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
CHEMBL1487650 5ht5a_human Human Yes 4.3 EC50 = 47608 Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
336 4 1 3 3.8 CC1=C(C=CC(=C1OC)CN2CCC3=C(C2)NC4=CC=CC=C34)OC
CHEMBL1487650 5ht5a_human Human Yes 4.3 EC50 = 47608 Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
336 4 1 3 3.8 CC1=C(C=CC(=C1OC)CN2CCC3=C(C2)NC4=CC=CC=C34)OC
CHEMBL1169627 5ht5a_human Human Yes 4.1 EC50 = 79156 Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
595 2 2 8 6.0 CN1CCC2=CC(=C3C=C2C1CC4=CC=C(C=C4)OC5=C6C(CC7=CC(=C(C=C7)O)O3)N(CCC6=CC(=C5O)OC)C)OC
CHEMBL1169627 5ht5a_human Human Yes 4.1 EC50 = 79156 Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
595 2 2 8 6.0 CN1CCC2=CC(=C3C=C2C1CC4=CC=C(C=C4)OC5=C6C(CC7=CC(=C(C=C7)O)O3)N(CCC6=CC(=C5O)OC)C)OC
CHEMBL517986 5ht5a_human Human Yes 4.1 EC50 = 85847 Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
300 4 3 5 1.3 CCN(C1=NC(=C(N=C1Cl)C(=O)N=C(N)N)N)C(C)C
CHEMBL517986 5ht5a_human Human Yes 4.1 EC50 = 85847 Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
300 4 3 5 1.3 CCN(C1=NC(=C(N=C1Cl)C(=O)N=C(N)N)N)C(C)C
CHEMBL1210154 5ht5a_human Human No 9.0 IC50 = 1 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cells
336 5 1 4 4.7 CC(=NOC(=O)NC1=CC=CC=C1)C2=CC=CC(=C2)C3=CC=CS3
CHEMBL1210154 5ht5a_human Human No 9.0 IC50 = 1 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cells
336 5 1 4 4.7 CC(=NOC(=O)NC1=CC=CC=C1)C2=CC=CC(=C2)C3=CC=CS3
CHEMBL102645 5ht5a_human Human No 6.0 IC50 = 1000 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
350 5 2 5 1.6 CC1(CNS(=O)(=O)N1CC2=CC3=C(C=C2)NC=C3CCN(C)C)C
CHEMBL323334 5ht5a_human Human No 6.9 IC50 = 125.9 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
350 5 1 5 1.2 CN1CCCN(S1(=O)=O)CC2=CC3=C(C=C2)NC=C3CCN(C)C
CHEMBL321963 5ht5a_human Human No 6.9 IC50 = 125.9 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
365 7 1 5 1.9 CCN1CCN(S1(=O)=O)CCC2=CC3=C(C=C2)NC=C3CCN(C)C
CHEMBL103549 5ht5a_human Human No 6.9 IC50 = 125.9 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
336 6 2 5 1.4 CN(C)CCC1=CNC2=C1C=C(C=C2)CCN3CCNS3(=O)=O
CHEMBL103371 5ht5a_human Human No 6.7 IC50 = 199.5 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
350 6 1 5 1.6 CN1CCN(S1(=O)=O)CCC2=CC3=C(C=C2)NC=C3CCN(C)C
CHEMBL103388 5ht5a_human Human No 6.7 IC50 = 199.5 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
470 8 2 6 1.8 CC(=O)NC1=CC=C(C=C1)CN2CCN(S2(=O)=O)CC3=CC4=C(C=C3)NC=C4CCN(C)C
CHEMBL2111620 5ht5a_human Human No 5.7 IC50 = 1995.3 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
325 4 1 6 1.0 CN1CCN(S1(=O)=O)CC2=CC3=C(C=C2)SC=C3CCN
CHEMBL320412 5ht5a_human Human No 6.6 IC50 = 251.2 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
350 5 2 5 1.6 CC1(CN(S(=O)(=O)N1)CC2=CC3=C(C=C2)NC=C3CCN(C)C)C
CHEMBL326263 5ht5a_human Human No 5.5 IC50 = 3380 Funct
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
504 10 0 6 5.9 C1CN(CCN1CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)OCCC4=CC=C(C=C4)C#N
CHEMBL128 5ht5a_human Human Yes 6.3 IC50 = 501.2 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
295 6 2 4 0.9 CNS(=O)(=O)CC1=CC2=C(C=C1)NC=C2CCN(C)C
CHEMBL318571 5ht5a_human Human No 6.3 IC50 = 501.2 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
365 6 1 5 1.9 CC(C)N1CCN(S1(=O)=O)CC2=CC3=C(C=C2)NC=C3CCN(C)C
CHEMBL117537 5ht5a_human Human No 5.3 IC50 = 5520 Funct
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
477 10 0 4 6.1 C1CN(CCN1CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)CCCC4=CC=CC=C4
CHEMBL103854 5ht5a_human Human No 6.2 IC50 = 631.0 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
308 4 2 5 0.1 CN1CCN(S1(=O)=O)CC2=CC3=C(C=C2)NC=C3CCN
CHEMBL319223 5ht5a_human Human No 6.2 IC50 = 631.0 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
322 4 1 5 1.2 CN1CCN(S1(=O)=O)C2=CC3=C(C=C2)NC=C3CCN(C)C
CHEMBL101138 5ht5a_human Human No 7.1 IC50 = 79.4 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
399 6 1 5 2.7 CN(C)CCC1=CNC2=C1C=C(C=C2)N3CCN(S3(=O)=O)CC4=CC=CC=C4
CHEMBL103205 5ht5a_human Human No 6.1 IC50 = 794.3 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
336 5 1 5 0.8 CN1CCN(S1(=O)=O)CC2=CC3=C(C=C2)NC=C3CCN(C)C
CHEMBL102548 5ht5a_human Human No 6.1 IC50 = 794.3 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
322 5 2 5 0.6 CN(C)CCC1=CNC2=C1C=C(C=C2)CN3CCNS3(=O)=O
CHEMBL102586 5ht5a_human Human No 6.1 IC50 = 794.3 Funct
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
322 5 2 5 0.6 CNCCC1=CNC2=C1C=C(C=C2)CN3CCN(S3(=O)=O)C
CHEMBL270177 5ht5a_human Human Yes 8.5 Kd = 3.0 Funct
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL270177 5ht5a_human Human Yes 8.5 Kd = 3.0 Funct
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL270177 5ht5a_human Human Yes 8.5 Kd = 3.2 Funct
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL270177 5ht5a_human Human Yes 8.5 Kd = 3.2 Funct
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL404511 5ht5a_human Human Yes 7.4 Kd = 38.9 Funct
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL404511 5ht5a_human Human Yes 7.4 Kd = 38.9 Funct
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL269964 5ht5a_human Human Yes 8.1 Kd = 7.4 Funct
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
210 1 2 1 1.6 CC1C2=C(C=CC=C2Cl)NC(=N1)NC
CHEMBL269964 5ht5a_human Human Yes 8.1 Kd = 7.4 Funct
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
210 1 2 1 1.6 CC1C2=C(C=CC=C2Cl)NC(=N1)NC
CHEMBL3654198 5ht5a_human Human No 9.2 Ki = 0.7 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
366 1 2 5 2.7 C1CN(CC2=C(C=CC(=C21)F)C3=C(C=C(C=C3F)F)F)C(=O)N=C(N)N
CHEMBL3654198 5ht5a_human Human No 9.2 Ki = 0.7 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
366 1 2 5 2.7 C1CN(CC2=C(C=CC(=C21)F)C3=C(C=C(C=C3F)F)F)C(=O)N=C(N)N
CHEMBL3654206 5ht5a_human Human No 9.1 Ki = 0.8 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
374 1 2 4 2.9 C1CC12CN(CC3=C(C=CC(=C23)F)C4=C(C=CC=C4F)F)C(=O)N=C(N)N
CHEMBL3654206 5ht5a_human Human No 9.1 Ki = 0.8 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
374 1 2 4 2.9 C1CC12CN(CC3=C(C=CC(=C23)F)C4=C(C=CC=C4F)F)C(=O)N=C(N)N
CHEMBL3654212 5ht5a_human Human No 9.1 Ki = 0.9 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
374 1 2 4 2.9 C1CC12CN(CC3=C(C=CC(=C23)F)C4=C(C=C(C=C4)F)F)C(=O)N=C(N)N
CHEMBL3654212 5ht5a_human Human No 9.1 Ki = 0.9 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
374 1 2 4 2.9 C1CC12CN(CC3=C(C=CC(=C23)F)C4=C(C=C(C=C4)F)F)C(=O)N=C(N)N
CHEMBL3654208 5ht5a_human Human No 9.1 Ki = 0.9 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
392 1 2 5 3.0 C1CC12CN(CC3=C(C=CC(=C23)F)C4=C(C=C(C=C4F)F)F)C(=O)N=C(N)N
CHEMBL3654208 5ht5a_human Human No 9.1 Ki = 0.9 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
392 1 2 5 3.0 C1CC12CN(CC3=C(C=CC(=C23)F)C4=C(C=C(C=C4F)F)F)C(=O)N=C(N)N
CHEMBL3654214 5ht5a_human Human No 9.0 Ki = 1.0 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
356 1 2 3 2.8 C1CC12CN(CC3=C(C=CC(=C23)F)C4=CC=CC=C4F)C(=O)N=C(N)N
CHEMBL3654214 5ht5a_human Human No 9.0 Ki = 1.0 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
356 1 2 3 2.8 C1CC12CN(CC3=C(C=CC(=C23)F)C4=CC=CC=C4F)C(=O)N=C(N)N
CHEMBL3654197 5ht5a_human Human No 9.0 Ki = 1.1 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
383 1 2 4 3.3 C1CN(CC2=C(C=CC(=C21)Cl)C3=C(C=C(C=C3F)F)F)C(=O)N=C(N)N
CHEMBL3654199 5ht5a_human Human No 9.0 Ki = 1.1 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
348 1 2 4 2.6 C1CN(CC2=C(C=CC(=C21)F)C3=C(C=CC=C3F)F)C(=O)N=C(N)N
CHEMBL3654197 5ht5a_human Human No 9.0 Ki = 1.1 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
383 1 2 4 3.3 C1CN(CC2=C(C=CC(=C21)Cl)C3=C(C=C(C=C3F)F)F)C(=O)N=C(N)N
CHEMBL3654199 5ht5a_human Human No 9.0 Ki = 1.1 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
348 1 2 4 2.6 C1CN(CC2=C(C=CC(=C21)F)C3=C(C=CC=C3F)F)C(=O)N=C(N)N
CHEMBL3644535 5ht5a_human Human No 8.9 Ki = 1.2 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.5 C1=CC(=C(C(=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)Cl)F
CHEMBL3644535 5ht5a_human Human No 8.9 Ki = 1.2 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.5 C1=CC(=C(C(=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)Cl)F
CHEMBL3654210 5ht5a_human Human No 8.9 Ki = 1.3 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
392 1 2 5 3.0 C1CC12CN(CC3=C(C=CC(=C23)F)C4=CC(=C(C=C4F)F)F)C(=O)N=C(N)N
CHEMBL3644530 5ht5a_human Human No 8.9 Ki = 1.3 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
358 2 2 5 3.3 CC1=CN=C(C2=C1C=CC(=C2)C(=O)N=C(N)N)C3=C(C=C(C=C3F)F)F
CHEMBL3644525 5ht5a_human Human No 8.9 Ki = 1.3 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.6 C1=CC2=NC=C(C(=C2C=C1C(=O)N=C(N)N)C3=C(C=C(C=C3)F)F)Cl
CHEMBL404372 5ht5a_rat Rat No 8.9 Ki = 1.3 Funct
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL404372 5ht5a_rat Rat No 8.9 Ki = 1.3 Funct
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL3654210 5ht5a_human Human No 8.9 Ki = 1.3 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
392 1 2 5 3.0 C1CC12CN(CC3=C(C=CC(=C23)F)C4=CC(=C(C=C4F)F)F)C(=O)N=C(N)N
CHEMBL3644530 5ht5a_human Human No 8.9 Ki = 1.3 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
358 2 2 5 3.3 CC1=CN=C(C2=C1C=CC(=C2)C(=O)N=C(N)N)C3=C(C=C(C=C3F)F)F
CHEMBL3644525 5ht5a_human Human No 8.9 Ki = 1.3 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.6 C1=CC2=NC=C(C(=C2C=C1C(=O)N=C(N)N)C3=C(C=C(C=C3)F)F)Cl
CHEMBL3644528 5ht5a_human Human No 8.9 Ki = 1.4 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
344 2 2 5 3.0 C1=CC(=C(C(=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)F
CHEMBL3644528 5ht5a_human Human No 8.9 Ki = 1.4 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
344 2 2 5 3.0 C1=CC(=C(C(=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)F
CHEMBL3654207 5ht5a_human Human No 8.8 Ki = 1.6 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
362 1 2 4 3.0 CC1CN(CC2=C(C=CC(=C12)F)C3=C(C=CC=C3F)F)C(=O)N=C(N)N
CHEMBL3644527 5ht5a_human Human No 8.8 Ki = 1.6 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.5 C1=CC(=C(C(=C1)Cl)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)F
CHEMBL404372 5ht5a_human Human No 8.8 Ki = 1.6 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL404372 5ht5a_human Human No 8.8 Ki = 1.6 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL3654207 5ht5a_human Human No 8.8 Ki = 1.6 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
362 1 2 4 3.0 CC1CN(CC2=C(C=CC(=C12)F)C3=C(C=CC=C3F)F)C(=O)N=C(N)N
CHEMBL3644527 5ht5a_human Human No 8.8 Ki = 1.6 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.5 C1=CC(=C(C(=C1)Cl)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)F
CHEMBL3644540 5ht5a_human Human No 8.7 Ki = 1.8 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
322 2 2 3 3.1 CC1=CN=C(C2=C1C=CC(=C2)C(=O)N=C(N)N)C3=CC=CC=C3F
CHEMBL256694 5ht5a_human Human No 8.7 Ki = 1.8 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
294 3 2 3 3.1 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)NCC(F)F
CHEMBL256694 5ht5a_human Human No 8.8 Ki = 1.8 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
294 3 2 3 3.1 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)NCC(F)F
CHEMBL3644540 5ht5a_human Human No 8.8 Ki = 1.8 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
322 2 2 3 3.1 CC1=CN=C(C2=C1C=CC(=C2)C(=O)N=C(N)N)C3=CC=CC=C3F
CHEMBL3654205 5ht5a_human Human No 8.7 Ki = 1.9 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
382 1 2 3 2.7 C1CN(CC2=C(C=CC(=C21)F)C3=C(C=C(C=N3)Cl)Cl)C(=O)N=C(N)N
CHEMBL3644537 5ht5a_human Human No 8.7 Ki = 1.9 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
340 2 2 4 3.2 CC1=CN=C(C2=C1C=CC(=C2)C(=O)N=C(N)N)C3=C(C=CC=C3F)F
CHEMBL3654205 5ht5a_human Human No 8.7 Ki = 1.9 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
382 1 2 3 2.7 C1CN(CC2=C(C=CC(=C21)F)C3=C(C=C(C=N3)Cl)Cl)C(=O)N=C(N)N
CHEMBL3644537 5ht5a_human Human No 8.7 Ki = 1.9 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
340 2 2 4 3.2 CC1=CN=C(C2=C1C=CC(=C2)C(=O)N=C(N)N)C3=C(C=CC=C3F)F
CHEMBL258075 5ht5a_human Human Yes 8.0 Ki = 10 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
219 2 2 2 1.3 CC1C2=C(C(=CC=C2)OC(C)C)NC(=N1)N
CHEMBL258075 5ht5a_human Human Yes 8.0 Ki = 10 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
219 2 2 2 1.3 CC1C2=C(C(=CC=C2)OC(C)C)NC(=N1)N
CHEMBL404511 5ht5a_human Human Yes 8.0 Ki = 10.1 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL269964 5ht5a_human Human Yes 8.0 Ki = 10.7 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
210 1 2 1 1.6 CC1C2=C(C=CC=C2Cl)NC(=N1)NC
CHEMBL269964 5ht5a_human Human Yes 8.0 Ki = 10.7 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
210 1 2 1 1.6 CC1C2=C(C=CC=C2Cl)NC(=N1)NC
CHEMBL269964 5ht5a_human Human Yes 8.0 Ki = 10.8 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
210 1 2 1 1.6 CC1C2=C(C=CC=C2Cl)NC(=N1)NC
CHEMBL128848 5ht5a_human Human No 7.0 Ki = 100 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
320 5 0 2 3.9 CN1C2=C(CN(CC2)CCCOC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL128099 5ht5a_human Human No 7.0 Ki = 100 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
334 6 0 2 4.2 CCN1C2=C(CN(CC2)CCCOC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL13816 5ht5a_human Human No 6.0 Ki = 1000 Funct
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
389 5 2 3 3.8 CN1CC(CC2C1CC3=CNC4=CC=CC2=C34)CNC(=O)OCC5=CC=CC=C5
CHEMBL56 5ht5a_human Human Yes 6.0 Ki = 1000 Funct
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
247 5 1 2 4.1 CCCN(CCC)C1CCC2=C(C1)C(=CC=C2)O
CHEMBL85 5ht5a_human Human Yes 6.0 Ki = 1000 Funct
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
411 4 0 6 2.7 CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
CHEMBL42 5ht5a_human Human Yes 6.0 Ki = 1000 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL2442270 5ht5a_human Human No 7.0 Ki = 101 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
226 1 3 1 0.9 C1=CC=C2C(=C1)C(=CN2)C=C3C(=O)N=C(N3)N
CHEMBL272517 5ht5a_human Human Yes 7.0 Ki = 103 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
175 1 2 1 1.0 CC1C2=CC=CC=C2NC(=N1)NC
CHEMBL272517 5ht5a_human Human Yes 7.0 Ki = 103 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
175 1 2 1 1.0 CC1C2=CC=CC=C2NC(=N1)NC
CHEMBL7143 5ht5a_human Human Yes 5.0 Ki = 10450 Funct
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
232 4 1 2 2.7 CC1=C(C2=C(N1)C=CC(=C2)OC)CCN(C)C
CHEMBL126666 5ht5a_human Human No 6.0 Ki = 1080 Funct
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
326 7 0 3 4.0 CN1C=C(C2=CC=CC=C21)CN(C)CCCOC3=CC=C(C=C3)F
CHEMBL126021 5ht5a_mouse Mouse No 6.0 Ki = 1100 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
244 3 1 2 1.6 CN1C2=C(CN(CC2)CCCO)C3=CC=CC=C31
CHEMBL2442274 5ht5a_human Human No 7.0 Ki = 112 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
305 1 3 1 1.6 C1=CC2=C(C(=C1)Br)NC=C2C=C3C(=O)N=C(N3)N
CHEMBL126021 5ht5a_human Human No 6.0 Ki = 1120 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
244 3 1 2 1.6 CN1C2=C(CN(CC2)CCCO)C3=CC=CC=C31
CHEMBL129230 5ht5a_mouse Mouse No 6.9 Ki = 115 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
350 5 0 3 3.7 CN1C2=C(CN(CC2)CCCC(=O)C3=CC=C(C=C3)F)C4=CC=CC=C41
CHEMBL3326982 5ht5a_human Human No 5.9 Ki = 1178 Funct
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
492 10 1 4 5.5 COC1=CC=CC=C1N2CCN(CC2)CCCCC(=O)NCC3=CC=CC=C3C4=CC=CC=C4Cl
CHEMBL3326982 5ht5a_human Human No 5.9 Ki = 1178 Funct
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
492 10 1 4 5.5 COC1=CC=CC=C1N2CCN(CC2)CCCCC(=O)NCC3=CC=CC=C3C4=CC=CC=C4Cl
CHEMBL190382 5ht5a_human Human No 7.9 Ki = 12.6 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
513 14 1 4 5.7 CN(C)CCN(CC1=CC=C(C=C1)C2=NC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)CCC4CCCC4
CHEMBL190382 5ht5a_human Human No 7.9 Ki = 12.6 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
513 14 1 4 5.7 CN(C)CCN(CC1=CC=C(C=C1)C2=NC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)CCC4CCCC4
CHEMBL125417 5ht5a_mouse Mouse No 6.9 Ki = 120 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
332 6 0 1 5.1 CN1C2=C(CN(CC2)CCCCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL125745 5ht5a_rat Rat No 5.9 Ki = 1200 Funct
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
300 4 1 3 2.5 C1=CC=C(C=C1)S(=O)(=O)N2C=CC3=C(C=CC=C32)CCN
CHEMBL402400 5ht5a_human Human No 6.9 Ki = 122 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
215 2 2 1 1.9 CC1C2=CC=CC=C2NC(=N1)NC3CCC3
CHEMBL402400 5ht5a_human Human No 6.9 Ki = 122 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
215 2 2 1 1.9 CC1C2=CC=CC=C2NC(=N1)NC3CCC3
CHEMBL128184 5ht5a_mouse Mouse No 5.9 Ki = 1220 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
368 6 0 4 4.0 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=C1C(=CC=C4)OC
CHEMBL2442271 5ht5a_human Human No 6.9 Ki = 123 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
305 1 3 1 1.6 C1=CC2=C(C(=C1)Br)C(=CN2)C=C3C(=O)N=C(N3)N
CHEMBL257302 5ht5a_human Human No 6.9 Ki = 124 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
271 4 2 1 4.1 CC1C2=CC=CC=C2NC(=N1)NCCC3CCCCC3
CHEMBL257302 5ht5a_human Human No 6.9 Ki = 124 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
271 4 2 1 4.1 CC1C2=CC=CC=C2NC(=N1)NCCC3CCCCC3
CHEMBL189262 5ht5a_human Human No 6.9 Ki = 125.9 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
490 11 2 3 6.3 C1CN(CCC1NCC2=CC=C(C=C2)C3=CC=C(C=C3)CNCCC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL189262 5ht5a_human Human No 6.9 Ki = 125.9 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
490 11 2 3 6.3 C1CN(CCC1NCC2=CC=C(C=C2)C3=CC=C(C=C3)CNCCC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL497963 5ht5a_human Human No 5.9 Ki = 1258.9 Funct
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
454 8 1 6 4.3 CC1=NC2=C(C=C1)C(=CC=C2)OCCN3CCC(CC3)CC4=CC(=CC=C4)NS(=O)(=O)C
CHEMBL497963 5ht5a_human Human No 5.9 Ki = 1258.9 Funct
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
454 8 1 6 4.3 CC1=NC2=C(C=C1)C(=CC=C2)OCCN3CCC(CC3)CC4=CC(=CC=C4)NS(=O)(=O)C
CHEMBL2442275 5ht5a_human Human No 5.9 Ki = 1282 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
319 1 2 2 1.8 CN1C(=O)C(=CC2=CNC3=C2C(=CC=C3)Br)N=C1N
CHEMBL3644524 5ht5a_human Human No 7.9 Ki = 13 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
358 2 2 5 3.4 CC1=NC2=C(C=C(C=C2)C(=O)N=C(N)N)C(=C1)C3=C(C=C(C=C3F)F)F
CHEMBL138989 5ht5a_human Human No 7.9 Ki = 13 Funct
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
335 1 1 2 3.2 CC1CC(N1C(=O)C2CN(C3CC4=CNC5=CC=CC(=C45)C3=C2)C)C
CHEMBL96504 5ht5a_human Human No 7.9 Ki = 13 Funct
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
338 5 0 3 4.0 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=CC=CC=C41
CHEMBL96504 5ht5a_mouse Mouse No 7.9 Ki = 13 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
338 5 0 3 4.0 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=CC=CC=C41
CHEMBL3644524 5ht5a_human Human No 7.9 Ki = 13 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
358 2 2 5 3.4 CC1=NC2=C(C=C(C=C2)C(=O)N=C(N)N)C(=C1)C3=C(C=C(C=C3F)F)F
CHEMBL129472 5ht5a_mouse Mouse No 6.9 Ki = 130 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
318 5 0 1 4.6 CN1C2=C(CN(CC2)CCCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL2058409 5ht5a_human Human No 5.9 Ki = 1323 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
319 1 2 1 1.8 CN1C(=CC2=CNC3=C2C=CC=C3Br)C(=O)N=C1N
CHEMBL129476 5ht5a_mouse Mouse No 6.9 Ki = 135 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
332 5 0 2 3.6 CN1C2=C(CN(CC2)CCCC(=O)C3=CC=CC=C3)C4=CC=CC=C41
CHEMBL128184 5ht5a_human Human No 5.9 Ki = 1395 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
368 6 0 4 4.0 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=C1C(=CC=C4)OC
CHEMBL2058418 5ht5a_human Human No 5.9 Ki = 1425 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
333 2 2 1 2.2 CNC1=NC(=O)C(=CC2=CNC3=C2C=CC=C3Br)N1C
CHEMBL2058415 5ht5a_human Human No 5.8 Ki = 1454 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
333 2 2 1 2.2 CNC1=NC(=O)C(=CC2=CNC3=C2C(=CC=C3)Br)N1C
CHEMBL270131 5ht5a_human Human No 5.8 Ki = 1472 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL270131 5ht5a_human Human No 5.8 Ki = 1472 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL273921 5ht5a_human Human No 5.8 Ki = 1479.1 Funct
Binding affinity towards cloned human 5-HT5A receptor was determinedBinding affinity towards cloned human 5-HT5A receptor was determined
423 4 1 4 3.0 C1CC2=CC=CC=C2C(=O)N(C1)CCN3CCC(CC3)N4C5=C(C=C(C=C5)F)NC4=O
CHEMBL1829959 5ht5a_human Human Yes 5.8 Ki = 1525 Funct
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
240 2 2 4 1.6 COC1=CC=CC2=C1C(=CN2)C3=NC(=NC=C3)N
CHEMBL1829959 5ht5a_human Human Yes 5.8 Ki = 1525 Funct
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
240 2 2 4 1.6 COC1=CC=CC2=C1C(=CN2)C3=NC(=NC=C3)N
CHEMBL270658 5ht5a_human Human Yes 6.8 Ki = 153 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
203 3 2 1 1.9 CCCNC1=NC(C2=CC=CC=C2N1)C
CHEMBL270658 5ht5a_human Human Yes 6.8 Ki = 153 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
203 3 2 1 1.9 CCCNC1=NC(C2=CC=CC=C2N1)C
CHEMBL2442277 5ht5a_human Human No 5.8 Ki = 1550 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
319 1 2 2 1.8 CN1C(=O)C(=CC2=CNC3=C2C=CC=C3Br)N=C1N
CHEMBL516088 5ht5a_human Human No 5.8 Ki = 1584 Funct
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
403 9 0 6 4.4 COC1=C(C=CC=C1OCCF)C(=O)C2CCN(CC2)CCC3=CC=C(C=C3)F
CHEMBL516088 5ht5a_human Human No 5.8 Ki = 1584 Funct
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
403 9 0 6 4.4 COC1=C(C=CC=C1OCCF)C(=O)C2CCN(CC2)CCC3=CC=C(C=C3)F
CHEMBL522708 5ht5a_human Human No 5.8 Ki = 1584.9 Funct
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
480 7 0 6 4.6 CC1=NC2=C(C=C1)C(=CC=C2)OCCN3CCC(CC3)CC4=CC(=CC=C4)N5CCCS5(=O)=O
CHEMBL522708 5ht5a_human Human No 5.8 Ki = 1584.9 Funct
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
480 7 0 6 4.6 CC1=NC2=C(C=C1)C(=CC=C2)OCCN3CCC(CC3)CC4=CC(=CC=C4)N5CCCS5(=O)=O
CHEMBL137781 5ht5a_human Human No 7.8 Ki = 16 Funct
Binding affinities against 5-hydroxytryptamine 5A receptorBinding affinities against 5-hydroxytryptamine 5A receptor
335 1 1 2 3.2 CC1CC(N1C(=O)C2CN(C3CC4=CNC5=CC=CC(=C45)C3=C2)C)C
CHEMBL126340 5ht5a_rat Rat No 5.8 Ki = 1600 Funct
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
433 7 0 4 5.2 CN(C)CCC1=C2C=C(N(C2=CC=C1)S(=O)(=O)C3=CC=CC=C3)C(=O)C4=CC=CC=C4
CHEMBL18041 5ht5a_human Human Yes 4.8 Ki = 16000 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
310 3 2 4 1.7 COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N
CHEMBL403102 5ht5a_human Human No 6.8 Ki = 163 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
245 3 2 2 1.4 CC1C2=CC=CC=C2NC(=N1)NCC3CCCO3
CHEMBL403102 5ht5a_human Human No 6.8 Ki = 163 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
245 3 2 2 1.4 CC1C2=CC=CC=C2NC(=N1)NCC3CCCO3
CHEMBL128185 5ht5a_human Human No 6.8 Ki = 165 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
368 6 0 4 4.0 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=C1C=CC(=C4)OC
CHEMBL129476 5ht5a_human Human No 6.8 Ki = 168 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
332 5 0 2 3.6 CN1C2=C(CN(CC2)CCCC(=O)C3=CC=CC=C3)C4=CC=CC=C41
CHEMBL278751 5ht5a_human Human Yes 6.8 Ki = 168 Funct
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
275 6 0 2 4.8 CCCN(CCC)C1CCC2=C(C1C)C=CC=C2OC
CHEMBL490632 5ht5a_human Human No 5.8 Ki = 1684 Funct
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
400 9 0 5 4.7 CC1=CC=C(C=C1)CCN2CCC(CC2)C(=O)C3=C(C(=CC=C3)OCCF)OC
CHEMBL490632 5ht5a_human Human No 5.8 Ki = 1684 Funct
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
400 9 0 5 4.7 CC1=CC=C(C=C1)CCN2CCC(CC2)C(=O)C3=C(C(=CC=C3)OCCF)OC
CHEMBL34652 5ht5a_rat Rat No 7.8 Ki = 17 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
247 7 0 2 4.0 CCCN(CCC)C1CC1C2=CC=CC=C2OC
CHEMBL2181166 5ht5a_human Human No 5.8 Ki = 1700 Funct
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
555 7 0 5 6.6 C1CN(CCC1COC2=C3C=CC=NC3=C4C=CC=C(C4=N2)F)CCCC5=CC=C(C=C5)I
CHEMBL129774 5ht5a_mouse Mouse No 5.8 Ki = 1710 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
328 3 0 1 4.4 CN1C2=C(CN(CC2)CC#CCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL125417 5ht5a_human Human No 6.8 Ki = 174 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
332 6 0 1 5.1 CN1C2=C(CN(CC2)CCCCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL256049 5ht5a_human Human No 6.8 Ki = 176 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
247 6 2 2 1.6 CCOCCCNC1=NC(C2=CC=CC=C2N1)C
CHEMBL256049 5ht5a_human Human No 6.8 Ki = 176 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
247 6 2 2 1.6 CCOCCCNC1=NC(C2=CC=CC=C2N1)C
CHEMBL129774 5ht5a_human Human No 5.8 Ki = 1775 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
328 3 0 1 4.4 CN1C2=C(CN(CC2)CC#CCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL338095 5ht5a_mouse Mouse No 6.8 Ki = 180 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
373 5 0 3 4.7 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=C1C=CC(=C4)Cl
CHEMBL95104 5ht5a_human Human Yes 6.7 Ki = 182.0 Funct
Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )
488 7 1 5 5.0 C1CC(N(C1)S(=O)(=O)C2=CC3=C(C=C2)C=CN3)CCN4CCC(CC4)OC5=CC=C(C=C5)Cl
CHEMBL2442273 5ht5a_human Human No 6.7 Ki = 184 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
305 1 3 1 1.6 C1=CC2=C(C=C1Br)NC=C2C=C3C(=O)N=C(N3)N
CHEMBL446356 5ht5a_human Human No 6.7 Ki = 185 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
330 5 0 1 4.6 CN1C2=C(CN(CC2)CC=CCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL132019 5ht5a_rat Rat No 6.7 Ki = 186 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
247 7 1 2 3.8 CCCN(CCC)CC1CC1C2=CC(=CC=C2)O
CHEMBL402874 5ht5a_human Human Yes 6.7 Ki = 189 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
217 4 2 1 2.2 CCCCNC1=NC(C2=CC=CC=C2N1)C
CHEMBL402874 5ht5a_human Human Yes 6.7 Ki = 189 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
217 4 2 1 2.2 CCCCNC1=NC(C2=CC=CC=C2N1)C
CHEMBL435814 5ht5a_human Human No 6.7 Ki = 190 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
335 5 1 3 3.2 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)N)C4=CC=CC=C41
CHEMBL340861 5ht5a_human Human No 5.7 Ki = 1920 Funct
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
288 5 0 3 2.7 CN1C=CC2=C1CCN(C2)CCCOC3=CC=C(C=C3)F
CHEMBL187415 5ht5a_human Human No 6.7 Ki = 199.5 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
490 11 2 3 6.3 C1CN(CCC1NCC2=CC=CC(=C2)C3=CC=C(C=C3)CNCCC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL3217984 5ht5a_human Human No 6.7 Ki = 199.5 Funct
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
308 0 0 3 3.7 CN1CCC2C(C1)C3=C4N2C5=CC=CC=C5CSC4=CC=C3
CHEMBL187415 5ht5a_human Human No 6.7 Ki = 199.5 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
490 11 2 3 6.3 C1CN(CCC1NCC2=CC=CC(=C2)C3=CC=C(C=C3)CNCCC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL273170 5ht5a_human Human Yes 8.7 Ki = 2 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
230 0 2 1 1.8 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)N
CHEMBL274384 5ht5a_mouse Mouse Yes 8.7 Ki = 2 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
402 3 1 2 4.0 CCN(CC)C(=O)C1CN(C2CC3=C(NC4=CC=CC(=C34)C2=C1)Br)C
CHEMBL273170 5ht5a_human Human Yes 8.7 Ki = 2 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
230 0 2 1 1.8 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)N
CHEMBL3644541 5ht5a_human Human No 8.6 Ki = 2.3 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.5 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2Cl)C3=C(C=C(C=C3)F)F
CHEMBL3644541 5ht5a_human Human No 8.6 Ki = 2.3 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.5 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2Cl)C3=C(C=C(C=C3)F)F
CHEMBL3654204 5ht5a_human Human No 8.6 Ki = 2.5 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
366 1 2 4 2.1 C1CN(CC2=C(C=CC(=C21)Cl)C3=C(C=NC=C3F)F)C(=O)N=C(N)N
CHEMBL3654204 5ht5a_human Human No 8.6 Ki = 2.5 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
366 1 2 4 2.1 C1CN(CC2=C(C=CC(=C21)Cl)C3=C(C=NC=C3F)F)C(=O)N=C(N)N
CHEMBL34653 5ht5a_rat Rat No 8.6 Ki = 2.6 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
233 6 1 2 3.6 CCCN(CCC)C1CC1C2=CC(=CC=C2)O
CHEMBL3654209 5ht5a_human Human No 8.6 Ki = 2.7 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
302 1 2 2 2.0 C1CC1C2=C3CN(CC4(C3=C(C=C2)F)CC4)C(=O)N=C(N)N
CHEMBL3654200 5ht5a_human Human No 8.6 Ki = 2.7 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
365 1 2 3 3.2 C1CN(CC2=C(C=CC(=C21)Cl)C3=C(C=C(C=C3)F)F)C(=O)N=C(N)N
CHEMBL3654209 5ht5a_human Human No 8.6 Ki = 2.7 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
302 1 2 2 2.0 C1CC1C2=C3CN(CC4(C3=C(C=C2)F)CC4)C(=O)N=C(N)N
CHEMBL3654200 5ht5a_human Human No 8.6 Ki = 2.7 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
365 1 2 3 3.2 C1CN(CC2=C(C=CC(=C21)Cl)C3=C(C=C(C=C3)F)F)C(=O)N=C(N)N
CHEMBL541993 5ht5a_rat Rat No 8.5 Ki = 2.9 Funct
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL541993 5ht5a_rat Rat No 8.5 Ki = 2.9 Funct
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL97518 5ht5a_human Human No 6.7 Ki = 200 Funct
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
367 5 3 3 2.9 CCC(C)(CNC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C)CO
CHEMBL126897 5ht5a_human Human No 6.7 Ki = 200 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
389 5 0 2 5.2 CN1C2=C(CN(CC2)CCCOC3=CC(=C(C=C3)Cl)Cl)C4=CC=CC=C41
CHEMBL126898 5ht5a_human Human No 6.7 Ki = 200 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
355 5 0 2 4.6 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)Cl)C4=CC=CC=C41
CHEMBL2111848 5ht5a_human Human No 6.7 Ki = 208 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
330 5 0 1 4.6 CN1C2=C(CN(CC2)CC=CCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL3752900 5ht5a_human Human No 5.7 Ki = 2089.3 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
275 7 1 1 3.5 C=CCN(CCC1=CNC2=C1C=C(C=C2)Cl)CC=C
CHEMBL3752900 5ht5a_human Human No 5.7 Ki = 2089.3 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
275 7 1 1 3.5 C=CCN(CCC1=CNC2=C1C=C(C=C2)Cl)CC=C
CHEMBL278509 5ht5a_human Human Yes 5.7 Ki = 2100 Funct
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
212 1 1 2 2.6 C1CN(CCN1)C2=CC3=CC=CC=C3C=C2
CHEMBL2413153 5ht5a_human Human No 5.7 Ki = 2128 Funct
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
405 9 0 7 2.1 CN1C(=O)C=NN(C1=O)CCCCN2CCN(CC2)C3=CC=CC=C3OCCF
CHEMBL266250 5ht5a_mouse Mouse Yes 6.7 Ki = 215 Funct
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
178 1 2 3 1.0 C1CN(CCN1)C2=CC=CC=C2O
CHEMBL257744 5ht5a_human Human No 7.7 Ki = 22.2 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
290 4 2 4 2.4 CC1C2=C(C=CC(=C2OC)Cl)NC(=N1)NCC(F)F
CHEMBL446459 5ht5a_human Human No 7.7 Ki = 22.2 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
283 5 2 4 2.6 CC1C2=C(C(=CC=C2)OC(C)C)NC(=N1)NCC(F)F
CHEMBL257744 5ht5a_human Human No 7.7 Ki = 22.2 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
290 4 2 4 2.4 CC1C2=C(C=CC(=C2OC)Cl)NC(=N1)NCC(F)F
CHEMBL446459 5ht5a_human Human No 7.7 Ki = 22.2 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
283 5 2 4 2.6 CC1C2=C(C(=CC=C2)OC(C)C)NC(=N1)NCC(F)F
CHEMBL258073 5ht5a_human Human No 7.6 Ki = 22.9 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
226 1 2 2 1.2 CC1C2=C(C=CC(=C2OC)Cl)NC(=N1)N
CHEMBL258073 5ht5a_human Human No 7.6 Ki = 22.9 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
226 1 2 2 1.2 CC1C2=C(C=CC(=C2OC)Cl)NC(=N1)N
CHEMBL481153 5ht5a_human Human No 5.7 Ki = 2200 Funct
Antagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assay
340 4 0 4 3.9 C1CCN(C1)CCOC(=O)N2C3=CC=CC=C3SC4=CC=CC=C42
CHEMBL467094 5ht5a_human Human Yes 5.7 Ki = 2224 Funct
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
339 2 0 5 3.2 CN1CCC2=CC(=C(C3=C2C1CC4=CC5=C(C=C43)OCO5)OC)OC
CHEMBL467094 5ht5a_human Human Yes 5.7 Ki = 2224 Funct
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
339 2 0 5 3.2 CN1CCC2=CC(=C(C3=C2C1CC4=CC5=C(C=C43)OCO5)OC)OC
CHEMBL126737 5ht5a_human Human No 6.7 Ki = 225 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
373 5 0 3 4.7 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=C1C(=CC=C4)Cl
CHEMBL338696 5ht5a_mouse Mouse No 6.7 Ki = 225 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
352 5 1 3 3.6 CN1C2=C(CN(CC2)CCCC(C3=CC=C(C=C3)F)O)C4=CC=CC=C41
CHEMBL3770342 5ht5a_human Human No 6.6 Ki = 227 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
336 2 3 2 2.3 C1CCC2(CC1)N=C(NC(=N2)NC3=CC(=CC=C3)Br)N
CHEMBL3770342 5ht5a_human Human No 6.6 Ki = 227 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
336 2 3 2 2.3 C1CCC2(CC1)N=C(NC(=N2)NC3=CC(=CC=C3)Br)N
CHEMBL199824 5ht5a_human Human Yes 6.6 Ki = 228.6 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
423 7 0 6 3.0 CN1C(=O)C=NN(C1=O)CCCCN2CCN(CC2)C3=CC=CC4=C3C=C(C=C4)OC
CHEMBL199824 5ht5a_human Human Yes 6.6 Ki = 228.6 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
423 7 0 6 3.0 CN1C(=O)C=NN(C1=O)CCCCN2CCN(CC2)C3=CC=CC4=C3C=C(C=C4)OC
CHEMBL27441 5ht5a_human Human Yes 5.6 Ki = 2331 Funct
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
233 4 1 2 3.4 CCCNC1CCC2=C(C1C)C=CC=C2OC
CHEMBL2442276 5ht5a_human Human No 5.6 Ki = 2332 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
319 1 2 2 1.8 CN1C(=O)C(=CC2=CNC3=C2C=C(C=C3)Br)N=C1N
CHEMBL134331 5ht5a_rat Rat No 6.6 Ki = 239 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
261 8 0 2 4.2 CCCN(CCC)CC1CC1C2=CC=CC=C2OC
CHEMBL3754166 5ht5a_human Human No 5.6 Ki = 2398.8 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
319 7 1 1 3.5 C=CCN(CCC1=CNC2=C1C=C(C=C2)Br)CC=C
CHEMBL3754166 5ht5a_human Human No 5.6 Ki = 2398.8 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
319 7 1 1 3.5 C=CCN(CCC1=CNC2=C1C=C(C=C2)Br)CC=C
CHEMBL270841 5ht5a_human Human Yes 7.6 Ki = 24 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
175 1 2 1 1.1 CCC1C2=CC=CC=C2NC(=N1)N
CHEMBL270841 5ht5a_human Human Yes 7.6 Ki = 24 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
175 1 2 1 1.1 CCC1C2=CC=CC=C2NC(=N1)N
CHEMBL256048 5ht5a_human Human No 6.6 Ki = 241 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
247 6 2 2 1.7 CCCOCCNC1=NC(C2=CC=CC=C2N1)C
CHEMBL256048 5ht5a_human Human No 6.6 Ki = 241 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
247 6 2 2 1.7 CCCOCCNC1=NC(C2=CC=CC=C2N1)C
CHEMBL269236 5ht5a_mouse Mouse Yes 5.6 Ki = 2470 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
172 0 2 1 1.5 C1CNCC2=C1C3=CC=CC=C3N2
CHEMBL128848 5ht5a_mouse Mouse No 7.6 Ki = 25 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
320 5 0 2 3.9 CN1C2=C(CN(CC2)CCCOC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL187621 5ht5a_human Human No 7.6 Ki = 25.1 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
519 13 1 4 5.3 CN(C)CCN(CC1=CN=C(C=C1)C2=CC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)C=CC4=CC=CC=C4
CHEMBL187621 5ht5a_human Human No 7.6 Ki = 25.1 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
519 13 1 4 5.3 CN(C)CCN(CC1=CN=C(C=C1)C2=CC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)C=CC4=CC=CC=C4
CHEMBL402179 5ht5a_human Human Yes 7.6 Ki = 25.4 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
233 3 2 2 1.7 CC1C2=C(C(=CC=C2)OC(C)C)NC(=N1)NC
CHEMBL402179 5ht5a_human Human Yes 7.6 Ki = 25.4 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
233 3 2 2 1.7 CC1C2=C(C(=CC=C2)OC(C)C)NC(=N1)NC
CHEMBL130585 5ht5a_human Human No 6.6 Ki = 250 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
365 5 0 4 3.8 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)[N+](=O)[O-])C4=CC=CC=C41
CHEMBL126574 5ht5a_mouse Mouse No 6.6 Ki = 250 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
304 4 0 1 4.2 CN1C2=C(CN(CC2)CCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL56 5ht5a_human Human Yes 5.6 Ki = 2500 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
247 5 1 2 4.1 CCCN(CCC)C1CCC2=C(C1)C(=CC=C2)O
CHEMBL56 5ht5a_human Human Yes 5.6 Ki = 2500 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
247 5 1 2 4.1 CCCN(CCC)C1CCC2=C(C1)C(=CC=C2)O
CHEMBL439240 5ht5a_human Human Yes 7.6 Ki = 26.5 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
244 1 2 1 2.4 CCC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)N
CHEMBL439240 5ht5a_human Human Yes 7.6 Ki = 26.5 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
244 1 2 1 2.4 CCC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)N
CHEMBL343755 5ht5a_human Human No 7.6 Ki = 27 Funct
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
335 1 1 2 3.2 CC1CC(N1C(=O)C2CN(C3CC4=CNC5=CC=CC(=C45)C3=C2)C)C
CHEMBL338095 5ht5a_human Human No 6.6 Ki = 270 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
373 5 0 3 4.7 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=C1C=CC(=C4)Cl
CHEMBL403103 5ht5a_human Human No 6.6 Ki = 279 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
286 2 2 2 1.4 CC1C2=CC=CC=C2NC(=N1)NC3CCCCN(C3=O)C
CHEMBL403103 5ht5a_human Human No 6.6 Ki = 279 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
286 2 2 2 1.4 CC1C2=CC=CC=C2NC(=N1)NC3CCCCN(C3=O)C
CHEMBL404248 5ht5a_human Human No 7.6 Ki = 28.2 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
255 4 2 4 1.8 CC1C2=C(C(=CC=C2)OC)NC(=N1)NCC(F)F
CHEMBL404248 5ht5a_human Human No 7.6 Ki = 28.2 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
255 4 2 4 1.8 CC1C2=C(C(=CC=C2)OC)NC(=N1)NCC(F)F
CHEMBL270409 5ht5a_human Human Yes 5.6 Ki = 2800 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
175 1 1 1 0.8 CN(C)C1=NCC2=CC=CC=C2N1
CHEMBL270409 5ht5a_human Human Yes 5.6 Ki = 2800 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
175 1 1 1 0.8 CN(C)C1=NCC2=CC=CC=C2N1
CHEMBL338696 5ht5a_human Human No 6.6 Ki = 285 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
352 5 1 3 3.6 CN1C2=C(CN(CC2)CCCC(C3=CC=C(C=C3)F)O)C4=CC=CC=C41
CHEMBL161507 5ht5a_human Human No 6.5 Ki = 287 Funct
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
261 5 1 3 3.3 CCCNC1CCC2=C(C=CC=C2C1C)C(=O)OC
CHEMBL338081 5ht5a_mouse Mouse No 6.5 Ki = 295 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
334 6 0 2 3.6 CN1C2=C(CN(CC2)CCCOCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL24462 5ht5a_human Human Yes 8.5 Ki = 3 Funct
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
228 1 2 3 1.8 C1CN(CCN1)C2=CC=CC3=C2C=C(C=C3)O
CHEMBL3644533 5ht5a_human Human No 8.5 Ki = 3.3 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
326 2 2 4 2.9 C1=CC=C(C(=C1)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)F
CHEMBL3644533 5ht5a_human Human No 8.5 Ki = 3.3 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
326 2 2 4 2.9 C1=CC=C(C(=C1)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)F
CHEMBL3644534 5ht5a_human Human No 8.5 Ki = 3.4 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
343 2 2 3 3.4 C1=CC=C(C(=C1)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)Cl
CHEMBL3644534 5ht5a_human Human No 8.5 Ki = 3.4 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
343 2 2 3 3.4 C1=CC=C(C(=C1)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F)Cl
CHEMBL3654196 5ht5a_human Human No 8.4 Ki = 3.6 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
348 1 2 4 2.6 C1CN(CC2=C(C=CC=C21)C3=CC(=C(C=C3F)F)F)C(=O)N=C(N)N
CHEMBL3654196 5ht5a_human Human No 8.4 Ki = 3.6 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
348 1 2 4 2.6 C1CN(CC2=C(C=CC=C21)C3=CC(=C(C=C3F)F)F)C(=O)N=C(N)N
CHEMBL3654211 5ht5a_human Human No 8.4 Ki = 3.7 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
366 1 2 5 2.7 C1CN(CC2=C(C=CC(=C21)F)C3=CC(=C(C=C3F)F)F)C(=O)N=C(N)N
CHEMBL3644526 5ht5a_human Human No 8.4 Ki = 3.7 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
372 2 2 5 3.8 CC1=C(N=C2C=CC(=CC2=C1C3=C(C=C(C=C3F)F)F)C(=O)N=C(N)N)C
CHEMBL3654211 5ht5a_human Human No 8.4 Ki = 3.7 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
366 1 2 5 2.7 C1CN(CC2=C(C=CC(=C21)F)C3=CC(=C(C=C3F)F)F)C(=O)N=C(N)N
CHEMBL3644526 5ht5a_human Human No 8.4 Ki = 3.7 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
372 2 2 5 3.8 CC1=C(N=C2C=CC(=CC2=C1C3=C(C=C(C=C3F)F)F)C(=O)N=C(N)N)C
CHEMBL3654203 5ht5a_human Human No 8.4 Ki = 3.9 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
345 1 2 4 1.9 CC1=C2CCN(CC2=C(C=C1)C3=C(C=C(C=N3)F)F)C(=O)N=C(N)N
CHEMBL3654203 5ht5a_human Human No 8.4 Ki = 3.9 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
345 1 2 4 1.9 CC1=C2CCN(CC2=C(C=C1)C3=C(C=C(C=N3)F)F)C(=O)N=C(N)N
CHEMBL252258 5ht5a_human Human No 5.5 Ki = 3000 Funct
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
509 4 2 7 3.6 CC(=O)N1C2CCCC1C=C(C2)CN3C4CCC3CC(C4)NC(=O)NC5=CC(=CC(=C5)C(F)(F)F)F
CHEMBL252258 5ht5a_human Human No 5.5 Ki = 3000 Funct
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
509 4 2 7 3.6 CC(=O)N1C2CCCC1C=C(C2)CN3C4CCC3CC(C4)NC(=O)NC5=CC(=CC(=C5)C(F)(F)F)F
CHEMBL349843 5ht5a_human Human No 5.5 Ki = 3067 Funct
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
351 5 1 7 4.2 CCCNC1CCC2=C(C1C)C=CC=C2OS(=O)(=O)C(F)(F)F
CHEMBL189689 5ht5a_human Human No 7.5 Ki = 31.6 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
513 14 1 4 5.7 CN(C)CCN(CC1=CN=C(C=C1)C2=CC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)CCC4CCCC4
CHEMBL189689 5ht5a_human Human No 7.5 Ki = 31.6 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
513 14 1 4 5.7 CN(C)CCN(CC1=CN=C(C=C1)C2=CC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)CCC4CCCC4
CHEMBL336124 5ht5a_rat Rat No 6.5 Ki = 310 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
261 8 0 2 4.2 CCCN(CCC)CC1CC1C2=CC(=CC=C2)OC
CHEMBL425190 5ht5a_human Human Yes 5.5 Ki = 3162.3 Funct
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
413 6 0 5 4.2 CC1=NC2=C(C=C1)C(=CC=C2)OCCN3CCN(CC3)CC4=CC=CC5=C4N=CC=C5
CHEMBL425190 5ht5a_human Human Yes 5.5 Ki = 3162.3 Funct
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
413 6 0 5 4.2 CC1=NC2=C(C=C1)C(=CC=C2)OCCN3CCN(CC3)CC4=CC=CC5=C4N=CC=C5
CHEMBL269236 5ht5a_human Human Yes 5.5 Ki = 3200 Funct
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
172 0 2 1 1.5 C1CNCC2=C1C3=CC=CC=C3N2
CHEMBL3753318 5ht5a_human Human No 5.5 Ki = 3235.9 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
254 7 1 1 3.7 CC1=CC2=C(C=C1)NC=C2CCN(CC=C)CC=C
CHEMBL3753318 5ht5a_human Human No 5.5 Ki = 3235.9 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
254 7 1 1 3.7 CC1=CC2=C(C=C1)NC=C2CCN(CC=C)CC=C
CHEMBL1336 5ht5a_human Human Yes 5.5 Ki = 3296 Funct
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
465 5 3 7 4.1 CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
CHEMBL271253 5ht5a_human Human No 7.5 Ki = 33.4 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
294 3 2 3 3.1 CC1C2=C(C=CC(=C2NC(=N1)NCC(F)F)Cl)Cl
CHEMBL271253 5ht5a_human Human No 7.5 Ki = 33.4 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
294 3 2 3 3.1 CC1C2=C(C=CC(=C2NC(=N1)NCC(F)F)Cl)Cl
CHEMBL2111848 5ht5a_mouse Mouse No 6.5 Ki = 330 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
330 5 0 1 4.6 CN1C2=C(CN(CC2)CC=CCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL2391541 5ht5a_human Human Yes 5.5 Ki = 3311.3 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
270 8 1 2 2.8 COC1=CC2=C(C=C1)NC=C2CCN(CC=C)CC=C
CHEMBL2391541 5ht5a_human Human Yes 5.5 Ki = 3311.3 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
270 8 1 2 2.8 COC1=CC2=C(C=C1)NC=C2CCN(CC=C)CC=C
CHEMBL2058706 5ht5a_human Human No 5.5 Ki = 3324 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
319 2 3 1 2.0 CNC1=NC(=O)C(=CC2=CNC3=C2C=CC=C3Br)N1
CHEMBL424258 5ht5a_mouse Mouse No 6.5 Ki = 335 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
306 5 1 2 4.0 C1CN(CC2=C1C3=CC=CC=C3N2)CCCOC4=CC=CC=C4
CHEMBL2058703 5ht5a_human Human No 5.5 Ki = 3372 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
319 2 3 1 2.0 CNC1=NC(=O)C(=CC2=CNC3=C2C(=CC=C3)Br)N1
CHEMBL126138 5ht5a_human Human No 6.5 Ki = 340 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
365 5 1 4 3.9 CN1C2=C(CN(CC2)CCCC(=NO)C3=CC=C(C=C3)F)C4=CC=CC=C41
CHEMBL92139 5ht5a_rat Rat No 5.5 Ki = 3400 Funct
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
328 5 0 3 3.5 CN(C)CCC1=C2C=CN(C2=CC=C1)S(=O)(=O)C3=CC=CC=C3
CHEMBL340646 5ht5a_human Human No 6.5 Ki = 350 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
350 6 0 3 3.9 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)OC)C4=CC=CC=C41
CHEMBL446356 5ht5a_mouse Mouse No 6.5 Ki = 350 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
330 5 0 1 4.6 CN1C2=C(CN(CC2)CC=CCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL126823 5ht5a_mouse Mouse No 6.4 Ki = 360 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
320 5 0 2 3.9 CN1C2=C(CCN(C2)CCCOC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL256693 5ht5a_human Human No 7.4 Ki = 37 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
309 3 2 3 2.5 CC1C2=CC=CC=C2NC(=N1)NCC3COC4=CC=CC=C4O3
CHEMBL256693 5ht5a_human Human No 7.4 Ki = 37 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
309 3 2 3 2.5 CC1C2=CC=CC=C2NC(=N1)NCC3COC4=CC=CC=C4O3
CHEMBL133433 5ht5a_rat Rat No 6.4 Ki = 379 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
247 7 1 2 3.8 CCCN(CCC)CC1CC1C2=CC=CC=C2O
CHEMBL133935 5ht5a_rat Rat No 6.4 Ki = 388 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
261 8 0 2 4.2 CCCN(CCC)CC1CC1C2=CC(=CC=C2)OC
CHEMBL582877 5ht5a_human Human Yes 6.4 Ki = 389 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
296 2 3 2 1.3 CC1(N=C(NC(=N1)NC2=CC(=CC=C2)Br)N)C
CHEMBL582877 5ht5a_human Human Yes 6.4 Ki = 389 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
296 2 3 2 1.3 CC1(N=C(NC(=N1)NC2=CC(=CC=C2)Br)N)C
CHEMBL257450 5ht5a_human Human No 6.4 Ki = 397 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
207 3 2 2 1.3 CC1C2=CC=CC=C2NC(=N1)NCCF
CHEMBL257450 5ht5a_human Human No 6.4 Ki = 397 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
207 3 2 2 1.3 CC1C2=CC=CC=C2NC(=N1)NCCF
CHEMBL3644529 5ht5a_human Human No 8.4 Ki = 4.1 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.5 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2F)C3=C(C=C(C=C3)F)Cl
CHEMBL3644529 5ht5a_human Human No 8.4 Ki = 4.1 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
361 2 2 4 3.5 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2F)C3=C(C=C(C=C3)F)Cl
CHEMBL3654213 5ht5a_human Human No 8.4 Ki = 4.2 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
331 1 2 4 1.5 C1CN(CC2=C(C=CC=C21)C3=C(C=C(C=N3)F)F)C(=O)N=C(N)N
CHEMBL3654213 5ht5a_human Human No 8.4 Ki = 4.2 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
331 1 2 4 1.5 C1CN(CC2=C(C=CC=C21)C3=C(C=C(C=N3)F)F)C(=O)N=C(N)N
CHEMBL3654195 5ht5a_human Human No 8.4 Ki = 4.3 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
366 1 2 4 2.1 C1CN(CC2=C(C=CC(=C21)F)C3=NC=C(C=C3F)Cl)C(=O)N=C(N)N
CHEMBL3654195 5ht5a_human Human No 8.4 Ki = 4.3 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
366 1 2 4 2.1 C1CN(CC2=C(C=CC(=C21)F)C3=NC=C(C=C3F)Cl)C(=O)N=C(N)N
CHEMBL3644539 5ht5a_human Human No 8.3 Ki = 4.6 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
376 3 2 6 3.5 C1=CC(=C(C(=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)C(F)F)F
CHEMBL3644539 5ht5a_human Human No 8.3 Ki = 4.6 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
376 3 2 6 3.5 C1=CC(=C(C(=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)C(F)F)F
CHEMBL3644536 5ht5a_human Human No 8.3 Ki = 4.7 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
362 2 2 5 2.4 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2F)C3=C(C=NC=C3F)Cl
CHEMBL401745 5ht5a_human Human No 8.3 Ki = 4.7 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
240 1 2 2 1.5 CC1C2=C(C(=CC(=C2C)Cl)OC)NC(=N1)N
CHEMBL3644536 5ht5a_human Human No 8.3 Ki = 4.7 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
362 2 2 5 2.4 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2F)C3=C(C=NC=C3F)Cl
CHEMBL401745 5ht5a_human Human No 8.3 Ki = 4.7 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
240 1 2 2 1.5 CC1C2=C(C(=CC(=C2C)Cl)OC)NC(=N1)N
CHEMBL37844 5ht5a_rat Rat No 8.3 Ki = 4.9 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
233 6 1 2 3.6 CCCN(CCC)C1CC1C2=CC=CC=C2O
CHEMBL277120 5ht5a_human Human Yes 7.4 Ki = 40 Funct
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
212 1 1 2 2.6 C1CN(CCN1)C2=CC=CC3=CC=CC=C32
CHEMBL277120 5ht5a_mouse Mouse Yes 7.4 Ki = 40 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand
212 1 1 2 2.6 C1CN(CCN1)C2=CC=CC3=CC=CC=C32
CHEMBL126667 5ht5a_human Human No 6.4 Ki = 400 Funct
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
285 5 0 3 3.9 C1CN(CC2=CC=CC=C21)CCCOC3=CC=C(C=C3)F
CHEMBL93868 5ht5a_rat Rat No 5.4 Ki = 4000 Funct
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
328 5 0 3 3.5 CN(C)CCC1=CN(C2=CC=CC=C21)S(=O)(=O)C3=CC=CC=C3
CHEMBL441896 5ht5a_human Human No 6.4 Ki = 415 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL441896 5ht5a_human Human No 6.4 Ki = 415 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL3754496 5ht5a_human Human No 5.4 Ki = 4265.8 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
258 7 1 2 2.9 C=CCN(CCC1=CNC2=C1C=C(C=C2)F)CC=C
CHEMBL3754496 5ht5a_human Human No 5.4 Ki = 4265.8 Funct
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
258 7 1 2 2.9 C=CCN(CCC1=CNC2=C1C=C(C=C2)F)CC=C
CHEMBL1548 5ht5a_human Human Yes 7.4 Ki = 43 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
216 0 2 1 1.4 C1C2=C(C=CC(=C2Cl)Cl)NC(=N1)N
CHEMBL1548 5ht5a_human Human Yes 7.4 Ki = 43 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
216 0 2 1 1.4 C1C2=C(C=CC(=C2Cl)Cl)NC(=N1)N
CHEMBL423527 5ht5a_rat Rat No 6.4 Ki = 431 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
233 6 0 2 3.1 CCN(CC)CC1CC1C2=CC=CC=C2OC
CHEMBL125361 5ht5a_mouse Mouse No 6.4 Ki = 435 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
347 7 0 1 5.7 CN1C2=C(CN(CC2)CCCCCCC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL263700 5ht5a_rat Rat No 5.4 Ki = 4500 Funct
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
308 4 1 3 3.5 CN(C)CCC1=CN(C2=C1C=C(C=C2)O)C(=O)C3=CC=CC=C3
CHEMBL3770106 5ht5a_human Human Yes 6.3 Ki = 457 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
329 5 3 4 1.8 CCOC(=O)C1=CC(=CC=C1)NC2=NC3(CCCCC3)N=C(N2)N
CHEMBL3770106 5ht5a_human Human Yes 6.3 Ki = 457 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
329 5 3 4 1.8 CCOC(=O)C1=CC(=CC=C1)NC2=NC3(CCCCC3)N=C(N2)N
CHEMBL267615 5ht5a_human Human Yes 5.3 Ki = 4620 Funct
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
246 5 1 2 3.2 CCC1=C(C2=C(N1)C=CC(=C2)OC)CCN(C)C
CHEMBL2058428 5ht5a_human Human No 5.3 Ki = 4681 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
347 1 1 2 2.4 CN=C1N(C(=CC2=CNC3=C2C=CC(=C3)Br)C(=O)N1C)C
CHEMBL429925 5ht5a_human Human No 6.3 Ki = 488 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
243 2 2 4 2.1 CC1C2=CC=CC=C2NC(=N1)NCC(F)(F)F
CHEMBL429925 5ht5a_human Human No 6.3 Ki = 488 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
243 2 2 4 2.1 CC1C2=CC=CC=C2NC(=N1)NCC(F)(F)F
CHEMBL270177 5ht5a_human Human Yes 8.3 Ki = 5.0 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL270177 5ht5a_human Human Yes 8.3 Ki = 5.0 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL361256 5ht5a_human Human No 8.3 Ki = 5.0 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
519 13 1 4 5.3 CN(C)CCN(CC1=CC=C(C=C1)C2=NC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)C=CC4=CC=CC=C4
CHEMBL361256 5ht5a_human Human No 8.3 Ki = 5.0 Funct
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
519 13 1 4 5.3 CN(C)CCN(CC1=CC=C(C=C1)C2=NC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)C=CC4=CC=CC=C4
CHEMBL270177 5ht5a_human Human Yes 8.3 Ki = 5.1 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL270177 5ht5a_human Human Yes 8.3 Ki = 5.1 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL270177 5ht5a_human Human Yes 8.3 Ki = 5.1 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
196 0 2 1 1.2 CC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL3644531 5ht5a_human Human No 8.3 Ki = 5.3 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
345 2 2 6 1.9 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2F)C3=C(C=NC=C3F)F
CHEMBL3644531 5ht5a_human Human No 8.3 Ki = 5.3 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
345 2 2 6 1.9 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2F)C3=C(C=NC=C3F)F
CHEMBL429136 5ht5a_human Human No 8.2 Ki = 5.7 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
294 3 2 3 3.1 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)NCC(F)F
CHEMBL429136 5ht5a_human Human No 8.2 Ki = 5.7 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
294 3 2 3 3.1 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)NCC(F)F
CHEMBL96729 5ht5a_human Human No 5.3 Ki = 5000 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
281 5 2 4 0.5 CNS(=O)(=O)C1=CC2=C(C=C1)NC=C2CCN(C)C
CHEMBL96729 5ht5a_human Human No 5.3 Ki = 5000 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
281 5 2 4 0.5 CNS(=O)(=O)C1=CC2=C(C=C1)NC=C2CCN(C)C
CHEMBL256047 5ht5a_human Human No 6.3 Ki = 504 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
294 3 2 3 3.1 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)NCC(F)F
CHEMBL256047 5ht5a_human Human No 6.3 Ki = 504 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
294 3 2 3 3.1 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)NCC(F)F
CHEMBL341373 5ht5a_rat Rat No 6.3 Ki = 506 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
219 5 1 2 2.8 CCN(CC)CC1CC1C2=CC=CC=C2O
CHEMBL2058426 5ht5a_human Human No 5.3 Ki = 5080 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
347 1 1 2 2.4 CN=C1N(C(=CC2=CNC3=C2C(=CC=C3)Br)C(=O)N1C)C
CHEMBL338091 5ht5a_mouse Mouse Yes 6.3 Ki = 512 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
336 5 1 3 3.7 C1CN(CC2=C1NC3=CC=CC=C23)CCCC(=O)C4=CC=C(C=C4)F
CHEMBL7318 5ht5a_human Human Yes 5.3 Ki = 5160 Funct
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
294 5 1 2 4.0 CN(C)CCC1=C(NC2=C1C=C(C=C2)OC)C3=CC=CC=C3
CHEMBL3326993 5ht5a_human Human No 6.3 Ki = 517 Funct
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
506 11 1 4 5.9 COC1=CC=CC=C1N2CCN(CC2)CCCCCC(=O)NCC3=CC=CC=C3C4=CC=CC=C4Cl
CHEMBL3326993 5ht5a_human Human No 6.3 Ki = 517 Funct
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
506 11 1 4 5.9 COC1=CC=CC=C1N2CCN(CC2)CCCCCC(=O)NCC3=CC=CC=C3C4=CC=CC=C4Cl
CHEMBL92879 5ht5a_mouse Mouse Yes 5.3 Ki = 5300 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
186 0 1 1 1.4 CN1C2=C(CNCC2)C3=CC=CC=C31
CHEMBL92879 5ht5a_mouse Mouse Yes 5.3 Ki = 5300 Funct
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
186 0 1 1 1.4 CN1C2=C(CNCC2)C3=CC=CC=C31
CHEMBL511879 5ht5a_human Human Yes 5.3 Ki = 5355 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
319 1 2 2 1.8 CN1C(=O)C(=CC2=CNC3=C2C=CC(=C3)Br)N=C1N
CHEMBL96504 5ht5a_human Human No 7.3 Ki = 55 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
338 5 0 3 4.0 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=CC=CC=C41
CHEMBL96504 5ht5a_human Human No 7.3 Ki = 55 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
338 5 0 3 4.0 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=CC=CC=C41
CHEMBL129163 5ht5a_mouse Mouse No 6.3 Ki = 550 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
318 5 1 2 3.6 C1CN(CC2=C1C3=CC=CC=C3N2)CCCC(=O)C4=CC=CC=C4
CHEMBL464099 5ht5a_human Human Yes 6.3 Ki = 566 Funct
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assay
341 3 1 5 3.0 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)OC
CHEMBL464099 5ht5a_human Human Yes 6.3 Ki = 566 Funct
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assay
341 3 1 5 3.0 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)OC
CHEMBL132123 5ht5a_rat Rat No 7.2 Ki = 58 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
247 7 1 2 3.8 CCCN(CCC)CC1CC1C2=CC(=CC=C2)O
CHEMBL2181169 5ht5a_human Human No 5.2 Ki = 5805 Funct
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
460 5 0 3 6.1 CCCN1CCC(CC1)COC2=NC3=C(C=CC=C3I)C4=CC=CC=C42
CHEMBL126737 5ht5a_mouse Mouse No 6.2 Ki = 590 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
373 5 0 3 4.7 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=C1C(=CC=C4)Cl
CHEMBL3770981 5ht5a_human Human No 6.2 Ki = 595 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
357 6 2 4 2.4 CCOC(=O)C1=CC(=CC=C1)NC2=NC3(CCCCC3)N=C(N2)N(C)C
CHEMBL3770981 5ht5a_human Human No 6.2 Ki = 595 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
357 6 2 4 2.4 CCOC(=O)C1=CC(=CC=C1)NC2=NC3(CCCCC3)N=C(N2)N(C)C
CHEMBL3644538 5ht5a_human Human No 8.2 Ki = 6.2 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
362 2 2 5 2.5 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2F)C3=C(C=C(C=N3)F)Cl
CHEMBL3644538 5ht5a_human Human No 8.2 Ki = 6.2 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
362 2 2 5 2.5 C1=CC2=C(C=C1C(=O)N=C(N)N)C(=NC=C2F)C3=C(C=C(C=N3)F)Cl
CHEMBL408152 5ht5a_human Human No 8.2 Ki = 6.3 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
191 1 2 2 0.5 CC1C2=C(C(=CC=C2)OC)NC(=N1)N
CHEMBL271298 5ht5a_human Human Yes 8.2 Ki = 6.3 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
244 1 2 1 2.2 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)NC
CHEMBL408152 5ht5a_human Human No 8.2 Ki = 6.3 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
191 1 2 2 0.5 CC1C2=C(C(=CC=C2)OC)NC(=N1)N
CHEMBL271298 5ht5a_human Human Yes 8.2 Ki = 6.3 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
244 1 2 1 2.2 CC1C2=C(C=CC(=C2Cl)Cl)NC(=N1)NC
CHEMBL404511 5ht5a_human Human Yes 8.2 Ki = 6.3 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL404511 5ht5a_human Human Yes 8.2 Ki = 6.3 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL272781 5ht5a_human Human No 8.2 Ki = 6.5 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
230 0 2 1 1.8 CC1C2=C(C=CC(=C2NC(=N1)N)Cl)Cl
CHEMBL272781 5ht5a_human Human No 8.2 Ki = 6.5 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
230 0 2 1 1.8 CC1C2=C(C=CC(=C2NC(=N1)N)Cl)Cl
CHEMBL3654202 5ht5a_human Human No 8.2 Ki = 6.6 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
383 1 2 4 3.1 C1C(C2=C(C=CC(=C2CN1C(=O)N=C(N)N)C3=C(C=C(C=C3)F)F)Cl)F
CHEMBL3654202 5ht5a_human Human No 8.2 Ki = 6.6 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
383 1 2 4 3.1 C1C(C2=C(C=CC(=C2CN1C(=O)N=C(N)N)C3=C(C=C(C=C3)F)F)Cl)F
CHEMBL541993 5ht5a_human Human No 8.2 Ki = 6.8 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL541993 5ht5a_human Human No 8.2 Ki = 6.8 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
260 3 2 3 2.5 CC1C2=C(C=CC=C2Cl)NC(=N1)NCC(F)F
CHEMBL3654201 5ht5a_human Human No 8.2 Ki = 6.9 Funct
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
349 1 2 5 1.6 C1CN(CC2=C(C=CC(=C21)F)C3=C(C=C(C=N3)F)F)C(=O)N=C(N)N
CHEMBL3654201 5ht5a_human Human No 8.2 Ki = 6.9 Funct
BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).BindingDB_Patents: Binding Assay. A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
349 1 2 5 1.6 C1CN(CC2=C(C=CC(=C21)F)C3=C(C=C(C=N3)F)F)C(=O)N=C(N)N
CHEMBL126438 5ht5a_mouse Mouse No 6.2 Ki = 600 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
306 5 1 2 4.0 C1CN(CC2=C1NC3=CC=CC=C23)CCCOC4=CC=CC=C4
CHEMBL2429890 5ht5a_human Human No 5.2 Ki = 6060 Funct
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
295 3 1 3 3.4 C1C2C3CC4C2C5C1C3C(C45)NCC6=CC7=C(C=C6)OCO7
CHEMBL126823 5ht5a_human Human No 6.2 Ki = 620 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
320 5 0 2 3.9 CN1C2=C(CCN(C2)CCCOC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL97518 5ht5a_mouse Mouse No 7.2 Ki = 63 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
367 5 3 3 2.9 CCC(C)(CNC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C)CO
CHEMBL13816 5ht5a_human Human No 6.2 Ki = 630 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
389 5 2 3 3.8 CN1CC(CC2C1CC3=CNC4=CC=CC2=C34)CNC(=O)OCC5=CC=CC=C5
CHEMBL126188 5ht5a_mouse Mouse No 6.2 Ki = 650 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
370 5 0 2 5.2 CN1C2=C(CN(CC2)CCCOC3=CC=CC4=CC=CC=C43)C5=CC=CC=C51
CHEMBL340511 5ht5a_mouse Mouse No 6.2 Ki = 655 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
370 5 0 2 5.2 CN1C2=C(CN(CC2)CCCOC3=CC4=CC=CC=C4C=C3)C5=CC=CC=C51
CHEMBL1170237 5ht5a_human Human No 5.2 Ki = 6725 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
333 1 2 2 2.4 CN1C(=CC2=CNC3=C2C=C(C=C3)Br)C(=O)N(C1=N)C
CHEMBL515472 5ht5a_human Human No 5.2 Ki = 6814 Funct
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
405 9 1 6 4.2 COC1=C(C=CC=C1OCCF)C(C2CCN(CC2)CCC3=CC=C(C=C3)F)O
CHEMBL515472 5ht5a_human Human No 5.2 Ki = 6814 Funct
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
405 9 1 6 4.2 COC1=C(C=CC=C1OCCF)C(C2CCN(CC2)CCC3=CC=C(C=C3)F)O
CHEMBL2058429 5ht5a_human Human No 5.2 Ki = 6913 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
347 1 1 2 2.4 CN=C1N(C(=CC2=CNC3=C2C=CC=C3Br)C(=O)N1C)C
CHEMBL3644532 5ht5a_human Human No 8.2 Ki = 7.1 Funct
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
356 3 2 5 2.9 COC1=C(C(=CC=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F
CHEMBL3644532 5ht5a_human Human No 8.2 Ki = 7.1 Funct
BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.BindingDB_Patents: Binding Inhibition Assay. A solution of the compound to be tested and 100 µM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 µl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 µl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 µl/well.Separately, 100 µl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
356 3 2 5 2.9 COC1=C(C(=CC=C1)F)C2=NC=C(C3=C2C=C(C=C3)C(=O)N=C(N)N)F
CHEMBL334553 5ht5a_rat Rat No 6.1 Ki = 736 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
247 7 0 2 4.0 CCCN(CCC)C1CC1C2=CC(=CC=C2)OC
CHEMBL126724 5ht5a_mouse Mouse No 7.1 Ki = 75 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
324 5 1 3 4.1 C1CN(CC2=C1NC3=CC=CC=C23)CCCOC4=CC=C(C=C4)F
CHEMBL128099 5ht5a_mouse Mouse No 7.1 Ki = 75 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
334 6 0 2 4.2 CCN1C2=C(CN(CC2)CCCOC3=CC=CC=C3)C4=CC=CC=C41
CHEMBL3104091 5ht5a_human Human No 6.1 Ki = 750 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
288 0 0 1 3.9 CN1CCC2=C(C1)C3=C4N2C5=CC=CC=C5CCC4=CC=C3
CHEMBL2432039 5ht5a_human Human No 5.1 Ki = 7502 Funct
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
277 3 1 1 2.7 C1C2C3CC4C2C5C1C3C(C45)NCC67C8C9C6C1C9C8C71
CHEMBL133020 5ht5a_rat Rat No 6.1 Ki = 752 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
247 7 1 2 3.8 CCCN(CCC)CC1CC1C2=CC=CC=C2O
CHEMBL2205811 5ht5a_human Human No 5.1 Ki = 7815 Funct
Binding affinity to 5-HT5A receptorBinding affinity to 5-HT5A receptor
309 4 1 3 2.8 COC1=CC=CC(=C1)CCN2C3C4C5CC6C4C2(C7C6C5C73)O
CHEMBL2058419 5ht5a_human Human No 5.1 Ki = 7828 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
333 1 2 2 2.4 CN1C(=CC2=CNC3=C2C(=CC=C3)Br)C(=O)N(C1=N)C
CHEMBL270840 5ht5a_human Human Yes 6.1 Ki = 805 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
189 2 2 1 1.5 CCCC1C2=CC=CC=C2NC(=N1)N
CHEMBL270840 5ht5a_human Human Yes 6.1 Ki = 805 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
189 2 2 1 1.5 CCCC1C2=CC=CC=C2NC(=N1)N
CHEMBL270176 5ht5a_human Human Yes 7.1 Ki = 84.4 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
210 1 2 1 1.7 CCC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL270176 5ht5a_human Human Yes 7.1 Ki = 84.4 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
210 1 2 1 1.7 CCC1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL295234 5ht5a_human Human Yes 6.1 Ki = 845 Funct
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
184 0 1 2 1.5 CC1=C2C(=C3C=CC=CC3=N2)CCN1
CHEMBL1258223 5ht5a_human Human No 5.1 Ki = 8589 Funct
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
397 8 1 6 4.1 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)NC)Cl
CHEMBL1258223 5ht5a_human Human No 5.1 Ki = 8589 Funct
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
397 8 1 6 4.1 CCCCN1CCC(CC1)COC(=O)C2=CC(=C(C3=C2OCCO3)NC)Cl
CHEMBL272355 5ht5a_human Human No 7.1 Ki = 87 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
225 3 2 3 1.8 CC1C2=CC=CC=C2NC(=N1)NCC(F)F
CHEMBL272355 5ht5a_human Human No 7.1 Ki = 87 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
225 3 2 3 1.8 CC1C2=CC=CC=C2NC(=N1)NCC(F)F
CHEMBL130586 5ht5a_mouse Mouse No 6.1 Ki = 875 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
397 7 0 2 5.5 C1CN(CC2=C1N(C3=CC=CC=C23)CC4=CC=CC=C4)CCCOC5=CC=CC=C5
CHEMBL2442272 5ht5a_human Human No 7.1 Ki = 89 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
305 1 3 1 1.6 C1=CC2=C(C=C1Br)C(=CN2)C=C3C(=O)N=C(N3)N
CHEMBL272752 5ht5a_human Human Yes 6.1 Ki = 892 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
182 0 2 1 0.8 C1C2=C(C(=CC=C2)Cl)NC(=N1)N
CHEMBL272752 5ht5a_human Human Yes 6.1 Ki = 892 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
182 0 2 1 0.8 C1C2=C(C(=CC=C2)Cl)NC(=N1)N
CHEMBL128945 5ht5a_mouse Mouse No 7.1 Ki = 90 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
348 6 0 2 4.5 CN1C2=C(CN(CC2)CCCCC3=CC=C(C=C3)OC)C4=CC=CC=C41
CHEMBL2058427 5ht5a_human Human No 5.0 Ki = 9118 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
347 1 1 2 2.4 CN=C1N(C(=CC2=CNC3=C2C=C(C=C3)Br)C(=O)N1C)C
CHEMBL126994 5ht5a_human Human No 6.0 Ki = 930 Funct
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
324 4 0 3 3.7 CN1C2=C(CN(CC2)CCOC3=CC=C(C=C3)F)C4=CC=CC=C41
CHEMBL341506 5ht5a_mouse Mouse No 7.0 Ki = 95 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
336 5 0 2 4.7 CN1C2=C(CN(CC2)CCCCC3=CC=C(C=C3)F)C4=CC=CC=C41
CHEMBL404365 5ht5a_human Human No 7.0 Ki = 96 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
261 3 2 3 0.5 CC1C2=CC=CC=C2NC(=N1)NCC3COCCO3
CHEMBL404365 5ht5a_human Human No 7.0 Ki = 96 Funct
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
261 3 2 3 0.5 CC1C2=CC=CC=C2NC(=N1)NCC3COCCO3
CHEMBL463249 5ht5a_human Human Yes 5.0 Ki = 9621 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
333 1 2 2 2.4 CN1C(=CC2=CNC3=C2C=CC(=C3)Br)C(=O)N(C1=N)C
CHEMBL128185 5ht5a_mouse Mouse No 7.0 Ki = 98 Funct
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
368 6 0 4 4.0 CN1C2=C(CN(CC2)CCCOC3=CC=C(C=C3)F)C4=C1C=CC(=C4)OC
CHEMBL401541 5ht5a_human Human No 7.0 Ki = 99 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
182 0 2 1 0.8 C1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL401541 5ht5a_human Human No 7.0 Ki = 99 Funct
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
182 0 2 1 0.8 C1C2=C(C=CC=C2Cl)NC(=N1)N
CHEMBL3771331 5ht5a_human Human No 6.0 Ki = 994 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
328 4 4 3 1.2 CCNC(=O)C1=CC(=CC=C1)NC2=NC3(CCCCC3)N=C(N2)N
CHEMBL3771331 5ht5a_human Human No 6.0 Ki = 994 Funct
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
328 4 4 3 1.2 CCNC(=O)C1=CC(=CC=C1)NC2=NC3(CCCCC3)N=C(N2)N
CHEMBL135894 5ht5a_rat Rat No 6.0 Ki = 998 Funct
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
261 8 0 2 4.2 CCCN(CCC)CC1CC1C2=CC=CC=C2OC