 = 14 nM Funct
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
406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1
CHEMBL235985 5ht6r_human Human No 6.8 EC50 = 148 nM Funct
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
378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12
CHEMBL584046 5ht6r_human Human No 7.8 EC50 = 15 nM Funct
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
363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21
CHEMBL565753 5ht6r_human Human No 6.8 EC50 = 154 nM Funct
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
335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21
CHEMBL193824 5ht6r_human Human No 6.8 EC50 = 159 nM Funct
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
338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21
CHEMBL236576 5ht6r_human Human No 5.8 EC50 = 1645 nM Funct
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
345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12
CHEMBL585931 5ht6r_human Human No 6.8 EC50 = 166 nM Funct
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
319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21
CHEMBL236577 5ht6r_human Human No 5.8 EC50 = 1680 nM Funct
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
361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12
CHEMBL393107 5ht6r_human Human No 6.8 EC50 = 172 nM Funct
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
401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1
CHEMBL238277 5ht6r_human Human No 6.8 EC50 = 174 nM Funct
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
334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12
CHEMBL188182 5ht6r_human Human Yes 6.8 EC50 = 178 nM Funct
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
300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21
CHEMBL565745 5ht6r_human Human No 7.8 EC50 = 18 nM Funct
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
335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21
CHEMBL606816 5ht6r_human Human No 6.8 EC50 = 180 nM Funct
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
453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12
CHEMBL236989 5ht6r_human Human No 6.7 EC50 = 181 nM Funct
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
340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12
CHEMBL394303 5ht6r_human Human Yes 6.7 EC50 = 191 nM Funct
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
314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1
CHEMBL606558 5ht6r_human Human No 8.7 EC50 = 2.2 nM Funct
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
399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1
CHEMBL2376482 5ht6r_human Human Yes 8.6 EC50 = 2.7 nM Funct
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
290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1
CHEMBL609994 5ht6r_human Human No 8.6 EC50 = 2.7 nM Funct
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
495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12
CHEMBL606548 5ht6r_human Human No 8.5 EC50 = 2.9 nM Funct
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
453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12
CHEMBL577687 5ht6r_human Human No 7.7 EC50 = 20 nM Funct
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
315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN
CHEMBL1081793 5ht6r_human Human No 6.7 EC50 = 203 nM Funct
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
416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1
CHEMBL399013 5ht6r_human Human No 5.7 EC50 = 2035 nM Funct
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
341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1
CHEMBL2376485 5ht6r_human Human No 7.7 EC50 = 21 nM Funct
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
367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1
CHEMBL393312 5ht6r_human Human No 6.6 EC50 = 231 nM Funct
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
359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1
CHEMBL371292 5ht6r_human Human No 7.6 EC50 = 24 nM Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21
CHEMBL568672 5ht6r_human Human No 7.6 EC50 = 24 nM Funct
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
319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21
CHEMBL371292 5ht6r_human Human No 7.6 EC50 = 24 nM Funct
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
340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21
CHEMBL236313 5ht6r_human Human No 7.6 EC50 = 25 nM Funct
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
437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1
CHEMBL578826 5ht6r_human Human No 7.6 EC50 = 25 nM Funct
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
329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21
CHEMBL578826 5ht6r_human Human No 7.6 EC50 = 25 nM Funct
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
329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21
CHEMBL371132 5ht6r_human Human No 6.6 EC50 = 269.5 nM Funct
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
356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21
CHEMBL576315 5ht6r_human Human No 7.6 EC50 = 27 nM Funct
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
301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21
CHEMBL236772 5ht6r_human Human No 6.6 EC50 = 273 nM Funct
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
409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12
CHEMBL400627 5ht6r_human Human No 6.6 EC50 = 278 nM Funct
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
345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12
CHEMBL565977 5ht6r_human Human No 7.6 EC50 = 28 nM Funct
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
397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21
CHEMBL391517 5ht6r_human Human No 6.5 EC50 = 297 nM Funct
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
409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12
CHEMBL457570 5ht6r_human Human No 8.5 EC50 = 3.2 nM Funct
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
406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1
CHEMBL606557 5ht6r_human Human No 8.5 EC50 = 3.2 nM Funct
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
437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12
CHEMBL393997 5ht6r_human Human No 7.5 EC50 = 30 nM Funct
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
375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12
CHEMBL579063 5ht6r_human Human No 7.5 EC50 = 30 nM Funct
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
347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21
CHEMBL393106 5ht6r_human Human No 6.5 EC50 = 306 nM Funct
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
373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1
CHEMBL1081094 5ht6r_human Human Yes 7.5 EC50 = 31 nM Funct
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
368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1
CHEMBL568249 5ht6r_human Human No 7.5 EC50 = 31 nM Funct
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
397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21
CHEMBL583389 5ht6r_human Human No 7.5 EC50 = 32 nM Funct
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
369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21
CHEMBL2376484 5ht6r_human Human No 7.5 EC50 = 32 nM Funct
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
360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1
CHEMBL2376487 5ht6r_human Human No 7.5 EC50 = 32 nM Funct
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
257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1
CHEMBL392746 5ht6r_human Human No 7.5 EC50 = 34 nM Funct
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
451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1
CHEMBL194568 5ht6r_human Human No 6.5 EC50 = 344.5 nM Funct
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
356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21
CHEMBL236404 5ht6r_human Human No 7.5 EC50 = 35 nM Funct
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
405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12
CHEMBL585098 5ht6r_human Human No 7.5 EC50 = 35 nM Funct
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
369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21
CHEMBL371292 5ht6r_human Human No 7.4 EC50 = 36 nM Funct
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
340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21
CHEMBL183203 5ht6r_human Human No 6.4 EC50 = 366 nM Funct
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
328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21
CHEMBL1082198 5ht6r_human Human No 7.4 EC50 = 38 nM Funct
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
362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12
CHEMBL235117 5ht6r_human Human No 7.4 EC50 = 38.7 nM Funct
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
423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1
CHEMBL1076684 5ht6r_human Human No 6.4 EC50 = 398 nM Funct
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
358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1
CHEMBL609993 5ht6r_human Human No 8.4 EC50 = 4.2 nM Funct
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
439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1
CHEMBL596199 5ht6r_human Human No 8.4 EC50 = 4.5 nM Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1
CHEMBL606559 5ht6r_human Human No 8.4 EC50 = 4.5 nM Funct
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
437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12
CHEMBL609743 5ht6r_human Human No 8.4 EC50 = 4.5 nM Funct
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
389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1
CHEMBL236976 5ht6r_human Human No 6.4 EC50 = 414 nM Funct
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
409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12
CHEMBL39 5ht6r_human Human Yes 7.4 EC50 = 42.1 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht6r_human Human Yes 7.4 EC50 = 43.6 nM Funct
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL365751 5ht6r_human Human Yes 7.4 EC50 = 44.8 nM Bind
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C
CHEMBL235070 5ht6r_human Human No 7.3 EC50 = 47 nM Funct
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
341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12
CHEMBL565730 5ht6r_human Human No 7.3 EC50 = 47 nM Funct
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
343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C
CHEMBL401018 5ht6r_human Human No 7.3 EC50 = 49 nM Funct
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
423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1
CHEMBL606705 5ht6r_human Human No 8.3 EC50 = 5.2 nM Funct
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
391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F
CHEMBL2376483 5ht6r_human Human No 8.3 EC50 = 5.3 nM Funct
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
230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1
CHEMBL609991 5ht6r_human Human No 8.2 EC50 = 5.8 nM Funct
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
423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1
CHEMBL392976 5ht6r_human Human No 7.3 EC50 = 50 nM Funct
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
409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1
CHEMBL393830 5ht6r_human Human No 7.3 EC50 = 50 nM Funct
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
375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12
CHEMBL565552 5ht6r_human Human No 7.3 EC50 = 51 nM Funct
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
379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21
CHEMBL363827 5ht6r_human Human No 7.3 EC50 = 51 nM Funct
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
356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21
CHEMBL398809 5ht6r_human Human No 6.3 EC50 = 520 nM Funct
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
395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12
CHEMBL236990 5ht6r_human Human No 7.3 EC50 = 54 nM Funct
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
384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12
CHEMBL1081095 5ht6r_human Human No 7.3 EC50 = 56 nM Funct
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
358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12
CHEMBL371318 5ht6r_human Human No 7.2 EC50 = 58.5 nM Funct
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
380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21
CHEMBL1079977 5ht6r_human Human No 6.2 EC50 = 592 nM Funct
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
391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 nM Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 nM Funct
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
380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 nM Funct
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
380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2
CHEMBL2376486 5ht6r_human Human No 8.2 EC50 = 6.6 nM Funct
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
258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1
CHEMBL1076665 5ht6r_human Human Yes 7.2 EC50 = 60 nM Funct
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
326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12
CHEMBL235734 5ht6r_human Human No 7.2 EC50 = 60 nM Funct
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
387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1
CHEMBL585930 5ht6r_human Human No 7.2 EC50 = 63 nM Funct
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
351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21
CHEMBL236104 5ht6r_human Human No 7.2 EC50 = 66 nM Funct
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
423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12
CHEMBL363843 5ht6r_human Human No 7.2 EC50 = 66 nM Funct
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
376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21
CHEMBL391713 5ht6r_human Human No 7.2 EC50 = 67 nM Funct
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
437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1
CHEMBL392899 5ht6r_human Human No 7.2 EC50 = 67 nM Funct
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
359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12
CHEMBL1080316 5ht6r_human Human No 7.2 EC50 = 68 nM Funct
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
344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 nM Bind
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
347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 nM Funct
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
347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 nM Funct
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
347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C
CHEMBL236812 5ht6r_human Human No 7.2 EC50 = 71 nM Funct
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
395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1
CHEMBL235306 5ht6r_human Human No 7.1 EC50 = 72 nM Funct
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
419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12
CHEMBL1081110 5ht6r_human Human No 7.1 EC50 = 73 nM Funct
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
388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1
CHEMBL363275 5ht6r_human Human No 7.1 EC50 = 73 nM Funct
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
300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12
CHEMBL236103 5ht6r_human Human No 7.1 EC50 = 80 nM Funct
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
409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12
CHEMBL1076583 5ht6r_human Human Yes 7.1 EC50 = 82 nM Funct
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
340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12
CHEMBL565731 5ht6r_human Human No 7.1 EC50 = 85 nM Funct
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
369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21
CHEMBL197845 5ht6r_human Human No 7.1 EC50 = 89.5 nM Funct
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
390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1
CHEMBL236987 5ht6r_human Human No 7.0 EC50 = 91 nM Funct
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
315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12
CHEMBL235118 5ht6r_human Human No 7.0 EC50 = 98 nM Funct
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
381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12
CHEMBL3781299 5ht6r_human Human No 9.8 IC50 = 0.2 nM Bind
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
517 7 1 5 3.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1
CHEMBL1922635 5ht6r_human Human Yes 9.6 IC50 = 0.2 nM Bind
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].
379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1
CHEMBL3781323 5ht6r_human Human No 9.6 IC50 = 0.3 nM Bind
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
457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCN(C)CC1
CHEMBL1922614 5ht6r_human Human Yes 9.5 IC50 = 0.3 nM Bind
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].
317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL3780579 5ht6r_human Human No 9.5 IC50 = 0.3 nM Bind
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
545 7 1 5 4.6 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1
CHEMBL1668587 5ht6r_human Human Yes 9.5 IC50 = 0.3 nM Bind
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].
346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL181066 5ht6r_human Human No 9.4 IC50 = 0.4 nM Funct
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
383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1
CHEMBL3781452 5ht6r_human Human No 9.3 IC50 = 0.5 nM Bind
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
457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCN(C)CC1
CHEMBL3779904 5ht6r_human Human No 9.3 IC50 = 0.5 nM Bind
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
469 8 1 6 3.1 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1
CHEMBL1922633 5ht6r_human Human Yes 9.3 IC50 = 0.6 nM Bind
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].
345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL187865 5ht6r_human Human No 9.2 IC50 = 0.6 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12
CHEMBL194307 5ht6r_human Human No 9.2 IC50 = 0.6 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12
CHEMBL1922639 5ht6r_human Human Yes 9.2 IC50 = 0.6 nM Bind
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].
359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1922630 5ht6r_human Human Yes 9.2 IC50 = 0.7 nM Bind
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].
331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL3780274 5ht6r_human Human No 9.2 IC50 = 0.7 nM Bind
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
443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCNCC1
CHEMBL353389 5ht6r_human Human No 9.2 IC50 = 0.7 nM Bind
Inhibition against human 5-hydroxytryptamine 6 receptorInhibition against human 5-hydroxytryptamine 6 receptor
356 5 1 1 5.1 CN(C)CCCc1c(-c2cccc(Br)c2)[nH]c2ccccc12
CHEMBL180221 5ht6r_human Human No 9.2 IC50 = 0.7 nM Funct
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
386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1
CHEMBL1668586 5ht6r_human Human Yes 9.1 IC50 = 0.7 nM Bind
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].
302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1
CHEMBL609739 5ht6r_human Human No 9.1 IC50 = 0.8 nM Funct
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
447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12
CHEMBL371886 5ht6r_human Human No 9.1 IC50 = 0.8 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC
CHEMBL444015 5ht6r_human Human No 9.1 IC50 = 0.8 nM Funct
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
353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1
CHEMBL2172186 5ht6r_human Human Yes 9.1 IC50 = 0.8 nM Bind
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.
357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3
CHEMBL1668588 5ht6r_human Human Yes 9.1 IC50 = 0.9 nM Bind
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].
332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1
CHEMBL3781179 5ht6r_human Human No 9.0 IC50 = 0.9 nM Bind
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
439 7 1 5 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCN(C)CC1
CHEMBL1091919 5ht6r_human Human Yes 9.0 IC50 = 0.9 nM Bind
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].
373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3
CHEMBL1091206 5ht6r_human Human No 9.0 IC50 = 1.0 nM Bind
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].
345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3
CHEMBL3781801 5ht6r_human Human No 9.0 IC50 = 1 nM Bind
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
455 8 2 6 2.8 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1
CHEMBL413525 5ht6r_human Human No 9.0 IC50 = 1 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12
CHEMBL3781263 5ht6r_human Human No 9.0 IC50 = 1.1 nM Bind
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
483 8 2 6 3.5 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1
CHEMBL610256 5ht6r_human Human No 9.0 IC50 = 1.1 nM Funct
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
473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12
CHEMBL1091207 5ht6r_human Human Yes 8.9 IC50 = 1.2 nM Bind
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].
359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3
CHEMBL3779974 5ht6r_human Human No 8.9 IC50 = 1.2 nM Bind
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
529 7 2 5 4.0 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(Br)cc34)CC2)cc1N1CCNCC1
CHEMBL3675189 5ht6r_human Human No 8.9 IC50 = 1.3 nM Bind
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].
430 7 1 8 3.1 CCOC(=O)Cc1c(C)nc2c(S(=O)(=O)c3ccccc3)c(NC(C)C)nn2c1C
CHEMBL3780141 5ht6r_human Human No 8.9 IC50 = 1.3 nM Bind
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
453 7 2 5 3.5 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccccc23)cc1N1CCNCC1
CHEMBL3781239 5ht6r_human Human No 8.9 IC50 = 1.3 nM Bind
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
457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCN(C)CC1
CHEMBL3113554 5ht6r_human Human No 8.9 IC50 = 1.3 nM Bind
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
345 3 1 6 2.7 CSc1nc2ccc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL178385 5ht6r_human Human No 8.9 IC50 = 1.3 nM Funct
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
373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1
CHEMBL1277918 5ht6r_human Human No 8.9 IC50 = 1.4 nM Funct
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
462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21
CHEMBL3780011 5ht6r_human Human No 8.9 IC50 = 1.4 nM Bind
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
497 8 1 6 3.9 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1
CHEMBL2172193 5ht6r_human Human No 8.9 IC50 = 1.4 nM Bind
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.
371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3
CHEMBL1092241 5ht6r_human Human No 8.8 IC50 = 1.5 nM Bind
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].
373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3
CHEMBL2172187 5ht6r_human Human No 8.8 IC50 = 1.5 nM Bind
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.
371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3
CHEMBL1277565 5ht6r_human Human No 8.8 IC50 = 1.6 nM Funct
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
406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21
CHEMBL3781399 5ht6r_human Human No 8.8 IC50 = 1.6 nM Bind
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
443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCNCC1
CHEMBL610259 5ht6r_human Human No 8.8 IC50 = 1.6 nM Funct
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
447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12
CHEMBL1909065 5ht6r_human Human Yes 8.8 IC50 = 1.7 nM Bind
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)
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
CHEMBL1277564 5ht6r_human Human No 8.8 IC50 = 1.7 nM Funct
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
420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1
CHEMBL1277656 5ht6r_human Human No 8.8 IC50 = 1.7 nM Funct
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
434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21
CHEMBL3780861 5ht6r_human Human No 8.8 IC50 = 1.7 nM Bind
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
531 7 2 5 4.3 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCNCC1
CHEMBL361180 5ht6r_human Human No 8.8 IC50 = 1.7 nM Funct
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
397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1
CHEMBL1277751 5ht6r_human Human No 8.7 IC50 = 1.8 nM Funct
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
448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21
CHEMBL1277836 5ht6r_human Human No 8.7 IC50 = 1.8 nM Funct
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
448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21
CHEMBL1277657 5ht6r_human Human No 8.7 IC50 = 1.9 nM Funct
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
420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21
CHEMBL392541 5ht6r_human Human No 8.0 IC50 = 10 nM Funct
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
437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1
CHEMBL520129 5ht6r_human Human No 8.0 IC50 = 10 nM Funct
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
434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1
CHEMBL193351 5ht6r_human Human No 8.0 IC50 = 10 nM Bind
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
260 1 1 1 3.8 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(C)CC1
CHEMBL2376482 5ht6r_human Human Yes 8.0 IC50 = 10 nM Bind
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
290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1
CHEMBL2376487 5ht6r_human Human No 8.0 IC50 = 10 nM Bind
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
257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1
CHEMBL1922635 5ht6r_human Human Yes 8.0 IC50 = 10 nM Funct
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.
379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1
CHEMBL606817 5ht6r_human Human No 8.0 IC50 = 10.4 nM Funct
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
419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12
CHEMBL4799851 5ht6r_human Human No 8.0 IC50 = 10.6 nM Funct
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
453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21
CHEMBL459989 5ht6r_human Human No 7.0 IC50 = 100 nM Funct
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
373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1
CHEMBL39 5ht6r_human Human Yes 7.0 IC50 = 100 nM Bind
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL195239 5ht6r_human Human Yes 7.0 IC50 = 100 nM Bind
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
274 2 2 1 4.3 CC(C)c1[nH]c2ccc(Cl)cc2c1C1=CCNCC1
CHEMBL2376489 5ht6r_human Human No 7.0 IC50 = 100 nM Bind
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
270 3 2 2 3.6 Cc1[nH]c2ccc(OC(C)C)cc2c1C1=CCNCC1
CHEMBL2376493 5ht6r_human Human No 7.0 IC50 = 100 nM Bind
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
274 2 1 2 4.0 CCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21
CHEMBL3286580 5ht6r_human Human Yes 6.0 IC50 = 1000 nM Funct
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
398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F
CHEMBL1170463 5ht6r_human Human Yes 6.0 IC50 = 1000 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
477 5 1 8 5.7 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1C
CHEMBL591570 5ht6r_human Human Yes 6.0 IC50 = 1000 nM Funct
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
306 2 0 2 4.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccccc2)C1
CHEMBL2376491 5ht6r_human Human No 6.0 IC50 = 1000 nM Bind
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
288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1
CHEMBL1278091 5ht6r_human Human No 7.0 IC50 = 101 nM Funct
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
390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1
CHEMBL1668587 5ht6r_human Human Yes 7.0 IC50 = 101 nM Funct
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.
346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1783608 5ht6r_human Human No 7.0 IC50 = 102 nM Funct
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
405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1
CHEMBL1642850 5ht6r_human Human No 7.0 IC50 = 103 nM Funct
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
408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1739214 5ht6r_human Human No 7.0 IC50 = 103 nM Funct
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
408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1642878 5ht6r_human Human No 7.0 IC50 = 103 nM Funct
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
422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1739546 5ht6r_human Human No 7.0 IC50 = 103 nM Funct
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
422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL3670291 5ht6r_human Human Yes 6.0 IC50 = 1037 nM Funct
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.
365 4 1 7 2.7 CNc1nn2c(-c3cccnc3)ccnc2c1S(=O)(=O)c1ccccc1
CHEMBL1783957 5ht6r_human Human Yes 6.0 IC50 = 1040 nM Funct
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
369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1
CHEMBL1173281 5ht6r_human Human Yes 6.0 IC50 = 1040 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
435 3 0 9 2.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCOCC1)c1sccc12
CHEMBL459988 5ht6r_human Human No 7.0 IC50 = 105 nM Funct
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
407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1
CHEMBL1173570 5ht6r_human Human Yes 6.0 IC50 = 1050 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
463 7 1 8 4.4 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1
CHEMBL589389 5ht6r_human Human Yes 6.0 IC50 = 1050 nM Funct
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
320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1
CHEMBL1783963 5ht6r_human Human Yes 5.0 IC50 = 10690 nM Funct
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
323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1
CHEMBL1079976 5ht6r_human Human No 7.0 IC50 = 107 nM Funct
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
404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1
CHEMBL1080380 5ht6r_human Human No 7.0 IC50 = 107 nM Funct
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
376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12
CHEMBL365753 5ht6r_human Human No 7.0 IC50 = 107.1 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1
CHEMBL1170291 5ht6r_human Human Yes 6.0 IC50 = 1070 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
509 4 1 8 5.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12
CHEMBL1783582 5ht6r_human Human No 7.0 IC50 = 108 nM Funct
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
397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1
CHEMBL1278180 5ht6r_human Human No 7.0 IC50 = 108 nM Funct
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
390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1
CHEMBL1173061 5ht6r_human Human Yes 6.0 IC50 = 1080 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
449 6 1 8 4.2 CC(Cc1ccccc1)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12
CHEMBL1559 5ht6r_human Human Yes 5.0 IC50 = 10887 nM Bind
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)
414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1
CHEMBL91 5ht6r_human Human Yes 5.0 IC50 = 10887 nM Bind
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)
414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1
CHEMBL1201049 5ht6r_human Human Yes 5.0 IC50 = 10899 nM Bind
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)
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL808 5ht6r_human Human Yes 5.0 IC50 = 10899 nM Bind
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)
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL3893286 5ht6r_human Human No 5.0 IC50 = 10900 nM Funct
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
403 7 1 4 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc(Cl)c2)nn1-c1ccccc1
CHEMBL394233 5ht6r_human Human No 8.0 IC50 = 11 nM Funct
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
381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12
CHEMBL484345 5ht6r_human Human No 8.0 IC50 = 11 nM Funct
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
394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12
CHEMBL93240 5ht6r_human Human Yes 8.0 IC50 = 11 nM Funct
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
356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C
CHEMBL42 5ht6r_human Human Yes 8.0 IC50 = 11 nM Bind
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)
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL3781260 5ht6r_human Human No 8.0 IC50 = 11 nM Bind
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
469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCN(C)CC1
CHEMBL3781948 5ht6r_human Human No 8.0 IC50 = 11 nM Bind
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
471 7 2 5 3.7 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3cc(F)ccc23)cc1N1CCNCC1
CHEMBL1642128 5ht6r_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
463 3 0 5 4.1 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)C(C)CC2=O
CHEMBL3113350 5ht6r_human Human No 8.0 IC50 = 11 nM Bind
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
365 3 1 6 3.0 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1Cl
CHEMBL369910 5ht6r_human Human No 8.0 IC50 = 11 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12
CHEMBL360234 5ht6r_human Human No 8.0 IC50 = 11.2 nM Funct
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
387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1
CHEMBL1922630 5ht6r_human Human Yes 8.0 IC50 = 11.3 nM Funct
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.
331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1935594 5ht6r_human Human No 7.9 IC50 = 11.7 nM Funct
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
359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21
CHEMBL1170672 5ht6r_human Human Yes 7.9 IC50 = 11.9 nM Bind
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
399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12
CHEMBL1172726 5ht6r_human Human Yes 7.0 IC50 = 110 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12
CHEMBL1173362 5ht6r_human Human Yes 7.0 IC50 = 110 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12
CHEMBL196466 5ht6r_human Human No 7.0 IC50 = 110 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21
CHEMBL366012 5ht6r_human Human No 7.0 IC50 = 110 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21
CHEMBL1172791 5ht6r_human Human Yes 6.0 IC50 = 1100 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
477 6 0 8 4.8 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12
CHEMBL1170464 5ht6r_human Human Yes 6.0 IC50 = 1110 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
477 5 1 8 5.7 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)cc1C
CHEMBL1668502 5ht6r_human Human Yes 6.0 IC50 = 1110 nM Funct
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.
319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1
CHEMBL1276926 5ht6r_human Human No 7.0 IC50 = 112 nM Funct
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
370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1
CHEMBL1909072 5ht6r_human Human Yes 7.0 IC50 = 112 nM Bind
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)
401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1
CHEMBL1668574 5ht6r_human Human Yes 7.0 IC50 = 112 nM Bind
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1
CHEMBL434932 5ht6r_human Human No 7.0 IC50 = 112 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12
CHEMBL1173206 5ht6r_human Human Yes 6.0 IC50 = 1120 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
447 3 0 8 4.1 CC1CCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)CC1
CHEMBL1201023 5ht6r_human Human Yes 6.0 IC50 = 1121 nM Bind
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)
269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1
CHEMBL900 5ht6r_human Human Yes 6.0 IC50 = 1121 nM Bind
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)
269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1
CHEMBL589149 5ht6r_human Human Yes 6.0 IC50 = 1130 nM Funct
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
326 3 0 2 4.2 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(F)cc2)C1
CHEMBL534 5ht6r_human Human Yes 5.9 IC50 = 1141 nM Bind
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)
309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1
CHEMBL1170682 5ht6r_human Human Yes 5.9 IC50 = 1150 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12
CHEMBL1170686 5ht6r_human Human Yes 5.9 IC50 = 1150 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
471 5 1 9 4.6 COc1ccccc1Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12
CHEMBL1170276 5ht6r_human Human Yes 5.9 IC50 = 1160 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
435 6 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12
CHEMBL589390 5ht6r_human Human Yes 5.9 IC50 = 1160 nM Funct
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
319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1
CHEMBL460194 5ht6r_human Human No 6.9 IC50 = 117 nM Funct
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
411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12
CHEMBL1172597 5ht6r_human Human Yes 5.9 IC50 = 1170 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(Cl)cc1)c1sccc12
CHEMBL1762569 5ht6r_human Human No 5.9 IC50 = 1177 nM Funct
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.
330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1
CHEMBL1642884 5ht6r_human Human No 6.9 IC50 = 118 nM Funct
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
374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1739659 5ht6r_human Human No 6.9 IC50 = 118 nM Funct
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
374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1222137 5ht6r_human Human No 5.9 IC50 = 1180 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
451 4 0 2 5.0 CC(C)N(c1cccc(I)c1)S(=O)(=O)c1ccc2ccccc2c1
CHEMBL1171632 5ht6r_human Human Yes 5.9 IC50 = 1190 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12
CHEMBL1642882 5ht6r_human Human No 7.9 IC50 = 12 nM Funct
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
390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1739102 5ht6r_human Human No 7.9 IC50 = 12 nM Funct
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
390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL157138 5ht6r_human Human Yes 7.9 IC50 = 12 nM Bind
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)
338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC
CHEMBL3113360 5ht6r_human Human No 7.9 IC50 = 12 nM Bind
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
329 4 1 6 2.0 CCOc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL3113561 5ht6r_human Human No 7.9 IC50 = 12 nM Bind
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
423 3 1 6 3.4 CSc1nc2c(C)cc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL1922614 5ht6r_human Human Yes 7.9 IC50 = 12 nM Funct
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.
317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1922619 5ht6r_human Human Yes 7.9 IC50 = 12 nM Funct
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.
345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL3670293 5ht6r_human Human No 7.9 IC50 = 12 nM Funct
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.
395 5 1 8 2.7 CNc1nn2c(OC)cc(-c3cccnc3)nc2c1S(=O)(=O)c1ccccc1
CHEMBL598229 5ht6r_human Human No 7.9 IC50 = 12.5 nM Funct
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
392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1
CHEMBL236541 5ht6r_human Human No 6.9 IC50 = 120 nM Funct
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
389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1
CHEMBL459348 5ht6r_human Human No 6.9 IC50 = 120 nM Funct
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
411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12
CHEMBL1169724 5ht6r_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
469 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccc(Cl)c2)c2sccc23)cc1
CHEMBL3113355 5ht6r_human Human No 6.9 IC50 = 120 nM Bind
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
345 3 0 6 2.4 C/N=c1/c(S(=O)(=O)c2ccccc2)c(SC)nc2ccccn12
CHEMBL39 5ht6r_human Human Yes 6.9 IC50 = 120 nM Bind
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht6r_human Human Yes 6.9 IC50 = 120 nM Bind
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1173433 5ht6r_human Human No 5.9 IC50 = 1200 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12
CHEMBL1170472 5ht6r_human Human Yes 5.9 IC50 = 1210 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
455 4 1 8 4.9 Cc1ccc(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)cc1
CHEMBL1171486 5ht6r_human Human Yes 5.9 IC50 = 1220 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
477 7 1 8 4.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCCc2ccccc2)c2sccc23)c1
CHEMBL1173005 5ht6r_human Human Yes 5.9 IC50 = 1220 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
421 5 0 8 3.7 CCN(CC)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12
CHEMBL1173508 5ht6r_human Human No 5.9 IC50 = 1220 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1
CHEMBL194786 5ht6r_human Human No 6.9 IC50 = 123 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1
CHEMBL1642880 5ht6r_human Human No 6.9 IC50 = 125 nM Funct
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
356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1739648 5ht6r_human Human No 6.9 IC50 = 125 nM Funct
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
356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1169898 5ht6r_human Human Yes 5.9 IC50 = 1250 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
479 5 1 10 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc4c(c2)OCO4)c2sccc23)cc1
CHEMBL1172795 5ht6r_human Human No 5.9 IC50 = 1250 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12
CHEMBL104 5ht6r_human Human Yes 4.9 IC50 = 12543 nM Bind
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)
344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1
CHEMBL1642888 5ht6r_human Human No 6.9 IC50 = 126 nM Funct
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
386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1
CHEMBL1739615 5ht6r_human Human No 6.9 IC50 = 126 nM Funct
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
386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1
CHEMBL144265 5ht6r_human Human No 6.9 IC50 = 126 nM Bind
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
423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL93240 5ht6r_human Human Yes 6.9 IC50 = 127 nM Funct
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
356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C
CHEMBL411 5ht6r_human Human Yes 4.9 IC50 = 12892 nM Bind
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)
268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1
CHEMBL1641610 5ht6r_human Human No 6.9 IC50 = 129 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
399 3 0 5 2.5 Cc1ccc(S(=O)(=O)N2CCC(=O)c3c(N4CCN(C)CC4)cccc32)cc1
CHEMBL1172868 5ht6r_human Human Yes 5.9 IC50 = 1290 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12
CHEMBL1642848 5ht6r_human Human No 7.9 IC50 = 13 nM Funct
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
366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1739253 5ht6r_human Human No 7.9 IC50 = 13 nM Funct
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
366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1277105 5ht6r_human Human Yes 7.9 IC50 = 13 nM Funct
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
392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12
CHEMBL2172182 5ht6r_human Human No 7.9 IC50 = 13 nM Bind
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.
342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3
CHEMBL715 5ht6r_human Human Yes 7.9 IC50 = 13 nM Bind
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)
312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C
CHEMBL1221497 5ht6r_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1
CHEMBL444878 5ht6r_human Human No 7.9 IC50 = 13.8 nM Funct
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
352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1
CHEMBL39 5ht6r_human Human Yes 6.9 IC50 = 130 nM Bind
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL17157 5ht6r_human Human Yes 5.9 IC50 = 1306 nM Bind
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)
471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O
CHEMBL394232 5ht6r_human Human No 6.9 IC50 = 132 nM Funct
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
373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1
CHEMBL1277999 5ht6r_human Human No 6.9 IC50 = 132 nM Funct
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
374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1
CHEMBL1949761 5ht6r_human Human No 6.9 IC50 = 133 nM Funct
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
349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl
CHEMBL1963096 5ht6r_human Human No 6.9 IC50 = 133 nM Funct
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
349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl
CHEMBL1173284 5ht6r_human Human Yes 5.9 IC50 = 1330 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
463 5 0 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)cc1C
CHEMBL62193 5ht6r_human Human Yes 5.9 IC50 = 1339 nM Bind
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)
310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1
CHEMBL1173774 5ht6r_human Human No 5.9 IC50 = 1340 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
441 3 0 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(C2CCN(C)CC2)c2sccc23)c1
CHEMBL236405 5ht6r_human Human No 6.9 IC50 = 135 nM Funct
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
405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12
CHEMBL1949762 5ht6r_human Human No 6.9 IC50 = 135 nM Funct
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
391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1
CHEMBL1962863 5ht6r_human Human No 6.9 IC50 = 135 nM Funct
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
391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1
CHEMBL367088 5ht6r_human Human No 6.9 IC50 = 135 nM Bind
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12
CHEMBL2207386 5ht6r_human Human Yes 6.9 IC50 = 135.1 nM Funct
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
447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1
CHEMBL1170689 5ht6r_human Human Yes 5.9 IC50 = 1350 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
513 4 1 8 5.3 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)cc1C
CHEMBL116735 5ht6r_human Human No 5.9 IC50 = 1350 nM Bind
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL1852341 5ht6r_human Human No 6.9 IC50 = 136 nM Bind
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1
CHEMBL3216098 5ht6r_human Human No 6.9 IC50 = 136 nM Bind
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1
CHEMBL1949773 5ht6r_human Human No 5.9 IC50 = 1363 nM Funct
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
351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21
CHEMBL1963026 5ht6r_human Human No 5.9 IC50 = 1363 nM Funct
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
351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21
CHEMBL1642874 5ht6r_human Human No 6.9 IC50 = 137 nM Funct
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
450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12
CHEMBL1739700 5ht6r_human Human No 6.9 IC50 = 137 nM Funct
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
450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12
CHEMBL1172595 5ht6r_human Human Yes 5.9 IC50 = 1370 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
451 6 1 9 3.8 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)c1
CHEMBL1170274 5ht6r_human Human Yes 5.9 IC50 = 1380 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
449 5 1 8 4.8 CCc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1
CHEMBL1642886 5ht6r_human Human No 7.9 IC50 = 14 nM Funct
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
398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1
CHEMBL1739606 5ht6r_human Human No 7.9 IC50 = 14 nM Funct
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
398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1
CHEMBL606765 5ht6r_human Human No 7.9 IC50 = 14.1 nM Funct
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
437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12
CHEMBL178234 5ht6r_human Human No 7.9 IC50 = 14.1 nM Funct
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
378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21
CHEMBL281937 5ht6r_human Human Yes 7.8 IC50 = 14.8 nM Funct
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
302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1
CHEMBL1170672 5ht6r_human Human Yes 6.9 IC50 = 140 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12
CHEMBL1172404 5ht6r_human Human Yes 6.9 IC50 = 140 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
461 4 1 8 5.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12
CHEMBL629 5ht6r_human Human Yes 6.9 IC50 = 140 nM Bind
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)
277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C
CHEMBL2414704 5ht6r_human Human No 5.9 IC50 = 1400 nM Funct
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
551 6 0 7 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c(N(C)C)cccc34)c3ccccc23)CC1
CHEMBL3398395 5ht6r_human Human No 5.9 IC50 = 1400 nM Funct
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
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
CHEMBL4643549 5ht6r_human Human No 4.9 IC50 = 14000 nM Bind
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
430 5 1 6 4.0 CC(C)c1ccc(S(=O)(=O)Nc2ccc3nc(N4CCN(C)CC4)sc3c2)cc1
CHEMBL1670 5ht6r_human Human Yes 5.9 IC50 = 1402 nM Bind
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)
318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1
CHEMBL1086626 5ht6r_human Human No 5.9 IC50 = 1412 nM Bind
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1
CHEMBL236335 5ht6r_human Human No 6.9 IC50 = 142 nM Funct
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
375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1
CHEMBL3911908 5ht6r_human Human No 5.9 IC50 = 1420 nM Funct
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
420 7 1 5 4.1 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccccc1
CHEMBL1172723 5ht6r_human Human Yes 5.8 IC50 = 1430 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
469 4 1 8 5.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2ccc(Cl)cc2)c2sccc23)cc1C
CHEMBL589386 5ht6r_human Human Yes 5.8 IC50 = 1440 nM Funct
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
320 2 0 2 4.7 Cc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1
CHEMBL1762570 5ht6r_human Human Yes 6.8 IC50 = 147 nM Bind
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1
CHEMBL1172790 5ht6r_human Human Yes 5.8 IC50 = 1480 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
463 5 0 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)c1
CHEMBL1170439 5ht6r_human Human Yes 5.8 IC50 = 1490 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
403 6 1 9 2.5 COCCNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12
CHEMBL1642851 5ht6r_human Human No 7.8 IC50 = 15 nM Funct
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
406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1739215 5ht6r_human Human No 7.8 IC50 = 15 nM Funct
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
406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL3260795 5ht6r_human Human No 7.8 IC50 = 15 nM Funct
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
372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1
CHEMBL568673 5ht6r_human Human No 7.8 IC50 = 15 nM Funct
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
397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21
CHEMBL1099284 5ht6r_human Human Yes 7.8 IC50 = 15 nM Funct
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
359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1
CHEMBL1199172 5ht6r_human Human Yes 7.8 IC50 = 15 nM Funct
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
359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1
CHEMBL1385840 5ht6r_human Human Yes 7.8 IC50 = 15 nM Bind
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)
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
CHEMBL1642127 5ht6r_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
463 3 0 5 4.1 Cc1ccc2c(c1N1CCN(C)CC1)C(=O)CC(C)N2S(=O)(=O)c1ccc2ccccc2c1
CHEMBL3675190 5ht6r_human Human No 7.8 IC50 = 15.3 nM Bind
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].
401 5 1 7 1.9 CNc1nn2c(C)c(CC(=O)N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL194590 5ht6r_human Human No 7.8 IC50 = 15.5 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1
CHEMBL604102 5ht6r_human Human No 7.8 IC50 = 15.7 nM Funct
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
392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1
CHEMBL1170679 5ht6r_human Human Yes 6.8 IC50 = 150 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12)c1ccccc1
CHEMBL1172793 5ht6r_human Human Yes 6.8 IC50 = 150 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
461 5 1 9 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccs1)c1sccc12
CHEMBL1173777 5ht6r_human Human Yes 6.8 IC50 = 150 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
437 7 1 9 3.3 COCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12
CHEMBL592516 5ht6r_human Human Yes 5.8 IC50 = 1500 nM Funct
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
336 3 0 3 4.4 COc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1
CHEMBL723 5ht6r_human Human Yes 5.8 IC50 = 1519 nM Bind
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)
406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O
CHEMBL1173706 5ht6r_human Human Yes 5.8 IC50 = 1520 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
427 3 0 8 3.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCCCC2)c2sccc23)c1
CHEMBL954 5ht6r_human Human Yes 5.8 IC50 = 1522 nM Bind
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)
405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1
CHEMBL1642419 5ht6r_human Human No 5.8 IC50 = 1528 nM Funct
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
451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1
CHEMBL325516 5ht6r_human Human No 5.8 IC50 = 1530 nM Bind
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL1173207 5ht6r_human Human Yes 5.8 IC50 = 1540 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
447 3 0 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCCCCC1)c1sccc12
CHEMBL1922620 5ht6r_human Human Yes 5.8 IC50 = 1549 nM Funct
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.
388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1642862 5ht6r_human Human No 6.8 IC50 = 156 nM Funct
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
380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1739117 5ht6r_human Human No 6.8 IC50 = 156 nM Funct
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
380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1668582 5ht6r_human Human No 6.8 IC50 = 156 nM Funct
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.
371 3 0 6 3.4 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1
CHEMBL599466 5ht6r_human Human No 6.8 IC50 = 157 nM Funct
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
434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21
CHEMBL1171092 5ht6r_human Human Yes 5.8 IC50 = 1570 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12
CHEMBL1783953 5ht6r_human Human Yes 4.8 IC50 = 15750 nM Funct
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
291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1
CHEMBL592752 5ht6r_human Human Yes 6.8 IC50 = 158 nM Funct
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
304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1
CHEMBL575310 5ht6r_human Human No 5.8 IC50 = 1580 nM Funct
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
434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1
CHEMBL1783958 5ht6r_human Human Yes 5.8 IC50 = 1590 nM Funct
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
359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1
CHEMBL1642889 5ht6r_human Human No 7.8 IC50 = 16 nM Funct
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
406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1739616 5ht6r_human Human No 7.8 IC50 = 16 nM Funct
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
406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1403281 5ht6r_human Human Yes 7.8 IC50 = 16 nM Bind
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)
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
CHEMBL3780270 5ht6r_human Human No 7.8 IC50 = 16 nM Bind
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
469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCNCC1
CHEMBL1222234 5ht6r_human Human No 7.8 IC50 = 16 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12
CHEMBL1668585 5ht6r_human Human Yes 7.8 IC50 = 16 nM Funct
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.
302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL21343 5ht6r_human Human Yes 7.8 IC50 = 16 nM Bind
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1
CHEMBL292759 5ht6r_human Human Yes 7.8 IC50 = 16 nM Bind
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1
CHEMBL598443 5ht6r_human Human No 7.8 IC50 = 16.5 nM Funct
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
378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1
CHEMBL3659969 5ht6r_human Human No 7.8 IC50 = 16.6 nM Bind
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.
374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3
CHEMBL1091919 5ht6r_human Human Yes 7.8 IC50 = 16.8 nM Funct
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
373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3
CHEMBL605938 5ht6r_human Human No 5.8 IC50 = 1600 nM Funct
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
420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12
CHEMBL1173127 5ht6r_human Human Yes 5.8 IC50 = 1600 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
401 5 1 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1
CHEMBL964 5ht6r_human Human Yes 4.8 IC50 = 16001 nM Bind
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)
296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC
CHEMBL479548 5ht6r_human Human No 6.8 IC50 = 162 nM Funct
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
356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2
CHEMBL1065 5ht6r_human Human Yes 6.8 IC50 = 162 nM Bind
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)
353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO
CHEMBL1172938 5ht6r_human Human Yes 5.8 IC50 = 1620 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
493 5 1 9 3.5 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12
CHEMBL1642121 5ht6r_human Human No 6.8 IC50 = 165 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
465 4 0 6 3.4 COc1cc2c(cc1N1CCN(C)CC1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O
CHEMBL2407545 5ht6r_human Human No 5.8 IC50 = 1660 nM Funct
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
430 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(Cl)c4C)n[nH]c3C2=O)cc1
CHEMBL41 5ht6r_human Human Yes 5.8 IC50 = 1661 nM Bind
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)
309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F
CHEMBL762 5ht6r_human Human Yes 5.8 IC50 = 1670 nM Bind
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)
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL601304 5ht6r_human Human No 5.8 IC50 = 1680 nM Funct
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
304 2 0 2 4.3 Cc1ccc2c(c1)C1CN(C)CCC1N2/C=C/c1ccccc1
CHEMBL1852516 5ht6r_human Human No 5.8 IC50 = 1682 nM Bind
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1
CHEMBL3216758 5ht6r_human Human No 5.8 IC50 = 1682 nM Bind
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1
CHEMBL3675191 5ht6r_human Human Yes 5.8 IC50 = 1683 nM Funct
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.
472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL15245 5ht6r_human Human Yes 5.8 IC50 = 1689 nM Bind
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)
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
CHEMBL182099 5ht6r_human Human No 6.8 IC50 = 169 nM Funct
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
396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21
CHEMBL1086719 5ht6r_human Human No 7.8 IC50 = 17 nM Funct
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
374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1
CHEMBL1277466 5ht6r_human Human No 7.8 IC50 = 17 nM Funct
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
406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1
CHEMBL1642120 5ht6r_human Human No 7.8 IC50 = 17 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
449 3 0 5 3.8 C[C@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1
CHEMBL42 5ht6r_human Human Yes 7.8 IC50 = 17 nM Bind
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
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL1091208 5ht6r_human Human Yes 7.8 IC50 = 17.2 nM Bind
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].
359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3
CHEMBL236988 5ht6r_human Human No 7.8 IC50 = 17.5 nM Funct
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
360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC
CHEMBL597009 5ht6r_human Human No 7.8 IC50 = 17.5 nM Funct
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
420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1
CHEMBL1173359 5ht6r_human Human Yes 7.8 IC50 = 17.5 nM Bind
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
415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12
CHEMBL4175829 5ht6r_human Human No 7.8 IC50 = 17.6 nM Funct
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
339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1
CHEMBL4175829 5ht6r_human Human No 7.8 IC50 = 17.6 nM Bind
Partial inverse agonist activity at 5HT6R (unknown origin)Partial inverse agonist activity at 5HT6R (unknown origin)
339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1
CHEMBL484333 5ht6r_human Human No 6.8 IC50 = 170 nM Funct
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
462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1169707 5ht6r_human Human Yes 6.8 IC50 = 170 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12
CHEMBL1170696 5ht6r_human Human Yes 6.8 IC50 = 170 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
433 4 1 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCC1)c1sccc12
CHEMBL1170886 5ht6r_human Human Yes 6.8 IC50 = 170 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
427 4 1 8 4.3 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12
CHEMBL1172789 5ht6r_human Human Yes 6.8 IC50 = 170 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
463 5 1 8 5.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)c1
CHEMBL1922621 5ht6r_human Human No 6.8 IC50 = 172 nM Funct
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.
402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1922624 5ht6r_human Human Yes 6.8 IC50 = 173 nM Funct
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.
400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1642853 5ht6r_human Human No 6.8 IC50 = 174 nM Funct
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
420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12
CHEMBL1739217 5ht6r_human Human No 6.8 IC50 = 174 nM Funct
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
420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12
CHEMBL3675191 5ht6r_human Human Yes 6.8 IC50 = 174 nM Bind
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].
472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1170280 5ht6r_human Human Yes 5.8 IC50 = 1750 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
449 5 1 8 4.8 CCc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1
CHEMBL591801 5ht6r_human Human No 5.8 IC50 = 1750 nM Funct
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
308 2 0 2 4.1 CN1CCC2C(C1)c1cc(F)ccc1N2/C=C/c1ccccc1
CHEMBL574403 5ht6r_human Human No 6.8 IC50 = 176 nM Funct
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
449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12
CHEMBL1668569 5ht6r_human Human Yes 6.8 IC50 = 177 nM Funct
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.
349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1
CHEMBL4293999 5ht6r_human Human No 6.8 IC50 = 177.6 nM Funct
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
475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2
CHEMBL4081529 5ht6r_human Human No 5.8 IC50 = 1780 nM Funct
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
438 7 1 5 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccc(F)cc1
CHEMBL806 5ht6r_human Human Yes 4.8 IC50 = 17814 nM Bind
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)
276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1
CHEMBL1642424 5ht6r_human Human No 5.8 IC50 = 1783 nM Funct
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
421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1
CHEMBL1949760 5ht6r_human Human No 6.8 IC50 = 179 nM Funct
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
333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F
CHEMBL1962943 5ht6r_human Human No 6.8 IC50 = 179 nM Funct
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
333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F
CHEMBL1081794 5ht6r_human Human No 7.8 IC50 = 18 nM Funct
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
376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12
CHEMBL1668593 5ht6r_human Human Yes 7.8 IC50 = 18 nM Bind
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].
306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1
CHEMBL3113351 5ht6r_human Human No 7.8 IC50 = 18 nM Bind
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
399 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(Cl)c(Cl)c1
CHEMBL1170098 5ht6r_human Human Yes 6.8 IC50 = 180 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
449 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)cc1
CHEMBL592271 5ht6r_human Human Yes 6.8 IC50 = 180 nM Funct
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
320 2 0 2 4.7 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(F)cc2)CCN(C)C1
CHEMBL39 5ht6r_human Human Yes 6.8 IC50 = 180 nM Bind
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2414711 5ht6r_human Human No 5.8 IC50 = 1800 nM Funct
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
458 5 0 6 4.1 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1
CHEMBL1770373 5ht6r_human Human Yes 5.8 IC50 = 1800 nM Bind
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1
CHEMBL1169900 5ht6r_human Human Yes 5.7 IC50 = 1830 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
497 6 1 8 5.6 CC(C)c1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1
CHEMBL3398389 5ht6r_human Human No 5.7 IC50 = 1830 nM Funct
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
399 6 0 7 2.7 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccccc2)c2cccc([N+](=O)[O-])c12
CHEMBL395110 5ht6r_human Human Yes 5.7 IC50 = 1837 nM Bind
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)
310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1
CHEMBL1922621 5ht6r_human Human No 5.7 IC50 = 1858 nM Funct
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.
402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL236578 5ht6r_human Human No 6.7 IC50 = 186 nM Funct
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
359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1
CHEMBL631 5ht6r_human Human Yes 5.7 IC50 = 1863 nM Bind
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)
341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O
CHEMBL1668581 5ht6r_human Human Yes 6.7 IC50 = 187 nM Funct
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.
371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1
CHEMBL1668575 5ht6r_human Human Yes 5.7 IC50 = 1870 nM Funct
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.
323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1
CHEMBL1642116 5ht6r_human Human No 6.7 IC50 = 188 nM Funct
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
435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1
CHEMBL1173210 5ht6r_human Human Yes 6.7 IC50 = 188 nM Bind
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
385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12
CHEMBL1642864 5ht6r_human Human No 7.7 IC50 = 19 nM Funct
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
406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12
CHEMBL1739646 5ht6r_human Human No 7.7 IC50 = 19 nM Funct
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
406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12
CHEMBL1642883 5ht6r_human Human No 7.7 IC50 = 19 nM Funct
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
370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1
CHEMBL1739658 5ht6r_human Human No 7.7 IC50 = 19 nM Funct
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
370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1
CHEMBL60264 5ht6r_human Human Yes 7.7 IC50 = 19 nM Funct
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
487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I
CHEMBL1668588 5ht6r_human Human Yes 7.7 IC50 = 19 nM Funct
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.
332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1
CHEMBL180826 5ht6r_human Human No 7.7 IC50 = 19.5 nM Funct
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
340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21
CHEMBL1170093 5ht6r_human Human No 6.7 IC50 = 190 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
389 6 1 9 2.2 COCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12
CHEMBL1172792 5ht6r_human Human Yes 6.7 IC50 = 190 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
445 5 1 9 4.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccco1)c1sccc12
CHEMBL1170442 5ht6r_human Human Yes 5.7 IC50 = 1900 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
415 6 0 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(N(CC)CC)c2sccc23)cc1
CHEMBL1086756 5ht6r_human Human No 5.7 IC50 = 1904 nM Bind
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C
CHEMBL1173709 5ht6r_human Human Yes 5.7 IC50 = 1930 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
429 3 0 9 2.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCOCC2)c2sccc23)c1
CHEMBL633 5ht6r_human Human Yes 4.7 IC50 = 19441 nM Bind
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)
645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2
CHEMBL1173503 5ht6r_human Human Yes 5.7 IC50 = 1950 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
513 5 0 8 4.6 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12
CHEMBL2165541 5ht6r_human Human No 5.7 IC50 = 1951 nM Funct
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
422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1
CHEMBL495678 5ht6r_human Human No 5.7 IC50 = 1956 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1
CHEMBL571413 5ht6r_human Human No 6.7 IC50 = 197 nM Funct
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
335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21
CHEMBL1922623 5ht6r_human Human Yes 6.7 IC50 = 197 nM Funct
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.
387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL604669 5ht6r_human Human No 5.7 IC50 = 1980 nM Funct
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
316 2 0 2 5.0 C/C(=C/c1ccccc1)n1c2c(c3cc(C)ccc31)CN(C)CC2
CHEMBL1170664 5ht6r_human Human No 5.7 IC50 = 1990 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
441 3 0 8 4.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCC(C)CC2)c2sccc23)c1
CHEMBL1173132 5ht6r_human Human Yes 5.7 IC50 = 1990 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
442 4 1 9 1.9 NC(=O)C1CCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)CC1
CHEMBL4746584 5ht6r_human Human No 5.7 IC50 = 1995.3 nM Funct
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
284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1
CHEMBL4788250 5ht6r_human Human No 5.7 IC50 = 1995.3 nM Funct
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
284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1
CHEMBL1278000 5ht6r_human Human No 8.7 IC50 = 2 nM Funct
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
496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1
CHEMBL414668 5ht6r_human Human No 8.7 IC50 = 2 nM Bind
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
274 2 2 1 4.2 C1=C(c2c(-c3ccccc3)[nH]c3ccccc23)CCNC1
CHEMBL3782008 5ht6r_human Human No 8.7 IC50 = 2 nM Bind
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
465 7 1 5 3.6 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCN(C)CC1
CHEMBL2376561 5ht6r_human Human No 8.7 IC50 = 2 nM Bind
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
386 3 1 4 4.2 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1S(=O)(=O)c1ccccc1
CHEMBL3113362 5ht6r_human Human No 8.7 IC50 = 2 nM Bind
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
328 4 2 6 2.1 CCNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL431298 5ht6r_human Human Yes 8.7 IC50 = 2 nM Bind
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl
CHEMBL1668590 5ht6r_human Human Yes 8.7 IC50 = 2 nM Funct
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.
350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1
CHEMBL442 5ht6r_human Human Yes 8.7 IC50 = 2.0 nM Bind
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)
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
CHEMBL3779933 5ht6r_human Human No 8.7 IC50 = 2.1 nM Bind
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
503 7 2 5 3.5 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCNCC1
CHEMBL3782049 5ht6r_human Human No 8.7 IC50 = 2.1 nM Bind
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
495 8 1 6 3.6 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCN(C)CC5)c4)CC3)c2c1
CHEMBL1277752 5ht6r_human Human No 8.7 IC50 = 2.2 nM Funct
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
434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21
CHEMBL3781574 5ht6r_human Human No 8.6 IC50 = 2.3 nM Bind
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
469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(F)cc34)CC2)cc1N1CCNCC1
CHEMBL93240 5ht6r_human Human Yes 8.6 IC50 = 2.4 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C
CHEMBL3113361 5ht6r_human Human No 8.6 IC50 = 2.4 nM Bind
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
314 3 2 6 1.7 CNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL1201356 5ht6r_human Human Yes 8.6 IC50 = 2.5 nM Bind
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)
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
CHEMBL3780950 5ht6r_human Human No 8.6 IC50 = 2.6 nM Bind
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
469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCN(C)CC1
CHEMBL1922641 5ht6r_human Human No 8.6 IC50 = 2.7 nM Bind
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1
CHEMBL3780359 5ht6r_human Human No 8.6 IC50 = 2.7 nM Bind
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
425 7 2 5 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCNCC1
CHEMBL180606 5ht6r_human Human No 8.6 IC50 = 2.7 nM Funct
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
356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21
CHEMBL1083390 5ht6r_human Human Yes 8.6 IC50 = 2.8 nM Funct
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
353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1
CHEMBL1083390 5ht6r_human Human Yes 8.6 IC50 = 2.8 nM Funct
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
353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1
CHEMBL1277467 5ht6r_human Human No 8.5 IC50 = 2.9 nM Funct
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
370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21
CHEMBL1277837 5ht6r_human Human No 8.5 IC50 = 2.9 nM Funct
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
434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21
CHEMBL42 5ht6r_human Human Yes 7.7 IC50 = 20 nM Funct
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
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL2376486 5ht6r_human Human No 7.7 IC50 = 20 nM Bind
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
258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1
CHEMBL26379 5ht6r_human Human Yes 7.7 IC50 = 20 nM Bind
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
223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1
CHEMBL1668571 5ht6r_human Human Yes 7.7 IC50 = 20 nM Bind
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1
CHEMBL42 5ht6r_human Human Yes 7.7 IC50 = 20.3 nM Funct
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
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL1170673 5ht6r_human Human Yes 6.7 IC50 = 200 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12
CHEMBL1550957 5ht6r_human Human Yes 6.7 IC50 = 200 nM Bind
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
212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1
CHEMBL39 5ht6r_human Human Yes 6.7 IC50 = 200 nM Bind
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1173205 5ht6r_human Human Yes 5.7 IC50 = 2000 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
447 3 0 8 4.1 CC1CCCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)C1
CHEMBL1170688 5ht6r_human Human Yes 5.7 IC50 = 2010 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
513 4 1 8 5.3 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)c1
CHEMBL599023 5ht6r_human Human No 6.7 IC50 = 203 nM Funct
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
448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21
CHEMBL1172207 5ht6r_human Human Yes 5.7 IC50 = 2030 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
413 4 1 8 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)cc1
CHEMBL1172788 5ht6r_human Human Yes 5.7 IC50 = 2030 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
413 3 0 8 3.4 CC1CCCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)C1
CHEMBL2414732 5ht6r_human Human No 5.7 IC50 = 2040 nM Funct
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
446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1
CHEMBL2414732 5ht6r_human Human No 5.7 IC50 = 2040 nM Funct
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
446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1
CHEMBL2165524 5ht6r_human Human No 5.7 IC50 = 2056 nM Funct
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
432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1
CHEMBL1783970 5ht6r_human Human No 5.7 IC50 = 2060 nM Funct
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
306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1
CHEMBL591803 5ht6r_human Human Yes 4.7 IC50 = 20700 nM Funct
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
376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1
CHEMBL1642847 5ht6r_human Human No 7.7 IC50 = 21 nM Funct
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
420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12
CHEMBL1739252 5ht6r_human Human No 7.7 IC50 = 21 nM Funct
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
420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12
CHEMBL1935592 5ht6r_human Human No 7.7 IC50 = 21 nM Funct
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
343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1
CHEMBL3113359 5ht6r_human Human Yes 7.7 IC50 = 21 nM Bind
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
315 3 1 6 1.7 COc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL380556 5ht6r_human Human No 7.7 IC50 = 21 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21
CHEMBL606549 5ht6r_human Human No 7.7 IC50 = 21.1 nM Funct
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
411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1
CHEMBL594548 5ht6r_human Human No 7.7 IC50 = 21.6 nM Funct
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1
CHEMBL606815 5ht6r_human Human No 7.7 IC50 = 21.6 nM Funct
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
437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12
CHEMBL2393245 5ht6r_human Human No 7.7 IC50 = 21.8 nM Bind
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
364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL3040361 5ht6r_human Human No 7.7 IC50 = 21.8 nM Bind
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
364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL3398392 5ht6r_human Human No 5.7 IC50 = 2120 nM Funct
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
413 6 0 7 3.0 Cc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1
CHEMBL236579 5ht6r_human Human No 6.7 IC50 = 213 nM Funct
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
359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1
CHEMBL1173434 5ht6r_human Human Yes 5.7 IC50 = 2170 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12
CHEMBL1172 5ht6r_human Human Yes 5.7 IC50 = 2171 nM Bind
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)
310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1
CHEMBL1222028 5ht6r_human Human No 5.7 IC50 = 2191 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
423 5 0 4 4.2 CC(C)N(c1ccccc1N1CCN(C)CC1)S(=O)(=O)c1ccc2ccccc2c1
CHEMBL305660 5ht6r_human Human Yes 5.7 IC50 = 2197.4 nM Bind
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)
469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1
CHEMBL493 5ht6r_human Human Yes 7.7 IC50 = 22 nM Bind
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)
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
CHEMBL3113349 5ht6r_human Human No 7.7 IC50 = 22 nM Bind
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
349 3 1 6 2.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(F)cc1
CHEMBL3675195 5ht6r_human Human No 7.7 IC50 = 22 nM Funct
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.
349 4 2 7 1.5 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccc(F)cc1
CHEMBL2393244 5ht6r_human Human No 7.7 IC50 = 22.2 nM Bind
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
348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL3040288 5ht6r_human Human No 7.7 IC50 = 22.2 nM Bind
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
348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL1172727 5ht6r_human Human No 6.7 IC50 = 220 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
441 5 1 9 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1
CHEMBL3670284 5ht6r_human Human No 5.7 IC50 = 2200 nM Funct
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.
319 3 0 6 2.6 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(C)c1
CHEMBL1173577 5ht6r_human Human Yes 6.7 IC50 = 221 nM Bind
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
493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2
CHEMBL1169725 5ht6r_human Human Yes 5.7 IC50 = 2210 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
465 6 1 9 4.1 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1
CHEMBL1172724 5ht6r_human Human No 5.7 IC50 = 2260 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
483 4 1 8 5.5 Cc1cc(Cl)cc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1
CHEMBL1949765 5ht6r_human Human No 6.6 IC50 = 227 nM Funct
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
329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1
CHEMBL1962396 5ht6r_human Human No 6.6 IC50 = 227 nM Funct
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
329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1
CHEMBL603049 5ht6r_human Human Yes 5.6 IC50 = 2270 nM Funct
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
322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1
CHEMBL3675192 5ht6r_human Human Yes 5.6 IC50 = 2277 nM Funct
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.
486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL326263 5ht6r_human Human No 5.6 IC50 = 2280 nM Bind
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1
CHEMBL1642873 5ht6r_human Human No 7.6 IC50 = 23 nM Funct
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
422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12
CHEMBL1739699 5ht6r_human Human No 7.6 IC50 = 23 nM Funct
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
422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12
CHEMBL236336 5ht6r_human Human No 7.6 IC50 = 23 nM Funct
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
419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1
CHEMBL185850 5ht6r_human Human No 7.6 IC50 = 23 nM Bind
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
358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12
CHEMBL3659970 5ht6r_human Human No 7.6 IC50 = 23.9 nM Bind
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.
408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3
CHEMBL1668573 5ht6r_human Human No 6.6 IC50 = 230 nM Bind
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1
CHEMBL2207388 5ht6r_human Human No 6.6 IC50 = 233.5 nM Funct
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
369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1
CHEMBL589150 5ht6r_human Human Yes 5.6 IC50 = 2350 nM Funct
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
338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1
CHEMBL1197521 5ht6r_human Human No 6.6 IC50 = 238 nM Funct
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
451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21
CHEMBL575270 5ht6r_human Human No 6.6 IC50 = 238 nM Funct
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
451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21
CHEMBL1171992 5ht6r_human Human No 5.6 IC50 = 2380 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12
CHEMBL1668589 5ht6r_human Human Yes 7.6 IC50 = 24 nM Funct
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.
322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1
CHEMBL179814 5ht6r_human Human No 7.6 IC50 = 24 nM Bind
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1
CHEMBL383373 5ht6r_human Human No 7.6 IC50 = 24.5 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12
CHEMBL605292 5ht6r_human Human No 5.6 IC50 = 2400 nM Funct
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
393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21
CHEMBL2414725 5ht6r_human Human No 5.6 IC50 = 2400 nM Funct
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
474 5 0 7 3.7 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(C)c(/C=N/N2CCN(C)CC2)c2ccccc21
CHEMBL643 5ht6r_human Human Yes 5.6 IC50 = 2429 nM Bind
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)
284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C
CHEMBL3964100 5ht6r_human Human No 5.6 IC50 = 2430 nM Funct
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
419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3ccccc23)nn1-c1ccccc1
CHEMBL3398396 5ht6r_human Human No 5.6 IC50 = 2440 nM Funct
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
463 7 0 8 3.4 COc1ccc(Cl)cc1S(=O)(=O)n1cc(/C=N/N=C/N(C)C)c2c([N+](=O)[O-])cccc21
CHEMBL1949772 5ht6r_human Human No 6.6 IC50 = 245 nM Funct
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
329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1
CHEMBL1962399 5ht6r_human Human No 6.6 IC50 = 245 nM Funct
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
329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1
CHEMBL1200710 5ht6r_human Human Yes 6.6 IC50 = 245 nM Bind
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)
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL415 5ht6r_human Human Yes 6.6 IC50 = 245 nM Bind
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)
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL459371 5ht6r_human Human No 6.6 IC50 = 248 nM Funct
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
421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1
CHEMBL1668572 5ht6r_human Human Yes 7.6 IC50 = 25 nM Bind
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1
CHEMBL370507 5ht6r_human Human No 7.6 IC50 = 25 nM Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1
CHEMBL1922634 5ht6r_human Human Yes 7.6 IC50 = 25.2 nM Funct
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.
363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1
CHEMBL606816 5ht6r_human Human No 7.6 IC50 = 25.8 nM Funct
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
453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12
CHEMBL1173208 5ht6r_human Human Yes 6.6 IC50 = 250 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
429 5 1 9 3.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)cc1
CHEMBL3113358 5ht6r_human Human No 6.6 IC50 = 250 nM Bind
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
347 3 1 6 1.4 C[S+]([O-])c1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL1170473 5ht6r_human Human Yes 5.6 IC50 = 2500 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
459 4 1 8 4.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12
CHEMBL1783607 5ht6r_human Human No 6.6 IC50 = 251 nM Funct
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
405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1
CHEMBL3398398 5ht6r_human Human No 5.6 IC50 = 2530 nM Funct
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
449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc3ccccc3c2)c2cccc([N+](=O)[O-])c12
CHEMBL4128926 5ht6r_human Human No 6.6 IC50 = 254 nM Bind
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
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
CHEMBL591568 5ht6r_human Human No 5.6 IC50 = 2580 nM Funct
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
290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1
CHEMBL392318 5ht6r_human Human No 7.6 IC50 = 26 nM Funct
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
423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1
CHEMBL393158 5ht6r_human Human No 7.6 IC50 = 26 nM Funct
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
369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1
CHEMBL520343 5ht6r_human Human No 7.6 IC50 = 26 nM Funct
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
408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1642116 5ht6r_human Human No 7.6 IC50 = 26 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1
CHEMBL1922636 5ht6r_human Human No 7.6 IC50 = 26 nM Funct
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.
373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL433461 5ht6r_human Human Yes 7.6 IC50 = 26.3 nM Bind
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N
CHEMBL599663 5ht6r_human Human No 7.6 IC50 = 26.7 nM Funct
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
420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12
CHEMBL484927 5ht6r_human Human No 6.6 IC50 = 260 nM Funct
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
450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1169708 5ht6r_human Human Yes 6.6 IC50 = 260 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
435 5 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2)c2sccc23)cc1
CHEMBL1170275 5ht6r_human Human No 6.6 IC50 = 260 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
403 7 1 9 2.6 COCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12
CHEMBL1173135 5ht6r_human Human Yes 6.6 IC50 = 260 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
422 5 1 9 3.2 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccnc1)c1sccc12
CHEMBL1099282 5ht6r_human Human Yes 4.6 IC50 = 26000 nM Funct
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
293 2 1 3 1.4 CN1CCc2[nH]c3ccc(S(=O)(=O)N(C)C)cc3c2C1
CHEMBL39 5ht6r_human Human Yes 6.6 IC50 = 262 nM Bind
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL497749 5ht6r_human Human No 5.6 IC50 = 2634 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1
CHEMBL728 5ht6r_human Human Yes 6.6 IC50 = 267 nM Bind
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)
373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2
CHEMBL83 5ht6r_human Human Yes 5.6 IC50 = 2679 nM Bind
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)
371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1
CHEMBL144265 5ht6r_human Human No 6.6 IC50 = 269 nM Bind
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL1642887 5ht6r_human Human No 7.6 IC50 = 27 nM Funct
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
424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1739614 5ht6r_human Human No 7.6 IC50 = 27 nM Funct
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
424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12
CHEMBL1949764 5ht6r_human Human No 7.6 IC50 = 27 nM Funct
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
349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21
CHEMBL1963097 5ht6r_human Human No 7.6 IC50 = 27 nM Funct
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
349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21
CHEMBL1222135 5ht6r_human Human No 7.6 IC50 = 27 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
423 5 0 4 4.2 CC(C)N(c1ccc(N2CCN(C)CC2)cc1)S(=O)(=O)c1ccc2ccccc2c1
CHEMBL1091206 5ht6r_human Human No 7.6 IC50 = 27 nM Funct
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.
345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3
CHEMBL39 5ht6r_human Human Yes 7.6 IC50 = 27.5 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1170681 5ht6r_human Human Yes 6.6 IC50 = 270 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
455 5 1 8 4.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12
CHEMBL564 5ht6r_human Human Yes 6.6 IC50 = 274 nM Bind
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)
284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C
CHEMBL605081 5ht6r_human Human Yes 6.6 IC50 = 276 nM Funct
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
318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1
CHEMBL1201203 5ht6r_human Human Yes 5.6 IC50 = 2788 nM Bind
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)
307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1
CHEMBL438151 5ht6r_human Human Yes 5.6 IC50 = 2788 nM Bind
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)
307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1
CHEMBL237594 5ht6r_human Human No 7.6 IC50 = 28 nM Funct
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
389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1
CHEMBL597002 5ht6r_human Human No 7.6 IC50 = 28 nM Funct
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
406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1
CHEMBL19215 5ht6r_human Human Yes 7.6 IC50 = 28 nM Bind
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)
403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C
CHEMBL1642118 5ht6r_human Human No 7.6 IC50 = 28 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
449 3 0 5 3.8 CC1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1
CHEMBL3113365 5ht6r_human Human No 7.6 IC50 = 28 nM Bind
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
365 3 1 6 3.0 CSc1nc2ccc(Cl)cn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL356781 5ht6r_human Human No 7.6 IC50 = 28 nM Bind
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
349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL1172794 5ht6r_human Human Yes 7.6 IC50 = 28.3 nM Bind
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
401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1
CHEMBL1170099 5ht6r_human Human Yes 6.6 IC50 = 280 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12)c1ccccc1
CHEMBL3286556 5ht6r_human Human Yes 6.6 IC50 = 280 nM Bind
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C
CHEMBL1097614 5ht6r_human Human Yes 4.6 IC50 = 28000 nM Funct
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
480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1
CHEMBL1199305 5ht6r_human Human Yes 4.6 IC50 = 28000 nM Funct
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
480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1
CHEMBL1949767 5ht6r_human Human No 6.6 IC50 = 281 nM Funct
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
345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1
CHEMBL1962397 5ht6r_human Human No 6.6 IC50 = 281 nM Funct
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
345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1
CHEMBL516 5ht6r_human Human Yes 6.6 IC50 = 281 nM Bind
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)
287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1
CHEMBL592514 5ht6r_human Human Yes 5.6 IC50 = 2810 nM Funct
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
370 2 0 2 5.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(C(F)(F)F)cc2)CCN(C)C1
CHEMBL493625 5ht6r_human Human No 5.6 IC50 = 2839 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
457 8 1 5 3.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1
CHEMBL1491 5ht6r_human Human Yes 5.5 IC50 = 2898 nM Bind
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)
408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
CHEMBL1172728 5ht6r_human Human Yes 7.5 IC50 = 29 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
449 5 1 9 3.4 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCC1CCCO1)c1sccc12
CHEMBL2376485 5ht6r_human Human No 7.5 IC50 = 29 nM Bind
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
367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1
CHEMBL1169706 5ht6r_human Human Yes 6.5 IC50 = 290 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
465 5 1 10 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12
CHEMBL1172403 5ht6r_human Human Yes 6.5 IC50 = 290 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
451 6 1 9 3.8 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12
CHEMBL2414713 5ht6r_human Human No 5.5 IC50 = 2900 nM Funct
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
476 5 0 6 4.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1
CHEMBL3675192 5ht6r_human Human Yes 6.5 IC50 = 291 nM Bind
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].
486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1642413 5ht6r_human Human No 6.5 IC50 = 292 nM Funct
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
373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1
CHEMBL568935 5ht6r_human Human No 6.5 IC50 = 295 nM Funct
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
421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C
CHEMBL604668 5ht6r_human Human Yes 5.5 IC50 = 2950 nM Funct
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
324 2 0 2 4.5 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(F)cc2)C1
CHEMBL3398397 5ht6r_human Human No 5.5 IC50 = 2960 nM Funct
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
449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2cccc3ccccc23)c2cccc([N+](=O)[O-])c12
CHEMBL1783956 5ht6r_human Human Yes 5.5 IC50 = 2980 nM Funct
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
309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1
CHEMBL1221452 5ht6r_human Human No 8.5 IC50 = 3 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
471 6 0 4 5.0 CN1CCN(c2cccc(N(Cc3ccccc3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1
CHEMBL1222134 5ht6r_human Human No 8.5 IC50 = 3 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1
CHEMBL1222364 5ht6r_human Human No 8.5 IC50 = 3 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
409 5 0 4 3.8 CCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1
CHEMBL1668586 5ht6r_human Human Yes 8.5 IC50 = 3 nM Funct
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.
302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1
CHEMBL1278092 5ht6r_human Human Yes 8.5 IC50 = 3.2 nM Funct
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
356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21
CHEMBL3780252 5ht6r_human Human No 8.5 IC50 = 3.2 nM Bind
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
483 7 1 5 3.7 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCN(C)CC1
CHEMBL23038 5ht6r_human Human Yes 8.5 IC50 = 3.2 nM Bind
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1
CHEMBL1732 5ht6r_human Human Yes 8.5 IC50 = 3.2 nM Bind
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)
583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL119443 5ht6r_human Human Yes 8.5 IC50 = 3.2 nM Bind
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)
325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C
CHEMBL3113559 5ht6r_human Human No 8.5 IC50 = 3.4 nM Bind
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
345 3 1 6 2.7 CSc1nc2c(C)cccn2c(=N)c1S(=O)(=O)c1ccccc1
CHEMBL1935590 5ht6r_human Human No 8.4 IC50 = 3.6 nM Funct
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
331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3
CHEMBL1172726 5ht6r_human Human Yes 8.4 IC50 = 3.6 nM Bind
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
427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12
CHEMBL3780744 5ht6r_human Human No 8.4 IC50 = 3.7 nM Bind
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
451 7 2 5 3.3 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCNCC1
CHEMBL1642865 5ht6r_human Human No 8.4 IC50 = 3.8 nM Funct
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
394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1739655 5ht6r_human Human No 8.4 IC50 = 3.8 nM Funct
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
394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL180066 5ht6r_human Human No 8.4 IC50 = 3.9 nM Funct
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
370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1
CHEMBL1642849 5ht6r_human Human No 7.5 IC50 = 30 nM Funct
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
380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL1739254 5ht6r_human Human No 7.5 IC50 = 30 nM Funct
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
380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1
CHEMBL194843 5ht6r_human Human Yes 7.5 IC50 = 30 nM Bind
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
260 2 2 1 3.8 CCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1
CHEMBL195759 5ht6r_human Human Yes 7.5 IC50 = 30 nM Bind
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
274 2 1 1 4.2 CCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1
CHEMBL2376483 5ht6r_human Human No 7.5 IC50 = 30 nM Bind
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
230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1
CHEMBL1668500 5ht6r_human Human Yes 7.5 IC50 = 30 nM Bind
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL2393246 5ht6r_human Human No 7.5 IC50 = 30.4 nM Bind
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
360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL3040325 5ht6r_human Human No 7.5 IC50 = 30.4 nM Bind
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
360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1
CHEMBL1169899 5ht6r_human Human Yes 6.5 IC50 = 300 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
463 6 0 8 4.5 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12
CHEMBL328816 5ht6r_human Human No 6.5 IC50 = 300 nM Funct
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12
CHEMBL194412 5ht6r_human Human Yes 6.5 IC50 = 300 nM Bind
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
258 3 2 2 3.2 CCc1[nH]c2ccc(OC)cc2c1C1CCNCC1
CHEMBL3670280 5ht6r_human Human Yes 6.5 IC50 = 300 nM Funct
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.
367 3 0 6 3.6 CSc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL439849 5ht6r_rat Rat Yes 5.5 IC50 = 3000 nM Bind
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2
CHEMBL3670286 5ht6r_human Human No 4.5 IC50 = 30100 nM Funct
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.
412 5 0 8 3.4 COc1cc(-c2ccccn2)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12
CHEMBL1949768 5ht6r_human Human No 6.5 IC50 = 306 nM Funct
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
373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1
CHEMBL1963025 5ht6r_human Human No 6.5 IC50 = 306 nM Funct
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
373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1
CHEMBL3675193 5ht6r_human Human Yes 6.5 IC50 = 306 nM Bind
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].
470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1123 5ht6r_human Human Yes 5.5 IC50 = 3065 nM Bind
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)
309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC
CHEMBL27 5ht6r_human Human Yes 5.5 IC50 = 3065 nM Bind
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)
259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C
CHEMBL1255739 5ht6r_human Human Yes 5.5 IC50 = 3091 nM Bind
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)
261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1
CHEMBL1411979 5ht6r_human Human Yes 5.5 IC50 = 3091 nM Bind
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)
261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1
CHEMBL3781820 5ht6r_human Human No 7.5 IC50 = 31 nM Bind
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
455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCNCC1
CHEMBL361572 5ht6r_human Human No 7.5 IC50 = 31 nM Funct
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
374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21
CHEMBL1922623 5ht6r_human Human Yes 7.5 IC50 = 31.0 nM Bind
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].
387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1
CHEMBL1172795 5ht6r_human Human No 7.5 IC50 = 31.7 nM Bind
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
456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12
CHEMBL2407553 5ht6r_human Human No 6.5 IC50 = 310 nM Funct
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
439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1CC1CCNCC1
CHEMBL2407554 5ht6r_human Human No 6.5 IC50 = 310 nM Funct
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
439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3ccc4ccccc4c3)c2CCN1CC1CCNCC1
CHEMBL1642412 5ht6r_human Human Yes 6.5 IC50 = 310 nM Funct
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
397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1
CHEMBL1642115 5ht6r_human Human No 6.5 IC50 = 311 nM Bind
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1
CHEMBL599263 5ht6r_human Human No 6.5 IC50 = 316 nM Funct
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
406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21
CHEMBL1935600 5ht6r_human Human No 7.5 IC50 = 32 nM Funct
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
387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3
CHEMBL1170892 5ht6r_human Human Yes 7.5 IC50 = 32 nM Funct
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1Cl)c1sccc12
CHEMBL1091919 5ht6r_human Human Yes 7.5 IC50 = 32 nM Funct
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.
373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3
CHEMBL328816 5ht6r_human Human No 6.5 IC50 = 320 nM Funct
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12
CHEMBL1628227 5ht6r_human Human Yes 6.5 IC50 = 320 nM Bind
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)
279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21
CHEMBL3648343 5ht6r_human Human Yes 6.5 IC50 = 320 nM Bind
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
377 5 0 7 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1
CHEMBL1642418 5ht6r_human Human No 6.5 IC50 = 322 nM Funct
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
467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1
CHEMBL1783967 5ht6r_human Human Yes 5.5 IC50 = 3240 nM Funct
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
309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1
CHEMBL296419 5ht6r_human Human Yes 5.5 IC50 = 3266 nM Bind
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)
458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2
CHEMBL2407540 5ht6r_human Human No 5.5 IC50 = 3280 nM Funct
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
450 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(C(F)(F)F)c4)n[nH]c3C2=O)cc1
CHEMBL1949763 5ht6r_human Human No 7.5 IC50 = 33 nM Funct
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
333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21
CHEMBL1962395 5ht6r_human Human No 7.5 IC50 = 33 nM Funct
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
333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21
CHEMBL598851 5ht6r_human Human No 7.5 IC50 = 33.7 nM Funct
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
390 3 2 5