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 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
424 6 2 6 4.1 CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=C(N=C4N3C=CS4)Cl
CHEMBL362628 5ht6r_human Human Yes 10.2 EC50 = 0.1 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
424 6 2 6 4.1 CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=C(N=C4N3C=CS4)Cl
CHEMBL362628 5ht6r_human Human Yes 10.2 EC50 = 0.1 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
424 6 2 6 4.1 CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=C(N=C4N3C=CS4)Cl
CHEMBL362628 5ht6r_human Human Yes 10.2 EC50 = 0.1 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
424 6 2 6 4.1 CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=C(N=C4N3C=CS4)Cl
CHEMBL175835 5ht6r_human Human Yes 9.5 EC50 = 0.3 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
428 6 2 4 4.7 CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=CC4=C(C=C3)C(=CC=C4)Cl
CHEMBL175835 5ht6r_human Human Yes 9.5 EC50 = 0.3 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
428 6 2 4 4.7 CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=CC4=C(C=C3)C(=CC=C4)Cl
CHEMBL175835 5ht6r_human Human Yes 9.5 EC50 = 0.3 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
428 6 2 4 4.7 CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=CC4=C(C=C3)C(=CC=C4)Cl
CHEMBL175835 5ht6r_human Human Yes 9.5 EC50 = 0.3 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
428 6 2 4 4.7 CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=CC4=C(C=C3)C(=CC=C4)Cl
CHEMBL477650 5ht6r_human Human No 9.5 EC50 = 0.3 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
413 6 1 5 4.0 CC1=C(C2=C(C1)C=CC(=C2)NS(=O)(=O)C3=CSC4=CC=CC=C43)CCN(C)C
CHEMBL515307 5ht6r_human Human No 9.5 EC50 = 0.3 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 1 6 4.3 CN(C)CCC1=CCC2=C1C=C(C=C2)NS(=O)(=O)C3=C(N=C4N3C=CS4)Cl
CHEMBL477650 5ht6r_human Human No 9.5 EC50 = 0.3 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
413 6 1 5 4.0 CC1=C(C2=C(C1)C=CC(=C2)NS(=O)(=O)C3=CSC4=CC=CC=C43)CCN(C)C
CHEMBL515307 5ht6r_human Human No 9.5 EC50 = 0.3 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 1 6 4.3 CN(C)CCC1=CCC2=C1C=C(C=C2)NS(=O)(=O)C3=C(N=C4N3C=CS4)Cl
CHEMBL2113386 5ht6r_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
495 6 3 4 3.5 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)CC4=CC=CC=C4I
CHEMBL2113386 5ht6r_human Human No 9.4 EC50 = 0.4 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 4 3.5 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)CC4=CC=CC=C4I
CHEMBL2113386 5ht6r_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
495 6 3 4 3.5 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)CC4=CC=CC=C4I
CHEMBL2113386 5ht6r_human Human No 9.4 EC50 = 0.4 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 4 3.5 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)CC4=CC=CC=C4I
CHEMBL609741 5ht6r_human Human No 9.1 EC50 = 0.8 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 6 2.7 CC1=C(C(=NO1)C)S(=O)(=O)NC2=CC3=C(C=C2)NC=C3CC4CCCN4C
CHEMBL609741 5ht6r_human Human No 9.1 EC50 = 0.8 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 6 2.7 CC1=C(C(=NO1)C)S(=O)(=O)NC2=CC3=C(C=C2)NC=C3CC4CCCN4C
CHEMBL476006 5ht6r_human Human No 9.1 EC50 = 0.9 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
437 6 1 6 4.2 CC1=C(C2=C(C1)C=CC(=C2)NS(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN(C)C
CHEMBL476006 5ht6r_human Human No 9.1 EC50 = 0.9 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
437 6 1 6 4.2 CC1=C(C2=C(C1)C=CC(=C2)NS(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN(C)C
CHEMBL606639 5ht6r_human Human No 9.0 EC50 = 1 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
390 5 3 4 3.6 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL606639 5ht6r_human Human No 9.0 EC50 = 1 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
390 5 3 4 3.6 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL609995 5ht6r_human Human No 9.0 EC50 = 1.1 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 5 3.5 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)F
CHEMBL606547 5ht6r_human Human No 9.0 EC50 = 1.1 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
404 5 2 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4Cl
CHEMBL609995 5ht6r_human Human No 9.0 EC50 = 1.1 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 5 3.5 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)F
CHEMBL606547 5ht6r_human Human No 9.0 EC50 = 1.1 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
404 5 2 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4Cl
CHEMBL609742 5ht6r_human Human No 8.9 EC50 = 1.3 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
390 5 3 4 3.6 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4Cl
CHEMBL610254 5ht6r_human Human No 8.9 EC50 = 1.3 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
384 5 2 4 3.8 CC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(C=C2)NC=C3CC4CCCN4C
CHEMBL609992 5ht6r_human Human No 8.9 EC50 = 1.3 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 5 3.5 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4F
CHEMBL609742 5ht6r_human Human No 8.9 EC50 = 1.3 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
390 5 3 4 3.6 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4Cl
CHEMBL610254 5ht6r_human Human No 8.9 EC50 = 1.3 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
384 5 2 4 3.8 CC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(C=C2)NC=C3CC4CCCN4C
CHEMBL609992 5ht6r_human Human No 8.9 EC50 = 1.3 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 5 3.5 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4F
CHEMBL609737 5ht6r_human Human No 8.9 EC50 = 1.4 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 4 3.0 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4
CHEMBL609737 5ht6r_human Human No 8.9 EC50 = 1.4 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 4 3.0 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4
CHEMBL606556 5ht6r_human Human No 8.8 EC50 = 1.6 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
404 5 2 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL606556 5ht6r_human Human No 8.8 EC50 = 1.6 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
404 5 2 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL196622 5ht6r_human Human No 7.0 EC50 = 102.8 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
439 4 0 4 5.1 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Br
CHEMBL196622 5ht6r_human Human No 7.0 EC50 = 102.8 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
439 4 0 4 5.1 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Br
CHEMBL235986 5ht6r_human Human No 7.0 EC50 = 108.5 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
335 4 1 3 3.2 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC(=CC=C3)Cl)CCN
CHEMBL235986 5ht6r_human Human No 7.0 EC50 = 108.5 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
335 4 1 3 3.2 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC(=CC=C3)Cl)CCN
CHEMBL584049 5ht6r_human Human No 7.0 EC50 = 110 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 7 1.9 C1=CC(=CC(=C1)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN)C(F)(F)F
CHEMBL584049 5ht6r_human Human No 7.0 EC50 = 110 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 7 1.9 C1=CC(=CC(=C1)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN)C(F)(F)F
CHEMBL1550957 5ht6r_human Human Yes 6.0 EC50 = 1100 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 2.2 CC1=C(C2=CC=CC=C2N1)C3=CCNCC3
CHEMBL565724 5ht6r_human Human No 6.9 EC50 = 120 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
410 5 0 6 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=C(N=C4N3C=CS4)Cl
CHEMBL565724 5ht6r_human Human No 6.9 EC50 = 120 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
410 5 0 6 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=C(N=C4N3C=CS4)Cl
CHEMBL1094370 5ht6r_human Human No 6.9 EC50 = 125 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
361 3 1 3 3.1 C1CNCC1N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL1094370 5ht6r_human Human No 6.9 EC50 = 125 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
361 3 1 3 3.1 C1CNCC1N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL26379 5ht6r_human Human Yes 6.9 EC50 = 130 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 1.5 C1CNCC=C1C2=CNC3=C2C=C(C=C3)C#N
CHEMBL475969 5ht6r_human Human No 7.9 EC50 = 14 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
407 6 1 4 4.2 CC1=C(C2=C(C1)C=CC(=C2)S(=O)(=O)NC3=CC=CC4=CC=CC=C43)CCN(C)C
CHEMBL475969 5ht6r_human Human No 7.9 EC50 = 14 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
407 6 1 4 4.2 CC1=C(C2=C(C1)C=CC(=C2)S(=O)(=O)NC3=CC=CC4=CC=CC=C43)CCN(C)C
CHEMBL235985 5ht6r_human Human No 6.8 EC50 = 148 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
379 4 1 3 3.2 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=CC=C3Br)CCN
CHEMBL235985 5ht6r_human Human No 6.8 EC50 = 148 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
379 4 1 3 3.2 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=CC=C3Br)CCN
CHEMBL584046 5ht6r_human Human No 7.8 EC50 = 15 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
364 5 0 4 2.7 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC(=CC=C3)Cl
CHEMBL584046 5ht6r_human Human No 7.8 EC50 = 15 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
364 5 0 4 2.7 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC(=CC=C3)Cl
CHEMBL565753 5ht6r_human Human No 6.8 EC50 = 154 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 5 2.0 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CS3
CHEMBL565753 5ht6r_human Human No 6.8 EC50 = 154 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 5 2.0 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CS3
CHEMBL193824 5ht6r_human Human No 6.8 EC50 = 159 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 3 3.0 C1CNCC(=C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL193824 5ht6r_human Human No 6.8 EC50 = 159 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 3 3.0 C1CNCC(=C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL236576 5ht6r_human Human No 5.8 EC50 = 1645 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 1.8 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(C=C4)F
CHEMBL236576 5ht6r_human Human No 5.8 EC50 = 1645 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 1.8 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(C=C4)F
CHEMBL585931 5ht6r_human Human No 6.8 EC50 = 166 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 1.2 C1=CC2=C(N=C1)N(C=C2S(=O)(=O)C3=CC=C(C=C3)F)CCN
CHEMBL585931 5ht6r_human Human No 6.8 EC50 = 166 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 1.2 C1=CC2=C(N=C1)N(C=C2S(=O)(=O)C3=CC=C(C=C3)F)CCN
CHEMBL236577 5ht6r_human Human No 5.8 EC50 = 1680 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
362 3 1 4 2.4 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL236577 5ht6r_human Human No 5.8 EC50 = 1680 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
362 3 1 4 2.4 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL393107 5ht6r_human Human No 6.8 EC50 = 172 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
402 4 0 5 3.5 CC(C)N1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL393107 5ht6r_human Human No 6.8 EC50 = 172 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
402 4 0 5 3.5 CC(C)N1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL238277 5ht6r_human Human No 6.8 EC50 = 174 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
335 4 1 3 3.2 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=C(C=C3)Cl)CCN
CHEMBL238277 5ht6r_human Human No 6.8 EC50 = 174 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
335 4 1 3 3.2 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=C(C=C3)Cl)CCN
CHEMBL188182 5ht6r_human Human Yes 6.8 EC50 = 178 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 3 1.8 C1=CC=C(C=C1)S(=O)(=O)C2=CN(C3=CC=CC=C32)CCN
CHEMBL188182 5ht6r_human Human Yes 6.8 EC50 = 178 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 3 1.8 C1=CC=C(C=C1)S(=O)(=O)C2=CN(C3=CC=CC=C32)CCN
CHEMBL565745 5ht6r_human Human No 7.8 EC50 = 18 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
336 4 1 4 1.7 C1=CC(=CC(=C1)Cl)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN
CHEMBL565745 5ht6r_human Human No 7.8 EC50 = 18 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
336 4 1 4 1.7 C1=CC(=CC(=C1)Cl)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN
CHEMBL606816 5ht6r_human Human No 6.8 EC50 = 180 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 8 4.6 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)OC(F)(F)F
CHEMBL606816 5ht6r_human Human No 6.8 EC50 = 180 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 8 4.6 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)OC(F)(F)F
CHEMBL236989 5ht6r_human Human No 6.7 EC50 = 181 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
341 4 1 4 3.5 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=C(S3)Cl)CCN
CHEMBL236989 5ht6r_human Human No 6.7 EC50 = 181 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
341 4 1 4 3.5 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=C(S3)Cl)CCN
CHEMBL394303 5ht6r_human Human Yes 6.7 EC50 = 191 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 3 2.9 CC1=CC=C(C=C1)S(=O)(=O)N2C=C(C3=CC=CC=C32)CCN
CHEMBL394303 5ht6r_human Human Yes 6.7 EC50 = 191 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 3 2.9 CC1=CC=C(C=C1)S(=O)(=O)N2C=C(C3=CC=CC=C32)CCN
CHEMBL606558 5ht6r_human Human No 8.7 EC50 = 2.2 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
400 6 2 5 3.4 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)OC
CHEMBL606558 5ht6r_human Human No 8.7 EC50 = 2.2 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
400 6 2 5 3.4 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)OC
CHEMBL609994 5ht6r_human Human No 8.6 EC50 = 2.7 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 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)I
CHEMBL2376482 5ht6r_human Human Yes 8.6 EC50 = 2.7 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
291 1 2 1 2.9 CC1=C(C2=C(N1)C=CC(=C2)Br)C3=CCNCC3
CHEMBL609994 5ht6r_human Human No 8.6 EC50 = 2.7 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 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)I
CHEMBL606548 5ht6r_human Human No 8.5 EC50 = 2.9 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 8 4.6 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)OC(F)(F)F
CHEMBL606548 5ht6r_human Human No 8.5 EC50 = 2.9 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 8 4.6 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)OC(F)(F)F
CHEMBL577687 5ht6r_human Human No 7.7 EC50 = 20 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 4 1.5 CC1=C(C2=C(N1CCN)N=CC=C2)S(=O)(=O)C3=CC=CC=C3
CHEMBL577687 5ht6r_human Human No 7.7 EC50 = 20 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 4 1.5 CC1=C(C2=C(N1CCN)N=CC=C2)S(=O)(=O)C3=CC=CC=C3
CHEMBL1081793 5ht6r_human Human No 6.7 EC50 = 203 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
417 5 0 5 3.7 CCN1CCCC(C1)N2C=C(C3=C2C=CC(=C3)OC)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1081793 5ht6r_human Human No 6.7 EC50 = 203 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
417 5 0 5 3.7 CCN1CCCC(C1)N2C=C(C3=C2C=CC(=C3)OC)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL399013 5ht6r_human Human No 5.7 EC50 = 2035 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 4 2.2 CN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC=C4
CHEMBL399013 5ht6r_human Human No 5.7 EC50 = 2035 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 4 2.2 CN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC=C4
CHEMBL2376485 5ht6r_human Human No 7.7 EC50 = 21 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 4 2.7 CC1=C(C2=C(N1)C=CC(=C2)NS(=O)(=O)C3=CC=CC=C3)C4=CCNCC4
CHEMBL393312 5ht6r_human Human No 6.6 EC50 = 231 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 2.3 CN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL393312 5ht6r_human Human No 6.6 EC50 = 231 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 2.3 CN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL371292 5ht6r_human Human Yes 7.6 EC50 = 24 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
340 3 1 3 3.3 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL568672 5ht6r_human Human No 7.6 EC50 = 24 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 1.2 C1=CC(=CC(=C1)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN)F
CHEMBL371292 5ht6r_human Human Yes 7.6 EC50 = 24 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 3 3.3 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL371292 5ht6r_human Human Yes 7.6 EC50 = 24 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
340 3 1 3 3.3 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL568672 5ht6r_human Human No 7.6 EC50 = 24 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 1.2 C1=CC(=CC(=C1)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN)F
CHEMBL371292 5ht6r_human Human Yes 7.6 EC50 = 24 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 3 3.3 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL236313 5ht6r_human Human No 7.6 EC50 = 25 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
438 3 1 7 2.7 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL578826 5ht6r_human Human No 7.6 EC50 = 25 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 4 2.0 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC=C3
CHEMBL578826 5ht6r_human Human No 7.6 EC50 = 25 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 4 2.0 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC=C3
CHEMBL236313 5ht6r_human Human No 7.6 EC50 = 25 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
438 3 1 7 2.7 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL578826 5ht6r_human Human No 7.6 EC50 = 25 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 4 2.0 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC=C3
CHEMBL578826 5ht6r_human Human No 7.6 EC50 = 25 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 4 2.0 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC=C3
CHEMBL371132 5ht6r_human Human No 6.6 EC50 = 269.5 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 3.1 C1CNCC(=C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL371132 5ht6r_human Human No 6.6 EC50 = 269.5 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 3.1 C1CNCC(=C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL576315 5ht6r_human Human No 7.6 EC50 = 27 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 4 1.1 C1=CC=C(C=C1)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN
CHEMBL576315 5ht6r_human Human No 7.6 EC50 = 27 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 4 1.1 C1=CC=C(C=C1)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN
CHEMBL236772 5ht6r_human Human No 6.6 EC50 = 273 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 7 3.0 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL236772 5ht6r_human Human No 6.6 EC50 = 273 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 7 3.0 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL400627 5ht6r_human Human No 6.6 EC50 = 278 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 1.8 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL400627 5ht6r_human Human No 6.6 EC50 = 278 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 1.8 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL565977 5ht6r_human Human No 7.6 EC50 = 28 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
398 5 0 4 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC(=CC(=C3)Cl)Cl
CHEMBL565977 5ht6r_human Human No 7.6 EC50 = 28 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
398 5 0 4 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC(=CC(=C3)Cl)Cl
CHEMBL391517 5ht6r_human Human No 6.5 EC50 = 297 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
410 3 1 4 3.3 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC(=C4)Cl)Cl
CHEMBL391517 5ht6r_human Human No 6.5 EC50 = 297 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
410 3 1 4 3.3 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC(=C4)Cl)Cl
CHEMBL457570 5ht6r_human Human No 8.5 EC50 = 3.2 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
407 6 1 4 4.2 CC1=C(C2=C(C1)C=CC(=C2)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3)CCN(C)C
CHEMBL606557 5ht6r_human Human No 8.5 EC50 = 3.2 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 7 4.3 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL457570 5ht6r_human Human No 8.5 EC50 = 3.2 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
407 6 1 4 4.2 CC1=C(C2=C(C1)C=CC(=C2)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3)CCN(C)C
CHEMBL606557 5ht6r_human Human No 8.5 EC50 = 3.2 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 7 4.3 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL393997 5ht6r_human Human No 7.5 EC50 = 30 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
376 3 1 4 2.7 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL579063 5ht6r_human Human No 7.5 EC50 = 30 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 2.1 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=C(C=C3)F
CHEMBL393997 5ht6r_human Human No 7.5 EC50 = 30 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
376 3 1 4 2.7 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL579063 5ht6r_human Human No 7.5 EC50 = 30 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 2.1 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=C(C=C3)F
CHEMBL393106 5ht6r_human Human No 6.5 EC50 = 306 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 2.7 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL393106 5ht6r_human Human No 6.5 EC50 = 306 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 2.7 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1081094 5ht6r_human Human Yes 7.5 EC50 = 31 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 3 3.7 CCN1CCCC(C1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL568249 5ht6r_human Human No 7.5 EC50 = 31 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
398 5 0 4 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=C(C=CC=C3Cl)Cl
CHEMBL1081094 5ht6r_human Human Yes 7.5 EC50 = 31 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 3 3.7 CCN1CCCC(C1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL568249 5ht6r_human Human No 7.5 EC50 = 31 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
398 5 0 4 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=C(C=CC=C3Cl)Cl
CHEMBL583389 5ht6r_human Human No 7.5 EC50 = 32 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
370 5 0 5 3.0 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=C(S3)Cl
CHEMBL583389 5ht6r_human Human No 7.5 EC50 = 32 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
370 5 0 5 3.0 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=C(S3)Cl
CHEMBL2376484 5ht6r_human Human No 7.5 EC50 = 32 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 7 2.9 CC1=C(C2=C(N1)C=CC(=C2)OS(=O)(=O)C(F)(F)F)C3=CCNCC3
CHEMBL2376487 5ht6r_human Human No 7.5 EC50 = 32 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 1 2 3 2.0 CC1=C(C2=C(N1)C=CC(=C2)[N+](=O)[O-])C3=CCNCC3
CHEMBL392746 5ht6r_human Human No 7.5 EC50 = 34 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
452 4 1 7 3.1 CCN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL392746 5ht6r_human Human No 7.5 EC50 = 34 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
452 4 1 7 3.1 CCN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL194568 5ht6r_human Human No 6.5 EC50 = 344.5 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 3.1 C1CNCC(=C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(C=C4)F
CHEMBL194568 5ht6r_human Human No 6.5 EC50 = 344.5 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 3.1 C1CNCC(=C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(C=C4)F
CHEMBL236404 5ht6r_human Human No 7.5 EC50 = 35 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
406 3 1 4 2.4 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Br
CHEMBL585098 5ht6r_human Human No 7.5 EC50 = 35 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
370 4 1 4 2.3 C1=CC2=C(N=C1)N(C=C2S(=O)(=O)C3=CC(=CC(=C3)Cl)Cl)CCN
CHEMBL236404 5ht6r_human Human No 7.5 EC50 = 35 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
406 3 1 4 2.4 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Br
CHEMBL585098 5ht6r_human Human No 7.5 EC50 = 35 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
370 4 1 4 2.3 C1=CC2=C(N=C1)N(C=C2S(=O)(=O)C3=CC(=CC(=C3)Cl)Cl)CCN
CHEMBL371292 5ht6r_human Human Yes 7.4 EC50 = 36 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 3 3.3 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL183203 5ht6r_human Human No 6.4 EC50 = 366 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 3 2.8 CN(C)CCN1C=C(C2=CC=CC=C21)S(=O)(=O)C3=CC=CC=C3
CHEMBL183203 5ht6r_human Human No 6.4 EC50 = 366 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 3 2.8 CN(C)CCN1C=C(C2=CC=CC=C21)S(=O)(=O)C3=CC=CC=C3
CHEMBL1082198 5ht6r_human Human No 7.4 EC50 = 38 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 5 2.7 C1CNCC1N2C=C(C3=C2C=CC(=C3)F)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1082198 5ht6r_human Human No 7.4 EC50 = 38 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 5 2.7 C1CNCC1N2C=C(C3=C2C=CC(=C3)F)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL235117 5ht6r_human Human No 7.4 EC50 = 38.7 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
424 3 0 4 3.8 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC(=C4)Cl)Cl
CHEMBL235117 5ht6r_human Human No 7.4 EC50 = 38.7 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
424 3 0 4 3.8 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC(=C4)Cl)Cl
CHEMBL1076684 5ht6r_human Human No 6.4 EC50 = 398 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 3.0 CN1CCC(C1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1076684 5ht6r_human Human No 6.4 EC50 = 398 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 3.0 CN1CCC(C1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL609993 5ht6r_human Human No 8.4 EC50 = 4.2 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 8 4.1 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)OC(F)(F)F
CHEMBL609993 5ht6r_human Human No 8.4 EC50 = 4.2 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 8 4.1 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)OC(F)(F)F
CHEMBL596199 5ht6r_human Human No 8.4 EC50 = 4.5 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
423 5 3 7 3.8 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)C(F)(F)F
CHEMBL609743 5ht6r_human Human No 8.4 EC50 = 4.5 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
390 5 3 4 3.6 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)Cl
CHEMBL606559 5ht6r_human Human No 8.4 EC50 = 4.5 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 7 4.3 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)C(F)(F)F
CHEMBL596199 5ht6r_human Human No 8.4 EC50 = 4.5 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
423 5 3 7 3.8 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)C(F)(F)F
CHEMBL609743 5ht6r_human Human No 8.4 EC50 = 4.5 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
390 5 3 4 3.6 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)Cl
CHEMBL606559 5ht6r_human Human No 8.4 EC50 = 4.5 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 7 4.3 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)C(F)(F)F
CHEMBL236976 5ht6r_human Human No 6.4 EC50 = 414 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 7 3.0 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(C=C4)C(F)(F)F
CHEMBL236976 5ht6r_human Human No 6.4 EC50 = 414 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 7 3.0 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(C=C4)C(F)(F)F
CHEMBL365751 5ht6r_human Human Yes 7.4 EC50 = 44.8 Funct
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
237 3 1 1 3.4 CC1=C(C2=C(N1)C=CC(=C2)Cl)CCN(C)C
CHEMBL365751 5ht6r_human Human Yes 7.4 EC50 = 44.8 Funct
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
237 3 1 1 3.4 CC1=C(C2=C(N1)C=CC(=C2)Cl)CCN(C)C
CHEMBL235070 5ht6r_human Human No 7.3 EC50 = 47 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 4 2.1 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC=C4
CHEMBL565730 5ht6r_human Human No 7.3 EC50 = 47 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 4 2.4 CC1=C(C2=C(N1CCN(C)C)N=CC=C2)S(=O)(=O)C3=CC=CC=C3
CHEMBL235070 5ht6r_human Human No 7.3 EC50 = 47 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 4 2.1 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC=C4
CHEMBL565730 5ht6r_human Human No 7.3 EC50 = 47 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 4 2.4 CC1=C(C2=C(N1CCN(C)C)N=CC=C2)S(=O)(=O)C3=CC=CC=C3
CHEMBL401018 5ht6r_human Human No 7.3 EC50 = 49 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 7 3.4 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL401018 5ht6r_human Human No 7.3 EC50 = 49 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 7 3.4 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL606705 5ht6r_human Human No 8.3 EC50 = 5.2 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 6 3.2 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=C(C=C(C=C4)F)F
CHEMBL606705 5ht6r_human Human No 8.3 EC50 = 5.2 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 6 3.2 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=C(C=C(C=C4)F)F
CHEMBL2376483 5ht6r_human Human Yes 8.3 EC50 = 5.3 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 2 2.3 CC1=C(C2=C(N1)C=CC(=C2)F)C3=CCNCC3
CHEMBL609991 5ht6r_human Human No 8.2 EC50 = 5.8 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 7 3.8 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL609991 5ht6r_human Human No 8.2 EC50 = 5.8 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 7 3.8 C1CC(NC1)CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL393830 5ht6r_human Human No 7.3 EC50 = 50 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
376 3 1 4 2.7 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC=C4Cl
CHEMBL392976 5ht6r_human Human No 7.3 EC50 = 50 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
410 4 0 5 3.9 CCN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL393830 5ht6r_human Human No 7.3 EC50 = 50 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
376 3 1 4 2.7 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC=C4Cl
CHEMBL392976 5ht6r_human Human No 7.3 EC50 = 50 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
410 4 0 5 3.9 CCN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL565552 5ht6r_human Human No 7.3 EC50 = 51 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 4 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC4=CC=CC=C43
CHEMBL363827 5ht6r_human Human No 7.3 EC50 = 51 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 3.1 C1CNCC(=C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4F
CHEMBL565552 5ht6r_human Human No 7.3 EC50 = 51 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 4 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC4=CC=CC=C43
CHEMBL363827 5ht6r_human Human No 7.3 EC50 = 51 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 3.1 C1CNCC(=C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4F
CHEMBL398809 5ht6r_human Human No 6.3 EC50 = 520 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 7 2.6 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL398809 5ht6r_human Human No 6.3 EC50 = 520 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 7 2.6 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL236990 5ht6r_human Human No 7.3 EC50 = 54 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
385 4 1 4 3.6 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=C(S3)Br)CCN
CHEMBL236990 5ht6r_human Human No 7.3 EC50 = 54 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
385 4 1 4 3.6 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=C(S3)Br)CCN
CHEMBL1081095 5ht6r_human Human No 7.3 EC50 = 56 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 2.9 C1CC(CNC1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1081095 5ht6r_human Human No 7.3 EC50 = 56 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 2.9 C1CC(CNC1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL371318 5ht6r_human Human No 7.2 EC50 = 58.5 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
381 3 1 4 4.3 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL371318 5ht6r_human Human No 7.2 EC50 = 58.5 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
381 3 1 4 4.3 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL1079977 5ht6r_human Human No 6.2 EC50 = 592 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 4 3.1 C1CC(CNC1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC5=C4N=CC=C5
CHEMBL1079977 5ht6r_human Human No 6.2 EC50 = 592 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 4 3.1 C1CC(CNC1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC5=C4N=CC=C5
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
381 4 1 5 3.8 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 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
381 4 1 5 3.8 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 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
381 4 1 5 3.8 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 Funct
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
381 4 1 5 3.8 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 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
381 4 1 5 3.8 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN
CHEMBL392760 5ht6r_human Human Yes 8.2 EC50 = 6.5 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
381 4 1 5 3.8 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN
CHEMBL2376486 5ht6r_human Human No 8.2 EC50 = 6.6 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 2.7 CC1=C(C2=C(N1)C=CC(=C2)SC)C3=CCNCC3
CHEMBL1076665 5ht6r_human Human Yes 7.2 EC50 = 60 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 3 2.5 C1CNCC1N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL235734 5ht6r_human Human No 7.2 EC50 = 60 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 3.0 CCN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1076665 5ht6r_human Human Yes 7.2 EC50 = 60 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 3 2.5 C1CNCC1N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL235734 5ht6r_human Human No 7.2 EC50 = 60 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 3.0 CCN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL585930 5ht6r_human Human No 7.2 EC50 = 63 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 4 2.3 C1=CC=C2C(=C1)C=CC=C2S(=O)(=O)C3=CN(C4=C3C=CC=N4)CCN
CHEMBL585930 5ht6r_human Human No 7.2 EC50 = 63 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 4 2.3 C1=CC=C2C(=C1)C=CC=C2S(=O)(=O)C3=CN(C4=C3C=CC=N4)CCN
CHEMBL236104 5ht6r_human Human No 7.2 EC50 = 66 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
424 3 2 7 2.3 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL363843 5ht6r_human Human No 7.2 EC50 = 66 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 5 3.5 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC(=C(C=C4)F)F
CHEMBL236104 5ht6r_human Human No 7.2 EC50 = 66 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
424 3 2 7 2.3 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL363843 5ht6r_human Human No 7.2 EC50 = 66 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 5 3.5 C1CC(CNC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC(=C(C=C4)F)F
CHEMBL391713 5ht6r_human Human No 7.2 EC50 = 67 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
438 4 0 4 4.2 CCN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC(=C4)Cl)Cl
CHEMBL392899 5ht6r_human Human No 7.2 EC50 = 67 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 2.2 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL391713 5ht6r_human Human No 7.2 EC50 = 67 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
438 4 0 4 4.2 CCN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC(=C4)Cl)Cl
CHEMBL392899 5ht6r_human Human No 7.2 EC50 = 67 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 2.2 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1080316 5ht6r_human Human No 7.2 EC50 = 68 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 2.6 C1CNCC1N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1080316 5ht6r_human Human No 7.2 EC50 = 68 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 2.6 C1CNCC1N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 Funct
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 2.1 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC(=C3)F
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 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 2.1 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC(=C3)F
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 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 2.1 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC(=C3)F
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 Funct
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 2.1 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC(=C3)F
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 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 2.1 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC(=C3)F
CHEMBL571858 5ht6r_human Human Yes 8.1 EC50 = 7.3 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 2.1 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=CC=CC(=C3)F
CHEMBL236812 5ht6r_human Human No 7.2 EC50 = 71 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
396 3 0 5 3.5 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL236812 5ht6r_human Human No 7.2 EC50 = 71 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
396 3 0 5 3.5 CN1CCCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL235306 5ht6r_human Human No 7.1 EC50 = 72 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
420 3 1 4 2.8 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Br
CHEMBL235306 5ht6r_human Human No 7.1 EC50 = 72 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
420 3 1 4 2.8 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Br
CHEMBL1081110 5ht6r_human Human No 7.1 EC50 = 73 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 2.9 COC1=CC2=C(C=C1)N(C=C2S(=O)(=O)C3=CC=CC(=C3)F)C4CCCNC4
CHEMBL363275 5ht6r_human Human Yes 7.1 EC50 = 73 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 3 2.5 C1=CC=C(C=C1)S(=O)(=O)N2C=C(C3=CC=CC=C32)CCN
CHEMBL1081110 5ht6r_human Human No 7.1 EC50 = 73 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 2.9 COC1=CC2=C(C=C1)N(C=C2S(=O)(=O)C3=CC=CC(=C3)F)C4CCCNC4
CHEMBL363275 5ht6r_human Human Yes 7.1 EC50 = 73 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 3 2.5 C1=CC=C(C=C1)S(=O)(=O)N2C=C(C3=CC=CC=C32)CCN
CHEMBL236103 5ht6r_human Human No 7.1 EC50 = 80 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
410 3 2 7 1.9 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL236103 5ht6r_human Human No 7.1 EC50 = 80 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
410 3 2 7 1.9 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL1076583 5ht6r_human Human Yes 7.1 EC50 = 82 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 3 2.8 C1CC(CNC1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL1076583 5ht6r_human Human Yes 7.1 EC50 = 82 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 3 2.8 C1CC(CNC1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL565731 5ht6r_human Human No 7.1 EC50 = 85 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 7 1.9 C1=CC=C(C(=C1)C(F)(F)F)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN
CHEMBL565731 5ht6r_human Human No 7.1 EC50 = 85 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 7 1.9 C1=CC=C(C(=C1)C(F)(F)F)S(=O)(=O)C2=CN(C3=C2C=CC=N3)CCN
CHEMBL197845 5ht6r_human Human No 7.1 EC50 = 89.5 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
391 4 1 4 2.8 CC1=NN(C(=C1)Cl)CS(=O)(=O)N2C=C(C3=CC=CC=C32)C4=CCCNC4
CHEMBL197845 5ht6r_human Human No 7.1 EC50 = 89.5 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
391 4 1 4 2.8 CC1=NN(C(=C1)Cl)CS(=O)(=O)N2C=C(C3=CC=CC=C32)C4=CCCNC4
CHEMBL236987 5ht6r_human Human No 7.0 EC50 = 91 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 4 1.9 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=C(C=C3)N)CCN
CHEMBL236987 5ht6r_human Human No 7.0 EC50 = 91 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 4 1.9 C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=CC=C(C=C3)N)CCN
CHEMBL235118 5ht6r_human Human No 7.0 EC50 = 98 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
382 3 1 5 3.1 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL235118 5ht6r_human Human No 7.0 EC50 = 98 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
382 3 1 5 3.1 C1CC(CNC1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL3781299 5ht6r_human Human No 9.8 IC50 = 0.2 Funct
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
518 7 1 6 4.7 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=C(C=C4)Br)OC
CHEMBL3781299 5ht6r_human Human No 9.8 IC50 = 0.2 Funct
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
518 7 1 6 4.7 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=C(C=C4)Br)OC
CHEMBL1922635 5ht6r_human Human No 9.6 IC50 = 0.2 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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].
380 4 2 6 2.3 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC(=CC=C3)Cl)C)CN
CHEMBL1922635 5ht6r_human Human No 9.6 IC50 = 0.2 Funct
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].
380 4 2 6 2.3 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC(=CC=C3)Cl)C)CN
CHEMBL3781323 5ht6r_human Human No 9.6 IC50 = 0.3 Funct
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
458 7 1 7 4.1 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=C(C=C4)F)OC
CHEMBL3781323 5ht6r_human Human No 9.6 IC50 = 0.3 Funct
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
458 7 1 7 4.1 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=C(C=C4)F)OC
CHEMBL1922614 5ht6r_human Human No 9.5 IC50 = 0.3 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 6 2.0 CC1=NC2=C(C(=NN2C(=C1)N)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1922614 5ht6r_human Human No 9.5 IC50 = 0.3 Funct
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 6 2.0 CC1=NC2=C(C(=NN2C(=C1)N)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL3780579 5ht6r_human Human No 9.5 IC50 = 0.3 Funct
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
547 7 1 6 5.6 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCN(CC2)C)C3=CC=CC4=C3C=C(C=C4)Br
CHEMBL3780579 5ht6r_human Human No 9.5 IC50 = 0.3 Funct
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
547 7 1 6 5.6 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCN(CC2)C)C3=CC=CC4=C3C=C(C=C4)Br
CHEMBL1668587 5ht6r_human Human No 9.5 IC50 = 0.3 Funct
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 6 2.1 CC1=NC2=C(C(=NN2C(=C1)COC)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1668587 5ht6r_human Human No 9.5 IC50 = 0.3 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 6 2.1 CC1=NC2=C(C(=NN2C(=C1)COC)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL181066 5ht6r_human Human No 9.4 IC50 = 0.4 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 5 2.3 COC1=CC2=C(C=C1)N(C=C2C3=CCNCC3)S(=O)(=O)C4=CC=C(C=C4)N
CHEMBL3781452 5ht6r_human Human No 9.3 IC50 = 0.5 Funct
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
458 7 1 7 4.1 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=C(C4=CC=CC=C34)F)OC
CHEMBL3781452 5ht6r_human Human No 9.3 IC50 = 0.5 Funct
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
458 7 1 7 4.1 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=C(C4=CC=CC=C34)F)OC
CHEMBL3779904 5ht6r_human Human No 9.3 IC50 = 0.5 Funct
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
470 8 1 7 4.0 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=C(C=C4)OC)OC
CHEMBL3779904 5ht6r_human Human No 9.3 IC50 = 0.5 Funct
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
470 8 1 7 4.0 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=C(C=C4)OC)OC
CHEMBL1922633 5ht6r_human Human No 9.3 IC50 = 0.6 Funct
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 6 1.6 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CN
CHEMBL1922633 5ht6r_human Human No 9.3 IC50 = 0.6 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 6 1.6 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CN
CHEMBL194307 5ht6r_human Human No 9.2 IC50 = 0.6 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 3 4.1 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL194307 5ht6r_human Human No 9.2 IC50 = 0.6 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 3 4.1 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL1922639 5ht6r_human Human No 9.2 IC50 = 0.6 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 6 2.1 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CCN
CHEMBL1922639 5ht6r_human Human No 9.2 IC50 = 0.6 Funct
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 6 2.1 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CCN
CHEMBL1922630 5ht6r_human Human No 9.2 IC50 = 0.7 Funct
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 6 2.1 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)N
CHEMBL1922630 5ht6r_human Human No 9.2 IC50 = 0.7 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 6 2.1 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)N
CHEMBL3780274 5ht6r_human Human No 9.2 IC50 = 0.7 Funct
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
444 7 2 7 3.6 COC1=C(C=C(C=C1)S(=O)(=O)NCCC2=CC=CC3=C2C=C(C=C3)F)N4CCNCC4
CHEMBL3780274 5ht6r_human Human No 9.2 IC50 = 0.7 Funct
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
444 7 2 7 3.6 COC1=C(C=C(C=C1)S(=O)(=O)NCCC2=CC=CC3=C2C=C(C=C3)F)N4CCNCC4
CHEMBL353389 5ht6r_human Human No 9.2 IC50 = 0.7 Funct
Inhibition against human 5-hydroxytryptamine 6 receptorInhibition against human 5-hydroxytryptamine 6 receptor
357 5 1 1 5.1 CN(C)CCCC1=C(NC2=CC=CC=C21)C3=CC(=CC=C3)Br
CHEMBL180221 5ht6r_human Human No 9.2 IC50 = 0.7 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 0 3 4.1 CN1CCC(=CC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4Cl
CHEMBL1668586 5ht6r_human Human No 9.1 IC50 = 0.7 Funct
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 5 2.4 CC1=CC=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1668586 5ht6r_human Human No 9.1 IC50 = 0.7 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 5 2.4 CC1=CC=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL609739 5ht6r_human Human No 9.1 IC50 = 0.8 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
448 5 2 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4Br
CHEMBL371886 5ht6r_human Human No 9.1 IC50 = 0.8 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
415 6 0 5 4.0 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC(=C(C=C4)OC)OC
CHEMBL609739 5ht6r_human Human No 9.1 IC50 = 0.8 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
448 5 2 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC=C4Br
CHEMBL371886 5ht6r_human Human No 9.1 IC50 = 0.8 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
415 6 0 5 4.0 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC(=C(C=C4)OC)OC
CHEMBL444015 5ht6r_human Human No 9.1 IC50 = 0.8 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 4 2.3 C1CNCC=C1C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(C=C4)N
CHEMBL2172186 5ht6r_human Human No 9.1 IC50 = 0.8 Funct
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 6 1.9 CNC1=NN2C3=C(CN(CC3)C)C=NC2=C1S(=O)(=O)C4=CC=CC=C4
CHEMBL1668588 5ht6r_human Human No 9.1 IC50 = 0.9 Funct
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 6 1.5 CC1=CC(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)CO
CHEMBL1668588 5ht6r_human Human No 9.1 IC50 = 0.9 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 6 1.5 CC1=CC(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)CO
CHEMBL3781179 5ht6r_human Human No 9.0 IC50 = 0.9 Funct
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
440 7 1 6 4.0 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=CC=CC=C43)OC
CHEMBL3781179 5ht6r_human Human No 9.0 IC50 = 0.9 Funct
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
440 7 1 6 4.0 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=CC=CC=C43)OC
CHEMBL1091919 5ht6r_human Human No 9.0 IC50 = 0.9 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 5 3.6 CC1=NC2=C(C(=NN2C3=C1CCCC3)SC)S(=O)(=O)C4=CC=CC=C4
CHEMBL1091919 5ht6r_human Human No 9.0 IC50 = 0.9 Funct
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 5 3.6 CC1=NC2=C(C(=NN2C3=C1CCCC3)SC)S(=O)(=O)C4=CC=CC=C4
CHEMBL1091206 5ht6r_human Human No 9.0 IC50 = 1.0 Funct
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 5 2.7 CSC1=NN2C3=C(CCC3)C=NC2=C1S(=O)(=O)C4=CC=CC=C4
CHEMBL3781801 5ht6r_human Human No 9.0 IC50 = 1 Funct
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
456 8 2 7 3.5 COC1=CC2=C(C=CC=C2CCNS(=O)(=O)C3=CC(=C(C=C3)OC)N4CCNCC4)C=C1
CHEMBL413525 5ht6r_human Human No 9.0 IC50 = 1 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
395 4 0 4 5.1 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL3781801 5ht6r_human Human No 9.0 IC50 = 1 Funct
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
456 8 2 7 3.5 COC1=CC2=C(C=CC=C2CCNS(=O)(=O)C3=CC(=C(C=C3)OC)N4CCNCC4)C=C1
CHEMBL413525 5ht6r_human Human No 9.0 IC50 = 1 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
395 4 0 4 5.1 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL3781263 5ht6r_human Human No 9.0 IC50 = 1.1 Funct
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
484 8 2 7 4.4 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCNCC2)C3=CC=CC4=C3C=C(C=C4)OC
CHEMBL610256 5ht6r_human Human No 9.0 IC50 = 1.1 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
474 5 2 5 5.8 CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC4=C(C=C3)NC=C4CC5CCCN5C
CHEMBL3781263 5ht6r_human Human No 9.0 IC50 = 1.1 Funct
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
484 8 2 7 4.4 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCNCC2)C3=CC=CC4=C3C=C(C=C4)OC
CHEMBL610256 5ht6r_human Human No 9.0 IC50 = 1.1 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
474 5 2 5 5.8 CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC4=C(C=C3)NC=C4CC5CCCN5C
CHEMBL1091207 5ht6r_human Human No 8.9 IC50 = 1.2 Funct
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 5 3.2 CSC1=NN2C3=C(CCCC3)C=NC2=C1S(=O)(=O)C4=CC=CC=C4
CHEMBL1091207 5ht6r_human Human No 8.9 IC50 = 1.2 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 5 3.2 CSC1=NN2C3=C(CCCC3)C=NC2=C1S(=O)(=O)C4=CC=CC=C4
CHEMBL3779974 5ht6r_human Human No 8.9 IC50 = 1.2 Funct
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
530 7 2 6 4.5 COC1=C(C=C(C=C1)S(=O)(=O)NCC2(CC2)C3=CC=CC4=C3C=C(C=C4)Br)N5CCNCC5
CHEMBL3779974 5ht6r_human Human No 8.9 IC50 = 1.2 Funct
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
530 7 2 6 4.5 COC1=C(C=C(C=C1)S(=O)(=O)NCC2(CC2)C3=CC=CC4=C3C=C(C=C4)Br)N5CCNCC5
CHEMBL3675189 5ht6r_human Human No 8.9 IC50 = 1.3 Funct
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].
431 8 1 7 3.7 CCOC(=O)CC1=C(N2C(=C(C(=N2)NC(C)C)S(=O)(=O)C3=CC=CC=C3)N=C1C)C
CHEMBL3675189 5ht6r_human Human No 8.9 IC50 = 1.3 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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].
431 8 1 7 3.7 CCOC(=O)CC1=C(N2C(=C(C(=N2)NC(C)C)S(=O)(=O)C3=CC=CC=C3)N=C1C)C
CHEMBL3780141 5ht6r_human Human No 8.9 IC50 = 1.3 Funct
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
454 7 2 6 4.4 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCNCC2)C3=CC=CC4=CC=CC=C43
CHEMBL3781239 5ht6r_human Human No 8.9 IC50 = 1.3 Funct
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
458 7 1 7 4.1 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=CC(=C4)F)OC
CHEMBL3780141 5ht6r_human Human No 8.9 IC50 = 1.3 Funct
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
454 7 2 6 4.4 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCNCC2)C3=CC=CC4=CC=CC=C43
CHEMBL3781239 5ht6r_human Human No 8.9 IC50 = 1.3 Funct
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
458 7 1 7 4.1 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=CC(=C4)F)OC
CHEMBL3113554 5ht6r_human Human No 8.9 IC50 = 1.3 Funct
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 5 1.9 CC1=CN2C(=NC(=C(C2=N)S(=O)(=O)C3=CC=CC=C3)SC)C=C1
CHEMBL178385 5ht6r_human Human No 8.9 IC50 = 1.3 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 2.8 C1CNCCC1C2=CN(C3=C2C=C(C=C3)F)S(=O)(=O)C4=CC=C(C=C4)N
CHEMBL1277918 5ht6r_human Human No 8.9 IC50 = 1.4 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
463 5 0 5 5.1 CC(C)CN1C2=C(C=C(C=C2)N3CCN(CC3)C)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL3780011 5ht6r_human Human No 8.9 IC50 = 1.4 Funct
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
498 8 1 7 4.8 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCN(CC2)C)C3=CC=CC4=C3C=C(C=C4)OC
CHEMBL1277918 5ht6r_human Human No 8.9 IC50 = 1.4 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
463 5 0 5 5.1 CC(C)CN1C2=C(C=C(C=C2)N3CCN(CC3)C)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL3780011 5ht6r_human Human No 8.9 IC50 = 1.4 Funct
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
498 8 1 7 4.8 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCN(CC2)C)C3=CC=CC4=C3C=C(C=C4)OC
CHEMBL2172193 5ht6r_human Human No 8.9 IC50 = 1.4 Funct
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 6 2.3 CC1=C2CN(CCC2=NC3=C(C(=NN13)NC)S(=O)(=O)C4=CC=CC=C4)C
CHEMBL1092241 5ht6r_human Human No 8.8 IC50 = 1.5 Funct
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 5 3.6 CC1=C2CCCCC2=NC3=C(C(=NN13)SC)S(=O)(=O)C4=CC=CC=C4
CHEMBL1092241 5ht6r_human Human No 8.8 IC50 = 1.5 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 5 3.6 CC1=C2CCCCC2=NC3=C(C(=NN13)SC)S(=O)(=O)C4=CC=CC=C4
CHEMBL2172187 5ht6r_human Human No 8.8 IC50 = 1.5 Funct
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 6 2.3 CC1=NC2=C(C(=NN2C3=C1CN(CC3)C)NC)S(=O)(=O)C4=CC=CC=C4
CHEMBL2172187 5ht6r_human Human No 8.8 IC50 = 1.5 Funct
BindingDB_Patents: 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.BindingDB_Patents: 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 6 2.3 CC1=NC2=C(C(=NN2C3=C1CN(CC3)C)NC)S(=O)(=O)C4=CC=CC=C4
CHEMBL1277565 5ht6r_human Human No 8.8 IC50 = 1.6 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
407 3 1 5 3.4 CN1C2=C(C=C(C=C2)N3CCNCC3)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL3781399 5ht6r_human Human No 8.8 IC50 = 1.6 Funct
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
444 7 2 7 3.6 COC1=C(C=C(C=C1)S(=O)(=O)NCCC2=CC=C(C3=CC=CC=C23)F)N4CCNCC4
CHEMBL610259 5ht6r_human Human No 8.8 IC50 = 1.6 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
448 5 2 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)Br
CHEMBL1277565 5ht6r_human Human No 8.8 IC50 = 1.6 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
407 3 1 5 3.4 CN1C2=C(C=C(C=C2)N3CCNCC3)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL3781399 5ht6r_human Human No 8.8 IC50 = 1.6 Funct
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
444 7 2 7 3.6 COC1=C(C=C(C=C1)S(=O)(=O)NCCC2=CC=C(C3=CC=CC=C23)F)N4CCNCC4
CHEMBL610259 5ht6r_human Human No 8.8 IC50 = 1.6 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
448 5 2 4 4.1 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=C(C=C4)Br
CHEMBL1909065 5ht6r_human Human No 8.8 IC50 = 1.7 Funct
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 17 3.9 CC1CC(C(OC1C2CC(C(O2)C3(CCC(O3)C4(CCC5(O4)CC(C(C(O5)C(C)C6C(C(C(C(O6)(CC(=O)O)O)C)OC)OC)C)O)C)C)OC7CC(C(C(O7)C)OC)OC)(C)O)C
CHEMBL1909065 5ht6r_human Human No 8.8 IC50 = 1.7 Funct
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 17 3.9 CC1CC(C(OC1C2CC(C(O2)C3(CCC(O3)C4(CCC5(O4)CC(C(C(O5)C(C)C6C(C(C(C(O6)(CC(=O)O)O)C)OC)OC)C)O)C)C)OC7CC(C(C(O7)C)OC)OC)(C)O)C
CHEMBL1277564 5ht6r_human Human No 8.8 IC50 = 1.7 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
421 3 0 5 3.9 CN1CCN(CC1)C2=CC3=C(C=C2)N(N=C3S(=O)(=O)C4=CC=CC5=CC=CC=C54)C
CHEMBL1277656 5ht6r_human Human No 8.8 IC50 = 1.7 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
435 4 0 5 4.2 CCN1C2=C(C=C(C=C2)N3CCN(CC3)C)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL3780861 5ht6r_human Human No 8.8 IC50 = 1.7 Funct
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
532 7 2 6 5.1 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCNCC2)C3=CC=CC4=C3C=C(C=C4)Br
CHEMBL1277564 5ht6r_human Human No 8.8 IC50 = 1.7 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
421 3 0 5 3.9 CN1CCN(CC1)C2=CC3=C(C=C2)N(N=C3S(=O)(=O)C4=CC=CC5=CC=CC=C54)C
CHEMBL1277656 5ht6r_human Human No 8.8 IC50 = 1.7 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
435 4 0 5 4.2 CCN1C2=C(C=C(C=C2)N3CCN(CC3)C)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL3780861 5ht6r_human Human No 8.8 IC50 = 1.7 Funct
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
532 7 2 6 5.1 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCNCC2)C3=CC=CC4=C3C=C(C=C4)Br
CHEMBL361180 5ht6r_human Human No 8.8 IC50 = 1.7 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 6 2.1 C1CNCC=C1C2=CN(C3=CC4=C(C=C32)OCO4)S(=O)(=O)C5=CC=C(C=C5)N
CHEMBL1277836 5ht6r_human Human No 8.7 IC50 = 1.8 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
449 4 0 5 4.6 CC(C)N1C2=C(C=C(C=C2)N3CCN(CC3)C)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1277751 5ht6r_human Human No 8.7 IC50 = 1.8 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
449 5 0 5 4.7 CCCN1C2=C(C=C(C=C2)N3CCN(CC3)C)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1277836 5ht6r_human Human No 8.8 IC50 = 1.8 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
449 4 0 5 4.6 CC(C)N1C2=C(C=C(C=C2)N3CCN(CC3)C)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1277751 5ht6r_human Human No 8.8 IC50 = 1.8 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
449 5 0 5 4.7 CCCN1C2=C(C=C(C=C2)N3CCN(CC3)C)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1277657 5ht6r_human Human No 8.7 IC50 = 1.9 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
421 4 1 5 3.7 CCN1C2=C(C=C(C=C2)N3CCNCC3)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1277657 5ht6r_human Human No 8.7 IC50 = 1.9 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
421 4 1 5 3.7 CCN1C2=C(C=C(C=C2)N3CCNCC3)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL392541 5ht6r_human Human No 8.0 IC50 = 10 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
438 4 1 7 2.8 CCN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL520129 5ht6r_human Human No 8.0 IC50 = 10 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
435 4 2 5 3.3 C1CC(CNC1)C(=O)NC2=CC3=C(C=C2)C=NN3S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL193351 5ht6r_human Human No 8.0 IC50 = 10 Funct
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
261 1 1 1 3.3 CC1=C(C2=C(N1)C=CC(=C2)Cl)C3=CCN(CC3)C
CHEMBL1922635 5ht6r_human Human No 8.0 IC50 = 10 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.
380 4 2 6 2.3 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC(=CC=C3)Cl)C)CN
CHEMBL392541 5ht6r_human Human No 8.0 IC50 = 10 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
438 4 1 7 2.8 CCN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=C(NC5N4C=CS5)Cl
CHEMBL520129 5ht6r_human Human No 8.0 IC50 = 10 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
435 4 2 5 3.3 C1CC(CNC1)C(=O)NC2=CC3=C(C=C2)C=NN3S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1922635 5ht6r_human Human No 8.0 IC50 = 10 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
380 4 2 6 2.3 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC(=CC=C3)Cl)C)CN
CHEMBL193351 5ht6r_human Human No 8.0 IC50 = 10 Funct
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
261 1 1 1 3.3 CC1=C(C2=C(N1)C=CC(=C2)Cl)C3=CCN(CC3)C
CHEMBL2376482 5ht6r_human Human Yes 8.0 IC50 = 10 Funct
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
291 1 2 1 2.9 CC1=C(C2=C(N1)C=CC(=C2)Br)C3=CCNCC3
CHEMBL2376487 5ht6r_human Human No 8.0 IC50 = 10 Funct
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 1 2 3 2.0 CC1=C(C2=C(N1)C=CC(=C2)[N+](=O)[O-])C3=CCNCC3
CHEMBL606817 5ht6r_human Human No 8.0 IC50 = 10.4 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
420 5 2 4 4.7 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL606817 5ht6r_human Human No 8.0 IC50 = 10.4 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
420 5 2 4 4.7 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL459989 5ht6r_human Human No 7.0 IC50 = 100 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 2.3 COC1=CC(=CC=C1)S(=O)(=O)C2=CC=CC3=C2N=C(O3)N4CCNCC4
CHEMBL195239 5ht6r_human Human Yes 7.0 IC50 = 100 Funct
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
275 2 2 1 3.6 CC(C)C1=C(C2=C(N1)C=CC(=C2)Cl)C3=CCNCC3
CHEMBL459989 5ht6r_human Human No 7.0 IC50 = 100 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 2.3 COC1=CC(=CC=C1)S(=O)(=O)C2=CC=CC3=C2N=C(O3)N4CCNCC4
CHEMBL195239 5ht6r_human Human Yes 7.0 IC50 = 100 Funct
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
275 2 2 1 3.6 CC(C)C1=C(C2=C(N1)C=CC(=C2)Cl)C3=CCNCC3
CHEMBL2376489 5ht6r_human Human No 7.0 IC50 = 100 Funct
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 3.0 CC1=C(C2=C(N1)C=CC(=C2)OC(C)C)C3=CCNCC3
CHEMBL2376493 5ht6r_human Human No 7.0 IC50 = 100 Funct
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
275 2 1 1 3.1 CCN1C(=C(C2=C1C=CC(=C2)Cl)C3=CCNCC3)C
CHEMBL1170463 5ht6r_human Human Yes 6.0 IC50 = 1000 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
478 5 1 7 5.7 CC1=C(C(=CC=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)C(C)C)C
CHEMBL591570 5ht6r_human Human Yes 6.0 IC50 = 1000 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 4.1 CN1CCC2=C(C1)C3=C(N2C=CC4=CC=CC=C4)C=CC(=C3)F
CHEMBL1170463 5ht6r_human Human Yes 6.0 IC50 = 1000 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
478 5 1 7 5.7 CC1=C(C(=CC=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)C(C)C)C
CHEMBL591570 5ht6r_human Human Yes 6.0 IC50 = 1000 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 4.1 CN1CCC2=C(C1)C3=C(N2C=CC4=CC=CC=C4)C=CC(=C3)F
CHEMBL2376491 5ht6r_human Human No 6.0 IC50 = 1000 Funct
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 3.8 CC1=C(C2=C(N1)C=CC(=C2)C3=CC=CC=C3)C4=CCNCC4
CHEMBL1278091 5ht6r_human Human No 7.0 IC50 = 101 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
391 3 1 5 3.2 CN1CCN(CC1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC=C4Cl
CHEMBL1668587 5ht6r_human Human No 7.0 IC50 = 101 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 6 2.1 CC1=NC2=C(C(=NN2C(=C1)COC)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1278091 5ht6r_human Human No 7.0 IC50 = 101 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
391 3 1 5 3.2 CN1CCN(CC1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC=C4Cl
CHEMBL1668587 5ht6r_human Human No 7.0 IC50 = 101 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 6 2.1 CC1=NC2=C(C(=NN2C(=C1)COC)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1783608 5ht6r_human Human No 7.0 IC50 = 102 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
406 3 1 4 4.2 CN1CCC(CC1)C2=C3C=C(C=CC3=NN2)S(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL1783608 5ht6r_human Human No 7.0 IC50 = 102 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
406 3 1 4 4.2 CN1CCC(CC1)C2=C3C=C(C=CC3=NN2)S(=O)(=O)C4=CC5=CC=CC=C5C=C4
CHEMBL3670291 5ht6r_human Human No 6.0 IC50 = 1037 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 6 2.6 CNC1=NN2C(=CC=NC2=C1S(=O)(=O)C3=CC=CC=C3)C4=CN=CC=C4
CHEMBL3670291 5ht6r_human Human No 6.0 IC50 = 1037 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 6 2.6 CNC1=NN2C(=CC=NC2=C1S(=O)(=O)C3=CC=CC=C3)C4=CN=CC=C4
CHEMBL1783957 5ht6r_human Human Yes 6.0 IC50 = 1040 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
370 3 0 2 3.5 CN1CCC2=C(C1)C3=C(N2CCC4=CC=CC=N4)C=CC(=C3)Br
CHEMBL1173281 5ht6r_human Human Yes 6.0 IC50 = 1040 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
436 3 0 8 2.7 C1COCCN1C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1783957 5ht6r_human Human Yes 6.0 IC50 = 1040 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
370 3 0 2 3.5 CN1CCC2=C(C1)C3=C(N2CCC4=CC=CC=N4)C=CC(=C3)Br
CHEMBL1173281 5ht6r_human Human Yes 6.0 IC50 = 1040 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
436 3 0 8 2.7 C1COCCN1C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL459988 5ht6r_human Human No 7.0 IC50 = 105 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 4.1 CN1CCN(CC1)C2=NC3=C(O2)C=CC=C3S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL459988 5ht6r_human Human No 7.0 IC50 = 105 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 4.1 CN1CCN(CC1)C2=NC3=C(O2)C=CC=C3S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1173570 5ht6r_human Human Yes 6.0 IC50 = 1050 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
464 7 1 7 5.1 CCC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCC5=CC=CC=C5
CHEMBL589389 5ht6r_human Human Yes 6.0 IC50 = 1050 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 2 3.8 CN1CCC2=C(C1)C3=C(N2CCC4=CC=CC=C4)C=CC(=C3)OC
CHEMBL1173570 5ht6r_human Human Yes 6.0 IC50 = 1050 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
464 7 1 7 5.1 CCC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCC5=CC=CC=C5
CHEMBL589389 5ht6r_human Human Yes 6.0 IC50 = 1050 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 2 3.8 CN1CCC2=C(C1)C3=C(N2CCC4=CC=CC=C4)C=CC(=C3)OC
CHEMBL1783963 5ht6r_human Human Yes 5.0 IC50 = 10690 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 3.2 CC1=NC=C(C=C1)CCN2C3=C(CN(CC3)C)C4=C2C=CC(=C4)F
CHEMBL1783963 5ht6r_human Human Yes 5.0 IC50 = 10690 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 3.2 CC1=NC=C(C=C1)CCN2C3=C(CN(CC3)C)C4=C2C=CC(=C4)F
CHEMBL1079976 5ht6r_human Human No 7.0 IC50 = 107 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
405 3 0 3 4.5 CN1CCCC(C1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1080380 5ht6r_human Human No 7.0 IC50 = 107 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 3 3.7 C1CNCC1N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1079976 5ht6r_human Human No 7.0 IC50 = 107 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
405 3 0 3 4.5 CN1CCCC(C1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1080380 5ht6r_human Human No 7.0 IC50 = 107 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 3 3.7 C1CNCC1N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL365753 5ht6r_human Human No 7.0 IC50 = 107.1 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
409 3 0 3 4.7 CN1CCC(C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC(=C(C=C4)Cl)Cl
CHEMBL365753 5ht6r_human Human No 7.0 IC50 = 107.1 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
409 3 0 3 4.7 CN1CCC(C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC(=C(C=C4)Cl)Cl
CHEMBL1170291 5ht6r_human Human Yes 6.0 IC50 = 1070 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
510 4 1 10 5.4 C1=CC(=CC(=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl)C(F)(F)F
CHEMBL1170291 5ht6r_human Human Yes 6.0 IC50 = 1070 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
510 4 1 10 5.4 C1=CC(=CC(=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl)C(F)(F)F
CHEMBL1783582 5ht6r_human Human No 7.0 IC50 = 108 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
398 4 1 4 4.1 CC(C)C1=CC=C(C=C1)S(=O)(=O)C2=CC3=C(NN=C3C=C2)C4CCN(CC4)C
CHEMBL1278180 5ht6r_human Human No 7.0 IC50 = 108 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
391 3 1 5 3.2 CN1CCN(CC1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=C(C=C4)Cl
CHEMBL1783582 5ht6r_human Human No 7.0 IC50 = 108 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
398 4 1 4 4.1 CC(C)C1=CC=C(C=C1)S(=O)(=O)C2=CC3=C(NN=C3C=C2)C4CCN(CC4)C
CHEMBL1278180 5ht6r_human Human No 7.0 IC50 = 108 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
391 3 1 5 3.2 CN1CCN(CC1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=C(C=C4)Cl
CHEMBL1173061 5ht6r_human Human Yes 6.0 IC50 = 1080 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
450 6 1 7 4.7 CC(CC1=CC=CC=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1173061 5ht6r_human Human Yes 6.0 IC50 = 1080 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
450 6 1 7 4.7 CC(CC1=CC=CC=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL91 5ht6r_human Human Yes 5.0 IC50 = 10887 Funct
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)
416 6 0 2 5.3 C1=CC(=C(C=C1Cl)Cl)COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl
CHEMBL808 5ht6r_human Human Yes 5.0 IC50 = 10899 Funct
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)
382 6 0 2 5.3 C1=CC(=CC=C1COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl)Cl
CHEMBL394233 5ht6r_human Human No 8.0 IC50 = 11 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
382 4 1 5 2.3 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)CC4=CC=C(S4)Cl
CHEMBL484345 5ht6r_human Human No 8.0 IC50 = 11 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 5 2.8 C1=CC=C2C(=C1)C=CC=C2S(=O)(=O)N3C4=C(C=N3)C(=CC=C4)NC(=O)CCN
CHEMBL42 5ht6r_human Human Yes 8.0 IC50 = 11 Funct
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)
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL3781948 5ht6r_human Human No 8.0 IC50 = 11 Funct
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
472 7 2 7 4.5 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCNCC2)C3=CC=CC4=C3C=CC(=C4)F
CHEMBL3781260 5ht6r_human Human No 8.0 IC50 = 11 Funct
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
470 8 1 7 4.0 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=CC=C4OC)OC
CHEMBL1642128 5ht6r_human Human No 8.0 IC50 = 11 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
464 3 0 6 4.1 CC1CC(=O)C2=C(C=C(C=C2N1S(=O)(=O)C3=CC4=CC=CC=C4C=C3)C)N5CCN(CC5)C
CHEMBL369910 5ht6r_human Human No 8.0 IC50 = 11 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
459 4 0 4 6.4 CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)N3C=C(C4=CC=CC=C43)CC5CCCN5C
CHEMBL394233 5ht6r_human Human No 8.0 IC50 = 11 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
382 4 1 5 2.3 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)CC4=CC=C(S4)Cl
CHEMBL484345 5ht6r_human Human No 8.0 IC50 = 11 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 5 2.8 C1=CC=C2C(=C1)C=CC=C2S(=O)(=O)N3C4=C(C=N3)C(=CC=C4)NC(=O)CCN
CHEMBL42 5ht6r_human Human Yes 8.0 IC50 = 11 Funct
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)
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL3781948 5ht6r_human Human No 8.0 IC50 = 11 Funct
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
472 7 2 7 4.5 CC(C)(CNS(=O)(=O)C1=CC(=C(C=C1)OC)N2CCNCC2)C3=CC=CC4=C3C=CC(=C4)F
CHEMBL3781260 5ht6r_human Human No 8.0 IC50 = 11 Funct
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
470 8 1 7 4.0 CN1CCN(CC1)C2=C(C=CC(=C2)S(=O)(=O)NCCC3=CC=CC4=C3C=CC=C4OC)OC
CHEMBL1642128 5ht6r_human Human No 8.0 IC50 = 11 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
464 3 0 6 4.1 CC1CC(=O)C2=C(C=C(C=C2N1S(=O)(=O)C3=CC4=CC=CC=C4C=C3)C)N5CCN(CC5)C
CHEMBL3113350 5ht6r_human Human No 8.0 IC50 = 11 Funct
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
366 3 1 5 2.6 CSC1=C(C(=N)N2C=CC=CC2=N1)S(=O)(=O)C3=CC=CC=C3Cl
CHEMBL369910 5ht6r_human Human No 8.0 IC50 = 11 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
459 4 0 4 6.4 CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)N3C=C(C4=CC=CC=C43)CC5CCCN5C
CHEMBL360234 5ht6r_human Human No 8.0 IC50 = 11.2 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
388 3 2 4 2.9 C1CNCC=C1C2=CN(C3=C2C=CC(=C3)Cl)S(=O)(=O)C4=CC=C(C=C4)N
CHEMBL1922630 5ht6r_human Human No 8.0 IC50 = 11.3 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 6 2.1 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)N
CHEMBL1922630 5ht6r_human Human No 8.0 IC50 = 11.3 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 6 2.1 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)N
CHEMBL1935594 5ht6r_human Human No 7.9 IC50 = 11.7 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 5 3.2 CC1(C2=C(CCN1)C3=C(O2)C=C(C=C3)S(=O)(=O)C4=CC=CC(=C4)F)C
CHEMBL1935594 5ht6r_human Human No 7.9 IC50 = 11.7 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 5 3.2 CC1(C2=C(CCN1)C3=C(O2)C=C(C=C3)S(=O)(=O)C4=CC=CC(=C4)F)C
CHEMBL1170672 5ht6r_human Human Yes 7.9 IC50 = 11.9 Funct
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 7 3.6 C1CCC(C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1170672 5ht6r_human Human Yes 7.9 IC50 = 11.9 Funct
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 7 3.6 C1CCC(C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1173362 5ht6r_human Human Yes 7.0 IC50 = 110 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
424 6 1 8 2.8 COCCNC1=NC2=C(N=NN2C3=C1SC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL1172726 5ht6r_human Human Yes 7.0 IC50 = 110 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
428 5 1 8 3.5 C1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC=CS5
CHEMBL196466 5ht6r_human Human No 7.0 IC50 = 110 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
453 5 1 6 4.4 CC1=C(SC(=N1)N)S(=O)(=O)N2C=C(C3=CC=CC=C32)C4CCN(C4)CC5=CC=CC=C5
CHEMBL366012 5ht6r_human Human No 7.0 IC50 = 110 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
501 5 0 4 6.0 C1CN(CC1C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Br)CC5=CC=CC=C5
CHEMBL1173362 5ht6r_human Human Yes 7.0 IC50 = 110 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
424 6 1 8 2.8 COCCNC1=NC2=C(N=NN2C3=C1SC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL1172726 5ht6r_human Human Yes 7.0 IC50 = 110 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
428 5 1 8 3.5 C1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC=CS5
CHEMBL196466 5ht6r_human Human No 7.0 IC50 = 110 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
453 5 1 6 4.4 CC1=C(SC(=N1)N)S(=O)(=O)N2C=C(C3=CC=CC=C32)C4CCN(C4)CC5=CC=CC=C5
CHEMBL366012 5ht6r_human Human No 7.0 IC50 = 110 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
501 5 0 4 6.0 C1CN(CC1C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Br)CC5=CC=CC=C5
CHEMBL1172791 5ht6r_human Human Yes 6.0 IC50 = 1100 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
478 6 0 7 5.1 CCN(CC1=CC=CC=C1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=C(C=CC(=C5)C)C
CHEMBL1172791 5ht6r_human Human Yes 6.0 IC50 = 1100 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
478 6 0 7 5.1 CCN(CC1=CC=CC=C1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=C(C=CC(=C5)C)C
CHEMBL1170464 5ht6r_human Human Yes 6.0 IC50 = 1110 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
478 5 1 7 5.7 CC1=C(C=C(C=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)C(C)C)C
CHEMBL1668502 5ht6r_human Human No 6.0 IC50 = 1110 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 5 2.4 CC1=CC=NC2=C(C(=NN12)SC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1170464 5ht6r_human Human Yes 6.0 IC50 = 1110 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
478 5 1 7 5.7 CC1=C(C=C(C=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)C(C)C)C
CHEMBL1668502 5ht6r_human Human No 6.0 IC50 = 1110 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 5 2.4 CC1=CC=NC2=C(C(=NN12)SC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1276926 5ht6r_human Human Yes 7.0 IC50 = 112 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 3.0 CC1=CC=C(C=C1)S(=O)(=O)C2=C3C=C(C=CC3=NN2)N4CCN(CC4)C
CHEMBL1909072 5ht6r_human Human Yes 7.0 IC50 = 112 Funct
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)
402 5 1 4 4.4 C1CN(CCC1C(=O)N)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL1668574 5ht6r_human Human Yes 7.0 IC50 = 112 Funct
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
351 3 0 6 2.9 CC1=CC(=NC2=C(C(=NN12)SC)S(=O)(=O)C3=CC=C(C=C3)F)C
CHEMBL434932 5ht6r_human Human No 7.0 IC50 = 112 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
439 4 0 4 5.1 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Br
CHEMBL1276926 5ht6r_human Human Yes 7.0 IC50 = 112 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 3.0 CC1=CC=C(C=C1)S(=O)(=O)C2=C3C=C(C=CC3=NN2)N4CCN(CC4)C
CHEMBL1668574 5ht6r_human Human Yes 7.0 IC50 = 112 Funct
BindingDB_Patents: Functional Assay. Functional assay using 5-HT6 receptors.BindingDB_Patents: Functional Assay. Functional assay using 5-HT6 receptors.
351 3 0 6 2.9 CC1=CC(=NC2=C(C(=NN12)SC)S(=O)(=O)C3=CC=C(C=C3)F)C
CHEMBL1909072 5ht6r_human Human Yes 7.0 IC50 = 112 Funct
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)
402 5 1 4 4.4 C1CN(CCC1C(=O)N)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL434932 5ht6r_human Human No 7.0 IC50 = 112 Funct
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
439 4 0 4 5.1 CN1CCCC1CC2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Br
CHEMBL1173206 5ht6r_human Human Yes 6.0 IC50 = 1120 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
448 3 0 7 4.4 CC1CCN(CC1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1173206 5ht6r_human Human Yes 6.0 IC50 = 1120 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
448 3 0 7 4.4 CC1CCN(CC1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL900 5ht6r_human Human Yes 6.0 IC50 = 1121 Funct
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 3.8 CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C
CHEMBL900 5ht6r_human Human Yes 6.0 IC50 = 1121 Funct
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 3.8 CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C
CHEMBL589149 5ht6r_human Human Yes 6.0 IC50 = 1130 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 3 4.0 CN1CCC2=C(C1)C3=C(N2CCC4=CC=C(C=C4)F)C=CC(=C3)F
CHEMBL589149 5ht6r_human Human Yes 6.0 IC50 = 1130 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 3 4.0 CN1CCC2=C(C1)C3=C(N2CCC4=CC=C(C=C4)F)C=CC(=C3)F
CHEMBL1170682 5ht6r_human Human Yes 5.9 IC50 = 1150 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
486 6 1 8 4.4 COC1=CC=CC=C1CNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Cl
CHEMBL1170686 5ht6r_human Human Yes 5.9 IC50 = 1150 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
472 5 1 8 4.5 COC1=CC=CC=C1NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Cl
CHEMBL1170682 5ht6r_human Human Yes 5.9 IC50 = 1150 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
486 6 1 8 4.4 COC1=CC=CC=C1CNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Cl
CHEMBL1170686 5ht6r_human Human Yes 5.9 IC50 = 1150 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
472 5 1 8 4.5 COC1=CC=CC=C1NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Cl
CHEMBL1170276 5ht6r_human Human Yes 5.9 IC50 = 1160 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
436 6 1 7 4.3 C1=CC=C(C=C1)CCNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL589390 5ht6r_human Human Yes 5.9 IC50 = 1160 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 2 3.5 CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)CCC4=CN=C(C=C4)C
CHEMBL1170276 5ht6r_human Human Yes 5.9 IC50 = 1160 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
436 6 1 7 4.3 C1=CC=C(C=C1)CCNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL589390 5ht6r_human Human Yes 5.9 IC50 = 1160 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 2 3.5 CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)CCC4=CN=C(C=C4)C
CHEMBL460194 5ht6r_human Human No 6.9 IC50 = 117 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
412 3 1 6 3.6 C1CN(CCN1)C2=NC3=C(O2)C=CC=C3S(=O)(=O)C4=C(C=CC(=C4)Cl)Cl
CHEMBL460194 5ht6r_human Human No 6.9 IC50 = 117 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
412 3 1 6 3.6 C1CN(CCN1)C2=NC3=C(O2)C=CC=C3S(=O)(=O)C4=C(C=CC(=C4)Cl)Cl
CHEMBL1172597 5ht6r_human Human Yes 5.9 IC50 = 1170 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 7 4.5 C1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC=C(C=C5)Cl
CHEMBL1172597 5ht6r_human Human Yes 5.9 IC50 = 1170 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 7 4.5 C1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC=C(C=C5)Cl
CHEMBL1762569 5ht6r_human Human No 5.9 IC50 = 1177 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 5 2.4 CC1=CC(=NC2=C(C(=NN12)N(C)C)S(=O)(=O)C3=CC=CC=C3)C
CHEMBL1762569 5ht6r_human Human No 5.9 IC50 = 1177 Funct
BindingDB_Patents: 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.BindingDB_Patents: 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 5 2.4 CC1=CC(=NC2=C(C(=NN12)N(C)C)S(=O)(=O)C3=CC=CC=C3)C
CHEMBL1222137 5ht6r_human Human No 5.9 IC50 = 1180 Funct
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 3 5.3 CC(C)N(C1=CC(=CC=C1)I)S(=O)(=O)C2=CC3=CC=CC=C3C=C2
CHEMBL1222137 5ht6r_human Human No 5.9 IC50 = 1180 Funct
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 3 5.3 CC(C)N(C1=CC(=CC=C1)I)S(=O)(=O)C2=CC3=CC=CC=C3C=C2
CHEMBL1171632 5ht6r_human Human Yes 5.9 IC50 = 1190 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
470 5 0 7 4.6 CN(CC1=CC=CC=C1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Cl
CHEMBL1171632 5ht6r_human Human Yes 5.9 IC50 = 1190 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
470 5 0 7 4.6 CN(CC1=CC=CC=C1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Cl
CHEMBL1922619 5ht6r_human Human No 7.9 IC50 = 12 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 6 2.8 CC1=NC2=C(C(=NN2C(=C1)N(C)C)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1922614 5ht6r_human Human No 7.9 IC50 = 12 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 6 2.0 CC1=NC2=C(C(=NN2C(=C1)N)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL3670293 5ht6r_human Human No 7.9 IC50 = 12 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 7 2.9 CNC1=NN2C(=CC(=NC2=C1S(=O)(=O)C3=CC=CC=C3)C4=CN=CC=C4)OC
CHEMBL1922619 5ht6r_human Human No 7.9 IC50 = 12 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 6 2.8 CC1=NC2=C(C(=NN2C(=C1)N(C)C)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1922614 5ht6r_human Human No 7.9 IC50 = 12 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 6 2.0 CC1=NC2=C(C(=NN2C(=C1)N)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL3670293 5ht6r_human Human No 7.9 IC50 = 12 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 7 2.9 CNC1=NN2C(=CC(=NC2=C1S(=O)(=O)C3=CC=CC=C3)C4=CN=CC=C4)OC
CHEMBL3113360 5ht6r_human Human No 7.9 IC50 = 12 Funct
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 5 1.8 CCOC1=C(C(=N)N2C=CC=CC2=N1)S(=O)(=O)C3=CC=CC=C3
CHEMBL3113561 5ht6r_human Human No 7.9 IC50 = 12 Funct
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
424 3 1 5 2.7 CC1=CC(=CN2C1=NC(=C(C2=N)S(=O)(=O)C3=CC=CC=C3)SC)Br
CHEMBL598229 5ht6r_human Human No 7.9 IC50 = 12.5 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 3.3 C1CN(CC1N)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL598229 5ht6r_human Human No 7.9 IC50 = 12.5 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 3.3 C1CN(CC1N)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL236541 5ht6r_human Human No 6.9 IC50 = 120 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
390 4 0 4 3.2 CCN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL459348 5ht6r_human Human No 6.9 IC50 = 120 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 9 3.2 C1CN(CCN1)C2=NC3=C(O2)C=CC=C3S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL1169724 5ht6r_human Human No 6.9 IC50 = 120 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
470 5 1 7 4.8 CC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC(=CC=C5)Cl
CHEMBL236541 5ht6r_human Human No 6.9 IC50 = 120 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
390 4 0 4 3.2 CCN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL459348 5ht6r_human Human No 6.9 IC50 = 120 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 9 3.2 C1CN(CCN1)C2=NC3=C(O2)C=CC=C3S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL1169724 5ht6r_human Human No 6.9 IC50 = 120 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
470 5 1 7 4.8 CC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC(=CC=C5)Cl
CHEMBL3113355 5ht6r_human Human No 6.9 IC50 = 120 Funct
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 5 2.0 CN=C1C(=C(N=C2N1C=CC=C2)SC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1173433 5ht6r_human Human Yes 5.9 IC50 = 1200 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
408 4 1 7 3.8 CC(C)NC1=NC2=C(N=NN2C3=C1SC=C3)S(=O)(=O)C4=CC=C(C=C4)Cl
CHEMBL1173433 5ht6r_human Human Yes 5.9 IC50 = 1200 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
408 4 1 7 3.8 CC(C)NC1=NC2=C(N=NN2C3=C1SC=C3)S(=O)(=O)C4=CC=C(C=C4)Cl
CHEMBL1170472 5ht6r_human Human Yes 5.9 IC50 = 1210 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 4 1 7 4.9 CC1=CC=C(C=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1170472 5ht6r_human Human Yes 5.9 IC50 = 1210 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 4 1 7 4.9 CC1=CC=C(C=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1171486 5ht6r_human Human Yes 5.9 IC50 = 1220 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
478 7 1 7 5.4 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCCC5=CC=CC=C5
CHEMBL1173508 5ht6r_human Human No 5.9 IC50 = 1220 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 7 2.4 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)N
CHEMBL1173005 5ht6r_human Human Yes 5.9 IC50 = 1220 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 0 7 3.8 CCN(CC)C1=NC2=C(N=NN2C3=C1SC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL1171486 5ht6r_human Human Yes 5.9 IC50 = 1220 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
478 7 1 7 5.4 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCCC5=CC=CC=C5
CHEMBL1173508 5ht6r_human Human No 5.9 IC50 = 1220 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 7 2.4 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)N
CHEMBL1173005 5ht6r_human Human Yes 5.9 IC50 = 1220 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 0 7 3.8 CCN(CC)C1=NC2=C(N=NN2C3=C1SC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL194786 5ht6r_human Human No 6.9 IC50 = 123 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 0 3 5.3 CC1=CC=C(C=C1)S(=O)(=O)N2C=C(C3=CC=CC=C32)C4CCN(C4)CC5=CC=CC=C5
CHEMBL194786 5ht6r_human Human No 6.9 IC50 = 123 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 0 3 5.3 CC1=CC=C(C=C1)S(=O)(=O)N2C=C(C3=CC=CC=C32)C4CCN(C4)CC5=CC=CC=C5
CHEMBL1172795 5ht6r_human Human No 5.9 IC50 = 1250 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
457 5 1 8 3.4 C1=CC(=CC(=C1)Cl)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CN=CC=C5
CHEMBL1169898 5ht6r_human Human Yes 5.9 IC50 = 1250 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
480 5 1 9 4.0 CC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC6=C(C=C5)OCO6
CHEMBL1172795 5ht6r_human Human No 5.9 IC50 = 1250 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
457 5 1 8 3.4 C1=CC(=CC(=C1)Cl)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CN=CC=C5
CHEMBL1169898 5ht6r_human Human Yes 5.9 IC50 = 1250 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
480 5 1 9 4.0 CC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC6=C(C=C5)OCO6
CHEMBL104 5ht6r_human Human Yes 4.9 IC50 = 12543 Funct
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)
345 4 0 1 5.0 C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4
CHEMBL104 5ht6r_human Human Yes 4.9 IC50 = 12543 Funct
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)
345 4 0 1 5.0 C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4
CHEMBL144265 5ht6r_human Human No 6.9 IC50 = 126 Funct
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
424 3 1 5 2.8 CC1=CN2C(=N)C(=C(N=C2C(=C1)Br)SC)S(=O)(=O)C3=CC=CC=C3
CHEMBL411 5ht6r_human Human Yes 4.9 IC50 = 12892 Funct
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 5.1 CCC(=C(CC)C1=CC=C(C=C1)O)C2=CC=C(C=C2)O
CHEMBL411 5ht6r_human Human Yes 4.9 IC50 = 12892 Funct
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 5.1 CCC(=C(CC)C1=CC=C(C=C1)O)C2=CC=C(C=C2)O
CHEMBL1641610 5ht6r_human Human No 6.9 IC50 = 129 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
400 3 0 6 2.4 CC1=CC=C(C=C1)S(=O)(=O)N2CCC(=O)C3=C(C=CC=C32)N4CCN(CC4)C
CHEMBL1641610 5ht6r_human Human No 6.9 IC50 = 129 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
400 3 0 6 2.4 CC1=CC=C(C=C1)S(=O)(=O)N2CCC(=O)C3=C(C=CC=C32)N4CCN(CC4)C
CHEMBL1172868 5ht6r_human Human Yes 5.9 IC50 = 1290 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
432 7 1 8 3.3 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCCOC
CHEMBL1172868 5ht6r_human Human Yes 5.9 IC50 = 1290 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
432 7 1 8 3.3 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCCOC
CHEMBL1277105 5ht6r_human Human Yes 7.9 IC50 = 13 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 3.4 C1CN(CCN1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL2172182 5ht6r_human Human No 7.9 IC50 = 13 Funct
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 5 1.4 CC1=NN2C3=C(CN(CC3)C)C=NC2=C1S(=O)(=O)C4=CC=CC=C4
CHEMBL715 5ht6r_human Human Yes 7.9 IC50 = 13 Funct
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 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL1221497 5ht6r_human Human No 7.9 IC50 = 13 Funct
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 5 3.6 CN1CCN(CC1)C2=CC(=CC=C2)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3
CHEMBL1277105 5ht6r_human Human Yes 7.9 IC50 = 13 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 3.4 C1CN(CCN1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL715 5ht6r_human Human Yes 7.9 IC50 = 13 Funct
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 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL1221497 5ht6r_human Human No 7.9 IC50 = 13 Funct
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 5 3.6 CN1CCN(CC1)C2=CC(=CC=C2)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3
CHEMBL444878 5ht6r_human Human No 7.9 IC50 = 13.8 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 3 3.4 CN1CCC(=CC1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4
CHEMBL394232 5ht6r_human Human No 6.9 IC50 = 132 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 2.7 CCN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1277999 5ht6r_human Human No 6.9 IC50 = 132 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 6 2.7 CN1CCN(CC1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL394232 5ht6r_human Human No 6.9 IC50 = 132 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 2.7 CCN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1277999 5ht6r_human Human No 6.9 IC50 = 132 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 6 2.7 CN1CCN(CC1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1173284 5ht6r_human Human Yes 5.9 IC50 = 1330 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
464 5 0 7 4.7 CC1=C(C=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)N(C)CC5=CC=CC=C5)C
CHEMBL1173284 5ht6r_human Human Yes 5.9 IC50 = 1330 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
464 5 0 7 4.7 CC1=C(C=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)N(C)CC5=CC=CC=C5)C
CHEMBL62193 5ht6r_human Human Yes 5.9 IC50 = 1339 Funct
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 8 1.6 COC1=NC(=NC(=C1)NS(=O)(=O)C2=CC=C(C=C2)N)OC
CHEMBL1173774 5ht6r_human Human No 5.9 IC50 = 1340 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 3 0 7 3.4 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)C5CCN(CC5)C
CHEMBL1173774 5ht6r_human Human No 5.9 IC50 = 1340 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 3 0 7 3.4 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)C5CCN(CC5)C
CHEMBL236405 5ht6r_human Human No 6.9 IC50 = 135 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
406 3 1 4 2.4 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(C=C4)Br
CHEMBL367088 5ht6r_human Human No 6.9 IC50 = 135 Funct
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
450 6 1 6 4.2 C1CCN(C1)CCN2C=CC3=C2C=CC(=C3)NS(=O)(=O)C4=C(N=C5N4C=CS5)Cl
CHEMBL236405 5ht6r_human Human No 6.9 IC50 = 135 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
406 3 1 4 2.4 C1CNCC1N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC=C(C=C4)Br
CHEMBL367088 5ht6r_human Human No 6.9 IC50 = 135 Funct
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
450 6 1 6 4.2 C1CCN(C1)CCN2C=CC3=C2C=CC(=C3)NS(=O)(=O)C4=C(N=C5N4C=CS5)Cl
CHEMBL2207386 5ht6r_human Human Yes 6.9 IC50 = 135.1 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
448 4 0 4 3.6 CN1CCN(CC1)CC2=C3C=CN(C3=CC=C2)S(=O)(=O)C4=CC=CC=C4Br
CHEMBL1170689 5ht6r_human Human Yes 5.9 IC50 = 1350 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
514 4 1 7 5.3 CC1=C(C=C(C=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Br)C
CHEMBL1170689 5ht6r_human Human Yes 5.9 IC50 = 1350 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
514 4 1 7 5.3 CC1=C(C=C(C=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Br)C
CHEMBL116735 5ht6r_human Human No 5.9 IC50 = 1350 Funct
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
481 9 0 5 5.8 C1CN(CCN1CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)CCC4=CC=C(C=C4)F
CHEMBL1172595 5ht6r_human Human Yes 5.9 IC50 = 1370 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
452 6 1 8 3.8 COC1=CC=CC(=C1)CNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1172595 5ht6r_human Human Yes 5.9 IC50 = 1370 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
452 6 1 8 3.8 COC1=CC=CC(=C1)CNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1170274 5ht6r_human Human Yes 5.9 IC50 = 1380 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
450 5 1 7 5.1 CCC1=CC(=CC=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)C
CHEMBL1170274 5ht6r_human Human Yes 5.9 IC50 = 1380 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
450 5 1 7 5.1 CCC1=CC(=CC=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)C
CHEMBL606765 5ht6r_human Human No 7.9 IC50 = 14.1 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 7 4.3 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL606765 5ht6r_human Human No 7.9 IC50 = 14.1 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 7 4.3 CN1CCCC1CC2=CNC3=C2C=C(C=C3)NS(=O)(=O)C4=CC=CC(=C4)C(F)(F)F
CHEMBL178234 5ht6r_human Human No 7.9 IC50 = 14.1 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
379 3 1 4 3.9 C1CNCC=C1C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(S4)Cl
CHEMBL281937 5ht6r_human Human Yes 7.8 IC50 = 14.8 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 1 3.8 CN1CCC(=CC1)C2=CN(C3=CC=CC=C32)CC4=CC=CC=C4
CHEMBL1172404 5ht6r_human Human Yes 6.9 IC50 = 140 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
462 4 1 7 5.3 C1CCCC(CC1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1170672 5ht6r_human Human Yes 6.9 IC50 = 140 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 7 3.6 C1CCC(C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1172404 5ht6r_human Human Yes 6.9 IC50 = 140 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
462 4 1 7 5.3 C1CCCC(CC1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1170672 5ht6r_human Human Yes 6.9 IC50 = 140 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 7 3.6 C1CCC(C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL3398395 5ht6r_human Human No 5.9 IC50 = 1400 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 7 0 8 2.7 CN(C)C=NN=CC1=CN(C2=C1C(=CC=C2)[N+](=O)[O-])S(=O)(=O)C3=C(C=CC(=C3)OC)OC
CHEMBL2414704 5ht6r_human Human No 5.9 IC50 = 1400 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
552 6 0 6 6.3 CN1CCN(CC1)N=CC2=C(N(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC5=C4C=CC=C5N(C)C)C6=CC=CC=C6
CHEMBL3398395 5ht6r_human Human No 5.9 IC50 = 1400 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 7 0 8 2.7 CN(C)C=NN=CC1=CN(C2=C1C(=CC=C2)[N+](=O)[O-])S(=O)(=O)C3=C(C=CC(=C3)OC)OC
CHEMBL1670 5ht6r_human Human Yes 5.9 IC50 = 1402 Funct
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)
320 3 0 0 6.2 C1=CC=C(C(=C1)C(C2=CC=C(C=C2)Cl)C(Cl)Cl)Cl
CHEMBL1086626 5ht6r_human Human No 5.9 IC50 = 1412 Funct
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
471 7 2 3 5.3 CC1=C(C=C(N1)C2=CC=CC=C2)C(=O)NCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL1086626 5ht6r_human Human No 5.9 IC50 = 1412 Funct
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
471 7 2 3 5.3 CC1=C(C=C(N1)C2=CC=CC=C2)C(=O)NCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL236335 5ht6r_human Human No 6.9 IC50 = 142 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
376 3 0 4 2.8 CN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL236335 5ht6r_human Human No 6.9 IC50 = 142 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
376 3 0 4 2.8 CN1CCC(C1)N2C=C(C3=C2N=CC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL1172723 5ht6r_human Human Yes 5.8 IC50 = 1430 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
470 4 1 7 5.2 CC1=C(C=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC5=CC=C(C=C5)Cl)C
CHEMBL1172723 5ht6r_human Human Yes 5.9 IC50 = 1430 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
470 4 1 7 5.2 CC1=C(C=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC5=CC=C(C=C5)Cl)C
CHEMBL589386 5ht6r_human Human Yes 5.8 IC50 = 1440 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 4.5 CC1=CC=C(C=C1)C=CN2C3=C(CN(CC3)C)C4=C2C=CC(=C4)F
CHEMBL589386 5ht6r_human Human Yes 5.8 IC50 = 1440 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 4.5 CC1=CC=C(C=C1)C=CN2C3=C(CN(CC3)C)C4=C2C=CC(=C4)F
CHEMBL1762570 5ht6r_human Human Yes 6.8 IC50 = 147 Funct
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
301 2 0 4 2.3 CC1=CC(=NC2=C(C(=NN12)C)S(=O)(=O)C3=CC=CC=C3)C
CHEMBL1172790 5ht6r_human Human Yes 5.8 IC50 = 1480 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
464 5 0 7 4.7 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)N(C)CC5=CC=CC=C5
CHEMBL1172790 5ht6r_human Human Yes 5.8 IC50 = 1480 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
464 5 0 7 4.7 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)N(C)CC5=CC=CC=C5
CHEMBL1170439 5ht6r_human Human Yes 5.8 IC50 = 1490 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 8 2.6 CC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCOC
CHEMBL1170439 5ht6r_human Human Yes 5.8 IC50 = 1490 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 8 2.6 CC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCOC
CHEMBL3260795 5ht6r_human Human No 7.8 IC50 = 15 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 2.5 C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)N4CC(CC4=O)C5=CC=CC=C5
CHEMBL568673 5ht6r_human Human No 7.8 IC50 = 15 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
398 5 0 4 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=C(C=CC(=C3)Cl)Cl
CHEMBL1642127 5ht6r_human Human No 7.8 IC50 = 15 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
464 3 0 6 4.1 CC1CC(=O)C2=C(N1S(=O)(=O)C3=CC4=CC=CC=C4C=C3)C=CC(=C2N5CCN(CC5)C)C
CHEMBL3260795 5ht6r_human Human No 7.8 IC50 = 15 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 2.5 C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)N4CC(CC4=O)C5=CC=CC=C5
CHEMBL568673 5ht6r_human Human No 7.8 IC50 = 15 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
398 5 0 4 3.3 CN(C)CCN1C=C(C2=C1N=CC=C2)S(=O)(=O)C3=C(C=CC(=C3)Cl)Cl
CHEMBL1642127 5ht6r_human Human No 7.8 IC50 = 15 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
464 3 0 6 4.1 CC1CC(=O)C2=C(N1S(=O)(=O)C3=CC4=CC=CC=C4C=C3)C=CC(=C2N5CCN(CC5)C)C
CHEMBL3675190 5ht6r_human Human No 7.8 IC50 = 15.3 Funct
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 6 2.2 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CC(=O)N(C)C
CHEMBL3675190 5ht6r_human Human No 7.8 IC50 = 15.3 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 6 2.2 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CC(=O)N(C)C
CHEMBL194590 5ht6r_human Human No 7.8 IC50 = 15.5 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 4 2.8 CN1CCC(C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(C=C4)N
CHEMBL194590 5ht6r_human Human No 7.8 IC50 = 15.5 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 4 2.8 CN1CCC(C1)C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=CC=C(C=C4)N
CHEMBL604102 5ht6r_human Human No 7.8 IC50 = 15.7 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 3.3 C1CN(CC1N)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL604102 5ht6r_human Human No 7.8 IC50 = 15.7 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 3.3 C1CN(CC1N)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1170679 5ht6r_human Human Yes 6.8 IC50 = 150 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
470 5 1 7 4.9 CC(C1=CC=CC=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1172793 5ht6r_human Human Yes 6.8 IC50 = 150 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
462 5 1 8 4.2 C1=CC(=CC(=C1)Cl)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC=CS5
CHEMBL1173777 5ht6r_human Human Yes 6.8 IC50 = 150 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
438 7 1 8 3.2 COCCCNC1=NC2=C(N=NN2C3=C1SC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL1170679 5ht6r_human Human Yes 6.8 IC50 = 150 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
470 5 1 7 4.9 CC(C1=CC=CC=C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1172793 5ht6r_human Human Yes 6.8 IC50 = 150 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
462 5 1 8 4.2 C1=CC(=CC(=C1)Cl)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC=CS5
CHEMBL1173777 5ht6r_human Human Yes 6.8 IC50 = 150 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
438 7 1 8 3.2 COCCCNC1=NC2=C(N=NN2C3=C1SC=C3)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL592516 5ht6r_human Human Yes 5.8 IC50 = 1500 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 4.1 CN1CCC2=C(C1)C3=C(N2C=CC4=CC=C(C=C4)OC)C=CC(=C3)F
CHEMBL592516 5ht6r_human Human Yes 5.8 IC50 = 1500 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 4.1 CN1CCC2=C(C1)C3=C(N2C=CC4=CC=C(C=C4)OC)C=CC(=C3)F
CHEMBL1173706 5ht6r_human Human Yes 5.8 IC50 = 1520 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
428 3 0 7 4.0 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)N5CCCCC5
CHEMBL1173706 5ht6r_human Human Yes 5.8 IC50 = 1520 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
428 3 0 7 4.0 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)N5CCCCC5
CHEMBL954 5ht6r_human Human Yes 5.8 IC50 = 1522 Funct
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 9 0 2 7.2 CCN(CC)CCOC1=CC=C(C=C1)C(=C(C2=CC=CC=C2)Cl)C3=CC=CC=C3
CHEMBL954 5ht6r_human Human Yes 5.8 IC50 = 1522 Funct
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 9 0 2 7.2 CCN(CC)CCOC1=CC=C(C=C1)C(=C(C2=CC=CC=C2)Cl)C3=CC=CC=C3
CHEMBL1642419 5ht6r_human Human No 5.8 IC50 = 1528 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
452 3 0 5 4.0 CN1CCN(CC1)C2=CN(C3=C2C=C(C=C3)Br)S(=O)(=O)C4=CC=C(C=C4)F
CHEMBL1642419 5ht6r_human Human No 5.8 IC50 = 1528 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
452 3 0 5 4.0 CN1CCN(CC1)C2=CN(C3=C2C=C(C=C3)Br)S(=O)(=O)C4=CC=C(C=C4)F
CHEMBL325516 5ht6r_human Human No 5.8 IC50 = 1530 Funct
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
497 10 0 6 6.3 C1CN(CCN1CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)OCCC4=CC=C(C=C4)F
CHEMBL1173207 5ht6r_human Human Yes 5.8 IC50 = 1540 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
448 3 0 7 4.3 C1CCCN(CC1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1173207 5ht6r_human Human Yes 5.8 IC50 = 1540 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
448 3 0 7 4.3 C1CCCN(CC1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1922620 5ht6r_human Human Yes 5.8 IC50 = 1549 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 7 2.7 CC1=NC2=C(C(=NN2C(=C1)NCCN(C)C)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1922620 5ht6r_human Human Yes 5.8 IC50 = 1549 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 7 2.7 CC1=NC2=C(C(=NN2C(=C1)NCCN(C)C)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1668582 5ht6r_human Human No 6.8 IC50 = 156 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.
372 3 0 6 3.1 CC1=CC=NC2=C(C(=NN12)SC)S(=O)(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL1668582 5ht6r_human Human No 6.8 IC50 = 156 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
372 3 0 6 3.1 CC1=CC=NC2=C(C(=NN12)SC)S(=O)(=O)C3=CC(=C(C=C3)F)Cl
CHEMBL599466 5ht6r_human Human No 6.8 IC50 = 157 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
435 4 1 5 4.0 CC(C)N1C2=C(C=C(C=C2)N3CCC(C3)N)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL599466 5ht6r_human Human No 6.8 IC50 = 157 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
435 4 1 5 4.0 CC(C)N1C2=C(C=C(C=C2)N3CCC(C3)N)C(=N1)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1171092 5ht6r_human Human Yes 5.8 IC50 = 1570 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
418 6 1 8 2.9 CC1=C(C=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCOC)C
CHEMBL1171092 5ht6r_human Human Yes 5.8 IC50 = 1570 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
418 6 1 8 2.9 CC1=C(C=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCCOC)C
CHEMBL1783953 5ht6r_human Human Yes 4.8 IC50 = 15750 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 2 2.8 CN1CCC2=C(C1)C3=CC=CC=C3N2CCC4=CC=CC=N4
CHEMBL1783953 5ht6r_human Human Yes 4.8 IC50 = 15750 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 2 2.8 CN1CCC2=C(C1)C3=CC=CC=C3N2CCC4=CC=CC=N4
CHEMBL592752 5ht6r_human Human Yes 6.8 IC50 = 158 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 1 4.2 CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)CCC4=CC=CC=C4
CHEMBL592752 5ht6r_human Human Yes 6.8 IC50 = 158 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 1 4.2 CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)CCC4=CC=CC=C4
CHEMBL575310 5ht6r_human Human No 5.8 IC50 = 1580 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
435 4 1 6 4.2 CN1CCC(C1)C2=CCC3=C2C=C(C=C3)NS(=O)(=O)C4=C(N=C5N4C=CS5)Cl
CHEMBL575310 5ht6r_human Human No 5.8 IC50 = 1580 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
435 4 1 6 4.2 CN1CCC(C1)C2=CCC3=C2C=C(C=C3)NS(=O)(=O)C4=C(N=C5N4C=CS5)Cl
CHEMBL1783958 5ht6r_human Human Yes 5.8 IC50 = 1590 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 5 3.6 CN1CCC2=C(C1)C3=C(N2CCC4=CC=CC=N4)C=CC(=C3)C(F)(F)F
CHEMBL1783958 5ht6r_human Human Yes 5.8 IC50 = 1590 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 5 3.6 CN1CCC2=C(C1)C3=C(N2CCC4=CC=CC=N4)C=CC(=C3)C(F)(F)F
CHEMBL1403281 5ht6r_human Human Yes 7.8 IC50 = 16 Funct
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)
576 5 3 6 2.7 CC(C)CC1C(=O)N2CCCC2C3(N1C(=O)C(O3)(C(C)C)NC(=O)C4CN(C5CC6=CNC7=CC=CC(=C67)C5=C4)C)O
CHEMBL3780270 5ht6r_human Human No 7.8 IC50 = 16 Funct
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
470 7 2 7 3.9 COC1=C(C=C(C=C1)S(=O)(=O)NCC2(CC2)C3=CC=CC4=C3C=CC(=C4)F)N5CCNCC5
CHEMBL1222234 5ht6r_human Human No 7.8 IC50 = 16 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
424 5 0 5 4.6 CC(C)N(C1=CC=CC(=C1)N2CCN(CC2)C)S(=O)(=O)C3=CC=CC4=CC=CC=C43
CHEMBL1668585 5ht6r_human Human No 7.8 IC50 = 16 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 5 2.4 CC1=NC2=C(C(=NN2C=C1)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL21343 5ht6r_human Human Yes 7.8 IC50 = 16 Funct
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
309 3 2 2 2.5 CCN(CC)C(=O)C1CNC2CC3=CNC4=CC=CC(=C34)C2=C1
CHEMBL292759 5ht6r_human Human Yes 7.8 IC50 = 16 Funct
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
440 5 1 6 3.0 CN1CCN(CC1)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)Br)OC
CHEMBL1668585 5ht6r_human Human No 7.8 IC50 = 16 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 5 2.4 CC1=NC2=C(C(=NN2C=C1)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1403281 5ht6r_human Human Yes 7.8 IC50 = 16 Funct
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)
576 5 3 6 2.7 CC(C)CC1C(=O)N2CCCC2C3(N1C(=O)C(O3)(C(C)C)NC(=O)C4CN(C5CC6=CNC7=CC=CC(=C67)C5=C4)C)O
CHEMBL3780270 5ht6r_human Human No 7.8 IC50 = 16 Funct
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
470 7 2 7 3.9 COC1=C(C=C(C=C1)S(=O)(=O)NCC2(CC2)C3=CC=CC4=C3C=CC(=C4)F)N5CCNCC5
CHEMBL1222234 5ht6r_human Human No 7.8 IC50 = 16 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
424 5 0 5 4.6 CC(C)N(C1=CC=CC(=C1)N2CCN(CC2)C)S(=O)(=O)C3=CC=CC4=CC=CC=C43
CHEMBL21343 5ht6r_human Human Yes 7.8 IC50 = 16 Funct
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
309 3 2 2 2.5 CCN(CC)C(=O)C1CNC2CC3=CNC4=CC=CC(=C34)C2=C1
CHEMBL292759 5ht6r_human Human Yes 7.8 IC50 = 16 Funct
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
440 5 1 6 3.0 CN1CCN(CC1)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)Br)OC
CHEMBL598443 5ht6r_human Human No 7.8 IC50 = 16.5 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 3.0 C1C(CN1C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54)N
CHEMBL598443 5ht6r_human Human No 7.8 IC50 = 16.5 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 3.0 C1C(CN1C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54)N
CHEMBL3659969 5ht6r_human Human No 7.8 IC50 = 16.6 Funct
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 6 1.8 CC1=NC2=C(C(=NN2C3=C1CNCC3)SC)S(=O)(=O)C4=CC=CC=C4
CHEMBL3659969 5ht6r_human Human No 7.8 IC50 = 16.6 Funct
BindingDB_Patents: 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.BindingDB_Patents: 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 6 1.8 CC1=NC2=C(C(=NN2C3=C1CNCC3)SC)S(=O)(=O)C4=CC=CC=C4
CHEMBL1091919 5ht6r_human Human No 7.8 IC50 = 16.8 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 5 3.6 CC1=NC2=C(C(=NN2C3=C1CCCC3)SC)S(=O)(=O)C4=CC=CC=C4
CHEMBL1091919 5ht6r_human Human No 7.8 IC50 = 16.8 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 5 3.6 CC1=NC2=C(C(=NN2C3=C1CCCC3)SC)S(=O)(=O)C4=CC=CC=C4
CHEMBL605938 5ht6r_human Human No 5.8 IC50 = 1600 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
421 4 2 6 3.8 C1CNCC1C2=CCC3=C2C=C(C=C3)NS(=O)(=O)C4=C(N=C5N4C=CS5)Cl
CHEMBL1173127 5ht6r_human Human Yes 5.8 IC50 = 1600 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
402 5 1 7 3.9 CCC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC(C)C
CHEMBL605938 5ht6r_human Human No 5.8 IC50 = 1600 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
421 4 2 6 3.8 C1CNCC1C2=CCC3=C2C=C(C=C3)NS(=O)(=O)C4=C(N=C5N4C=CS5)Cl
CHEMBL1173127 5ht6r_human Human Yes 5.8 IC50 = 1600 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
402 5 1 7 3.9 CCC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC(C)C
CHEMBL964 5ht6r_human Human Yes 4.8 IC50 = 16001 Funct
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)
297 7 0 4 3.9 CCN(CC)C(=S)SSC(=S)N(CC)CC
CHEMBL479548 5ht6r_human Human No 6.8 IC50 = 162 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 4 3.1 COC1=CC=CC=C1S(=O)(=O)N2C3=C(CCNCC3)C4=CC=CC=C42
CHEMBL479548 5ht6r_human Human No 6.8 IC50 = 162 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 4 3.1 COC1=CC=CC=C1S(=O)(=O)N2C3=C(CCNCC3)C4=CC=CC=C42
CHEMBL1172938 5ht6r_human Human Yes 5.8 IC50 = 1620 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
494 5 1 8 3.4 C1CC(OC1)CNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Br
CHEMBL1172938 5ht6r_human Human Yes 5.8 IC50 = 1620 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
494 5 1 8 3.4 C1CC(OC1)CNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=C(C=C5)Br
CHEMBL1642121 5ht6r_human Human No 6.8 IC50 = 165 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
466 4 0 7 3.3 CN1CCN(CC1)C2=C(C=C3C(=O)CCN(C3=C2)S(=O)(=O)C4=CC5=CC=CC=C5C=C4)OC
CHEMBL1642121 5ht6r_human Human No 6.8 IC50 = 165 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
466 4 0 7 3.3 CN1CCN(CC1)C2=C(C=C3C(=O)CCN(C3=C2)S(=O)(=O)C4=CC5=CC=CC=C5C=C4)OC
CHEMBL2407545 5ht6r_human Human No 5.8 IC50 = 1660 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
431 4 2 5 3.8 CC1=CC=C(C=C1)N2CCC3=C(C2=O)NN=C3NS(=O)(=O)C4=C(C(=CC=C4)Cl)C
CHEMBL41 5ht6r_human Human Yes 5.8 IC50 = 1661 Funct
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 5 4.0 CNCCC(C1=CC=CC=C1)OC2=CC=C(C=C2)C(F)(F)F
CHEMBL41 5ht6r_human Human Yes 5.8 IC50 = 1661 Funct
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 5 4.0 CNCCC(C1=CC=CC=C1)OC2=CC=C(C=C2)C(F)(F)F
CHEMBL601304 5ht6r_human Human No 5.8 IC50 = 1680 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 4.5 CC1=CC2=C(C=C1)N(C3C2CN(CC3)C)C=CC4=CC=CC=C4
CHEMBL601304 5ht6r_human Human No 5.8 IC50 = 1680 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 4.5 CC1=CC2=C(C=C1)N(C3C2CN(CC3)C)C=CC4=CC=CC=C4
CHEMBL3675191 5ht6r_human Human Yes 5.8 IC50 = 1683 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.
473 9 1 7 2.5 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CCC(=O)N(C)CCN(C)C
CHEMBL3675191 5ht6r_human Human Yes 5.8 IC50 = 1683 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
473 9 1 7 2.5 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CCC(=O)N(C)CCN(C)C
CHEMBL182099 5ht6r_human Human No 6.8 IC50 = 169 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 6 2.6 C1CNCC=C1C2=CN(C3=CC=CC=C32)S(=O)(=O)C4=NC=CC5=C4C=NS5
CHEMBL1086719 5ht6r_human Human No 7.8 IC50 = 17 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
375 3 0 3 3.6 CN1CCC(C1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL1277466 5ht6r_human Human No 7.8 IC50 = 17 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
407 3 1 5 3.9 CN1CCN(CC1)C2=CC=CC3=C(NN=C32)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1642120 5ht6r_human Human No 7.8 IC50 = 17 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
450 3 0 6 3.7 CC1CC(=O)C2=C(N1S(=O)(=O)C3=CC4=CC=CC=C4C=C3)C=C(C=C2)N5CCN(CC5)C
CHEMBL1086719 5ht6r_human Human No 7.8 IC50 = 17 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
375 3 0 3 3.6 CN1CCC(C1)N2C=C(C3=CC=CC=C32)S(=O)(=O)C4=CC(=CC=C4)Cl
CHEMBL1277466 5ht6r_human Human No 7.8 IC50 = 17 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
407 3 1 5 3.9 CN1CCN(CC1)C2=CC=CC3=C(NN=C32)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1642120 5ht6r_human Human No 7.8 IC50 = 17 Funct
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
450 3 0 6 3.7 CC1CC(=O)C2=C(N1S(=O)(=O)C3=CC4=CC=CC=C4C=C3)C=C(C=C2)N5CCN(CC5)C
CHEMBL42 5ht6r_human Human Yes 7.8 IC50 = 17 Funct
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
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL1091208 5ht6r_human Human No 7.8 IC50 = 17.2 Funct
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 5 3.2 CSC1=NN2C=C3CCCCC3=NC2=C1S(=O)(=O)C4=CC=CC=C4
CHEMBL1091208 5ht6r_human Human No 7.8 IC50 = 17.2 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 5 3.2 CSC1=NN2C=C3CCCCC3=NC2=C1S(=O)(=O)C4=CC=CC=C4
CHEMBL236988 5ht6r_human Human No 7.8 IC50 = 17.5 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 5 2.5 COC1=C(C=C(C=C1)S(=O)(=O)N2C=C(C3=CC=CC=C32)CCN)OC
CHEMBL597009 5ht6r_human Human No 7.8 IC50 = 17.5 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
421 4 1 5 4.3 CN(C)C1CCN(C1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1173359 5ht6r_human Human Yes 7.8 IC50 = 17.5 Funct
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 8 2.7 C1CC(OC1)CNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL236988 5ht6r_human Human No 7.8 IC50 = 17.5 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 5 2.5 COC1=C(C=C(C=C1)S(=O)(=O)N2C=C(C3=CC=CC=C32)CCN)OC
CHEMBL597009 5ht6r_human Human No 7.8 IC50 = 17.5 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
421 4 1 5 4.3 CN(C)C1CCN(C1)C2=CC3=C(NN=C3C=C2)S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1173359 5ht6r_human Human Yes 7.8 IC50 = 17.5 Funct
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 8 2.7 C1CC(OC1)CNC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL484333 5ht6r_human Human No 6.8 IC50 = 170 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
463 6 1 5 4.0 C1CCN(CC1)CCC(=O)NC2=CC3=C(C=C2)C=NN3S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1170696 5ht6r_human Human Yes 6.8 IC50 = 170 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
434 4 1 7 4.2 C1CCC(C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1170886 5ht6r_human Human Yes 6.8 IC50 = 170 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
428 4 1 7 4.7 C1CCCC(CC1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1169707 5ht6r_human Human Yes 6.8 IC50 = 170 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
436 5 0 7 4.0 CN(CC1=CC=CC=C1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1172789 5ht6r_human Human Yes 6.8 IC50 = 170 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
464 5 1 7 5.0 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC(C)C5=CC=CC=C5
CHEMBL484333 5ht6r_human Human No 6.8 IC50 = 170 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
463 6 1 5 4.0 C1CCN(CC1)CCC(=O)NC2=CC3=C(C=C2)C=NN3S(=O)(=O)C4=CC=CC5=CC=CC=C54
CHEMBL1170696 5ht6r_human Human Yes 6.8 IC50 = 170 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
434 4 1 7 4.2 C1CCC(C1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC(=CC=C5)Cl
CHEMBL1170886 5ht6r_human Human Yes 6.8 IC50 = 170 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
428 4 1 7 4.7 C1CCCC(CC1)NC2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1169707 5ht6r_human Human Yes 6.8 IC50 = 170 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
436 5 0 7 4.0 CN(CC1=CC=CC=C1)C2=NC3=C(N=NN3C4=C2SC=C4)S(=O)(=O)C5=CC=CC=C5
CHEMBL1172789 5ht6r_human Human Yes 6.8 IC50 = 170 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
464 5 1 7 5.0 CC1=CC(=C(C=C1)C)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC(C)C5=CC=CC=C5
CHEMBL1922621 5ht6r_human Human Yes 6.8 IC50 = 172 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.
403 7 1 7 2.9 CC1=NC2=C(C(=NN2C(=C1)N(C)CCN(C)C)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1922621 5ht6r_human Human Yes 6.8 IC50 = 172 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
403 7 1 7 2.9 CC1=NC2=C(C(=NN2C(=C1)N(C)CCN(C)C)NC)S(=O)(=O)C3=CC=CC=C3
CHEMBL1922624 5ht6r_human Human Yes 6.8 IC50 = 173 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.
401 4 1 7 2.7 CC1=NC2=C(C(=NN2C(=C1)N3CCN(CC3)C)NC)S(=O)(=O)C4=CC=CC=C4
CHEMBL1922624 5ht6r_human Human Yes 6.8 IC50 = 173 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
401 4 1 7 2.7 CC1=NC2=C(C(=NN2C(=C1)N3CCN(CC3)C)NC)S(=O)(=O)C4=CC=CC=C4
CHEMBL3675191 5ht6r_human Human Yes 6.8 IC50 = 174 Funct
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].
473 9 1 7 2.5 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CCC(=O)N(C)CCN(C)C
CHEMBL3675191 5ht6r_human Human Yes 6.8 IC50 = 174 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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].
473 9 1 7 2.5 CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)CCC(=O)N(C)CCN(C)C
CHEMBL1170280 5ht6r_human Human Yes 5.8 IC50 = 1750 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
450 5 1 7 5.1 CCC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC5=CC=CC(=C5)C
CHEMBL591801 5ht6r_human Human No 5.8 IC50 = 1750 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 3 4.2 CN1CCC2C(C1)C3=C(N2C=CC4=CC=CC=C4)C=CC(=C3)F
CHEMBL1170280 5ht6r_human Human Yes 5.8 IC50 = 1750 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
450 5 1 7 5.1 CCC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC5=CC=CC(=C5)C
CHEMBL591801 5ht6r_human Human No 5.8 IC50 = 1750 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 3 4.2 CN1CCC2C(C1)C3=C(N2C=CC4=CC=CC=C4)C=CC(=C3)F
CHEMBL574403 5ht6r_human Human No 6.8 IC50 = 176 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
450 5 3 7 2.7 C1CC(=NNC2=NCCN2)C3=C1C=CC(=C3)NS(=O)(=O)C4=C(N=C5N4C=CS5)Cl
CHEMBL574403 5ht6r_human Human No 6.8 IC50 = 176 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
450 5 3 7 2.7 C1CC(=NNC2=NCCN2)C3=C1C=CC(=C3)NS(=O)(=O)C4=C(N=C5N4C=CS5)Cl
CHEMBL1668569 5ht6r_human Human No 6.8 IC50 = 177 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 6 1.5 CC1=CC(=NC2=C(C(=NN12)SC)S(=O)(=O)C3=CC=CC=C3)CO
CHEMBL1668569 5ht6r_human Human No 6.8 IC50 = 177 Funct
BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general 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 6 1.5 CC1=CC(=NC2=C(C(=NN12)SC)S(=O)(=O)C3=CC=CC=C3)CO
CHEMBL806 5ht6r_human Human Yes 4.8 IC50 = 17814 Funct
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 2 1 6 3.3 CC(C)C(=O)NC1=CC(=C(C=C1)[N+](=O)[O-])C(F)(F)F
CHEMBL1642424 5ht6r_human Human No 5.8 IC50 = 1783 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
422 4 0 5 4.3 CCN1CCN(CC1)C2=CN(C3=C2C=C(C=C3)Cl)S(=O)(=O)C4=CC=C(C=C4)F
CHEMBL1642424 5ht6r_human Human No 5.8 IC50 = 1783 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
422 4 0 5 4.3 CCN1CCN(CC1)C2=CN(C3=C2C=C(C=C3)Cl)S(=O)(=O)C4=CC=C(C=C4)F
CHEMBL1081794 5ht6r_human Human No 7.8 IC50 = 18 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 5 3.0 C1CC(CNC1)N2C=C(C3=C2C=CC(=C3)F)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1668593 5ht6r_human Human No 7.8 IC50 = 18 Funct
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 2.1 CNC1=NN2C=CC=NC2=C1S(=O)(=O)C3=CC=C(C=C3)F
CHEMBL1081794 5ht6r_human Human No 7.8 IC50 = 18 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 5 3.0 C1CC(CNC1)N2C=C(C3=C2C=CC(=C3)F)S(=O)(=O)C4=CC=CC(=C4)F
CHEMBL1668593 5ht6r_human Human No 7.8 IC50 = 18 Funct
BindingDB_Patents: 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].BindingDB_Patents: 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 2.1 CNC1=NN2C=CC=NC2=C1S(=O)(=O)C3=CC=C(C=C3)F
CHEMBL3113351 5ht6r_human Human No 7.8 IC50 = 18 Funct
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
400 3 1 5 3.2 CSC1=C(C(=N)N2C=CC=CC2=N1)S(=O)(=O)C3=CC(=C(C=C3)Cl)Cl
CHEMBL1170098 5ht6r_human Human Yes 6.8 IC50 = 180 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
450 5 1 7 4.6 CC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC(C)C5=CC=CC=C5
CHEMBL592271 5ht6r_human Human Yes 6.8 IC50 = 180 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 4.5 CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)C=CC4=CC=C(C=C4)F
CHEMBL1170098 5ht6r_human Human Yes 6.8 IC50 = 180 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
450 5 1 7 4.6 CC1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NC(C)C5=CC=CC=C5
CHEMBL592271 5ht6r_human Human Yes 6.8 IC50 = 180 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 4.5 CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)C=CC4=CC=C(C=C4)F
CHEMBL1770373 5ht6r_human Human Yes 5.8 IC50 = 1800 Funct
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL2414711 5ht6r_human Human No 5.8 IC50 = 1800 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
459 5 0 5 4.9 CN1CCN(CC1)N=CC2=C(N(C3=CC=CC=C32)S(=O)(=O)C4=CC=CC=C4)C5=CC=CC=C5
CHEMBL1770373 5ht6r_human Human Yes 5.8 IC50 = 1800 Funct
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
239 2 1 3 2.1 C1CNCCC2=NC(=NC=C21)CC3=CC=CC=C3
CHEMBL1169900 5ht6r_human Human Yes 5.7 IC50 = 1830 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
498 6 1 7 5.6 CC(C)C1=CC=C(C=C1)S(=O)(=O)C2=C3N=C(C4=C(N3N=N2)C=CS4)NCC5=CC=CC=C5Cl
CHEMBL3398389 5ht6r_human Human No 5.7 IC50 = 1830 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 min