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
«

Versions

Package Name Version
Django 2.2.1
Python 3.6.7
debug_toolbar Debug Toolbar 1.11
polymorphic Polymorphic 2.0.3
rest_framework Django REST framework 3.9.3
rest_framework_swagger Rest_Framework_Swagger 2.2.0

Time

Resource usage

Resource Value
User CPU time 1738.781 msec
System CPU time 203.592 msec
Total CPU time 1942.373 msec
Elapsed time 2393.117 msec
Context switches 469 voluntary, 14 involuntary

Browser timing

Timing attribute Timeline Milliseconds since navigation start (+length)

Settings from protwis.settings

Setting Value
ABSOLUTE_URL_OVERRIDES {}
ADMINS []
ALLOWED_HOSTS ['*']
APPEND_SLASH True
AUTHENTICATION_BACKENDS ['django.contrib.auth.backends.ModelBackend']
AUTH_PASSWORD_VALIDATORS '********************'
AUTH_USER_MODEL 'auth.User'
BASE_DIR '/home/protwis/gpcrdb_test'
BUILD_CACHE_DIR '/home/protwis/gpcrdb_data/cache'
CACHES {'alignments': {'BACKEND': 'django.core.cache.backends.filebased.FileBasedCache', 'LOCATION': '/home/protwis/caches/test_alignment', 'OPTIONS': {'MAX_ENTRIES': 1000}}, 'default': {'BACKEND': 'django.core.cache.backends.filebased.FileBasedCache', 'LOCATION': '/home/protwis/caches/test/', 'OPTIONS': {'MAX_ENTRIES': 10000000}}}
CACHE_MIDDLEWARE_ALIAS 'default'
CACHE_MIDDLEWARE_KEY_PREFIX '********************'
CACHE_MIDDLEWARE_SECONDS 600
CSRF_COOKIE_AGE 31449600
CSRF_COOKIE_DOMAIN None
CSRF_COOKIE_HTTPONLY False
CSRF_COOKIE_NAME 'csrftoken'
CSRF_COOKIE_PATH '/'
CSRF_COOKIE_SAMESITE 'Lax'
CSRF_COOKIE_SECURE False
CSRF_FAILURE_VIEW 'django.views.csrf.csrf_failure'
CSRF_HEADER_NAME 'HTTP_X_CSRFTOKEN'
CSRF_TRUSTED_ORIGINS []
CSRF_USE_SESSIONS False
DATABASES {'default': {'ATOMIC_REQUESTS': False, 'AUTOCOMMIT': True, 'CONN_MAX_AGE': 0, 'ENGINE': 'django.db.backends.postgresql_psycopg2', 'HOST': 'localhost', 'NAME': 'protwis_202107', 'OPTIONS': {}, 'PASSWORD': '********************', 'PORT': '', 'TEST': {'CHARSET': None, 'COLLATION': None, 'MIRROR': None, 'NAME': None}, 'TIME_ZONE': None, 'USER': 'protwis'}}
DATABASE_ROUTERS []
DATA_DIR '/home/protwis/gpcrdb_data'
DATA_UPLOAD_MAX_MEMORY_SIZE 2621440
DATA_UPLOAD_MAX_NUMBER_FIELDS 1000
DATETIME_FORMAT 'N j, Y, P'
DATETIME_INPUT_FORMATS ['%Y-%m-%d %H:%M:%S', '%Y-%m-%d %H:%M:%S.%f', '%Y-%m-%d %H:%M', '%Y-%m-%d', '%m/%d/%Y %H:%M:%S', '%m/%d/%Y %H:%M:%S.%f', '%m/%d/%Y %H:%M', '%m/%d/%Y', '%m/%d/%y %H:%M:%S', '%m/%d/%y %H:%M:%S.%f', '%m/%d/%y %H:%M', '%m/%d/%y']
DATE_FORMAT 'N j, Y'
DATE_INPUT_FORMATS ['%Y-%m-%d', '%m/%d/%Y', '%m/%d/%y', '%b %d %Y', '%b %d, %Y', '%d %b %Y', '%d %b, %Y', '%B %d %Y', '%B %d, %Y', '%d %B %Y', '%d %B, %Y']
DEBUG True
DEBUG_PROPAGATE_EXCEPTIONS False
DEBUG_TOOLBAR_PATCH_SETTINGS False
DECIMAL_SEPARATOR '.'
DEFAULT_CHARSET 'utf-8'
DEFAULT_CONTENT_TYPE 'text/html'
DEFAULT_EXCEPTION_REPORTER_FILTER 'django.views.debug.SafeExceptionReporterFilter'
DEFAULT_FILE_STORAGE 'django.core.files.storage.FileSystemStorage'
DEFAULT_FROM_EMAIL 'webmaster@localhost'
DEFAULT_INDEX_TABLESPACE ''
DEFAULT_NUMBERING_SCHEME 'gpcrdb'
DEFAULT_PROTEIN_STATE 'inactive'
DEFAULT_SITE 'gpcr'
DEFAULT_TABLESPACE ''
DISALLOWED_USER_AGENTS []
DOCUMENTATION_URL 'https://docs.gpcrdb.org/'
EMAIL_BACKEND 'django.core.mail.backends.smtp.EmailBackend'
EMAIL_HOST 'localhost'
EMAIL_HOST_PASSWORD '********************'
EMAIL_HOST_USER ''
EMAIL_PORT 25
EMAIL_SSL_CERTFILE None
EMAIL_SSL_KEYFILE '********************'
EMAIL_SUBJECT_PREFIX '[Django] '
EMAIL_TIMEOUT None
EMAIL_USE_LOCALTIME False
EMAIL_USE_SSL False
EMAIL_USE_TLS False
FILE_CHARSET 'utf-8'
FILE_UPLOAD_DIRECTORY_PERMISSIONS None
FILE_UPLOAD_HANDLERS ['django.core.files.uploadhandler.MemoryFileUploadHandler', 'django.core.files.uploadhandler.TemporaryFileUploadHandler']
FILE_UPLOAD_MAX_MEMORY_SIZE 2621440
FILE_UPLOAD_PERMISSIONS None
FILE_UPLOAD_TEMP_DIR None
FIRST_DAY_OF_WEEK 0
FIXTURE_DIRS []
FORCE_SCRIPT_NAME None
FORMAT_MODULE_PATH None
FORM_RENDERER 'django.forms.renderers.DjangoTemplates'
GOOGLE_ANALYTICS_API '********************'
GOOGLE_ANALYTICS_KEY '********************'
IGNORABLE_404_URLS []
INSTALLED_APPS ('django.contrib.admin', 'django.contrib.auth', 'django.contrib.contenttypes', 'django.contrib.sessions', 'django.contrib.messages', 'django.contrib.staticfiles', 'django.contrib.humanize', 'debug_toolbar', 'rest_framework', 'rest_framework_swagger', 'polymorphic', 'common', 'api', 'news', 'pages', 'home', 'protein', 'family', 'residue', 'alignment', 'similaritysearch', 'similaritymatrix', 'structure', 'ligand', 'interaction', 'mutation', 'phylogenetic_trees', 'sitesearch', 'build_gpcr', 'construct', 'tools', 'drugs', 'signprot', 'signprot2', 'mutational_landscape', 'contactnetwork', 'seqsign', 'angles', 'hotspots')
INTERNAL_IPS '10.0.2.2'
LANGUAGES [('af', 'Afrikaans'), ('ar', 'Arabic'), ('ast', 'Asturian'), ('az', 'Azerbaijani'), ('bg', 'Bulgarian'), ('be', 'Belarusian'), ('bn', 'Bengali'), ('br', 'Breton'), ('bs', 'Bosnian'), ('ca', 'Catalan'), ('cs', 'Czech'), ('cy', 'Welsh'), ('da', 'Danish'), ('de', 'German'), ('dsb', 'Lower Sorbian'), ('el', 'Greek'), ('en', 'English'), ('en-au', 'Australian English'), ('en-gb', 'British English'), ('eo', 'Esperanto'), ('es', 'Spanish'), ('es-ar', 'Argentinian Spanish'), ('es-co', 'Colombian Spanish'), ('es-mx', 'Mexican Spanish'), ('es-ni', 'Nicaraguan Spanish'), ('es-ve', 'Venezuelan Spanish'), ('et', 'Estonian'), ('eu', 'Basque'), ('fa', 'Persian'), ('fi', 'Finnish'), ('fr', 'French'), ('fy', 'Frisian'), ('ga', 'Irish'), ('gd', 'Scottish Gaelic'), ('gl', 'Galician'), ('he', 'Hebrew'), ('hi', 'Hindi'), ('hr', 'Croatian'), ('hsb', 'Upper Sorbian'), ('hu', 'Hungarian'), ('hy', 'Armenian'), ('ia', 'Interlingua'), ('id', 'Indonesian'), ('io', 'Ido'), ('is', 'Icelandic'), ('it', 'Italian'), ('ja', 'Japanese'), ('ka', 'Georgian'), ('kab', 'Kabyle'), ('kk', 'Kazakh'), ('km', 'Khmer'), ('kn', 'Kannada'), ('ko', 'Korean'), ('lb', 'Luxembourgish'), ('lt', 'Lithuanian'), ('lv', 'Latvian'), ('mk', 'Macedonian'), ('ml', 'Malayalam'), ('mn', 'Mongolian'), ('mr', 'Marathi'), ('my', 'Burmese'), ('nb', 'Norwegian Bokmål'), ('ne', 'Nepali'), ('nl', 'Dutch'), ('nn', 'Norwegian Nynorsk'), ('os', 'Ossetic'), ('pa', 'Punjabi'), ('pl', 'Polish'), ('pt', 'Portuguese'), ('pt-br', 'Brazilian Portuguese'), ('ro', 'Romanian'), ('ru', 'Russian'), ('sk', 'Slovak'), ('sl', 'Slovenian'), ('sq', 'Albanian'), ('sr', 'Serbian'), ('sr-latn', 'Serbian Latin'), ('sv', 'Swedish'), ('sw', 'Swahili'), ('ta', 'Tamil'), ('te', 'Telugu'), ('th', 'Thai'), ('tr', 'Turkish'), ('tt', 'Tatar'), ('udm', 'Udmurt'), ('uk', 'Ukrainian'), ('ur', 'Urdu'), ('vi', 'Vietnamese'), ('zh-hans', 'Simplified Chinese'), ('zh-hant', 'Traditional Chinese')]
LANGUAGES_BIDI ['he', 'ar', 'fa', 'ur']
LANGUAGE_CODE 'en-us'
LANGUAGE_COOKIE_AGE None
LANGUAGE_COOKIE_DOMAIN None
LANGUAGE_COOKIE_NAME 'django_language'
LANGUAGE_COOKIE_PATH '/'
LOCALE_PATHS []
LOGGING {'disable_existing_loggers': False, 'formatters': {'verbose': {'datefmt': '%d/%b/%Y %H:%M:%S', 'format': '[%(asctime)s] %(levelname)s ' '[%(name)s:%(lineno)s] %(message)s'}, 'verbose_low': {'datefmt': '%d/%b/%Y %H:%M:%S', 'format': '[%(asctime)s] %(levelname)s ' '[%(name)s:%(lineno)s]'}}, 'handlers': {'build': {'class': 'logging.FileHandler', 'filename': 'logs/build.log', 'formatter': 'verbose', 'level': 'DEBUG'}, 'django': {'class': 'logging.FileHandler', 'filename': 'logs/django.log', 'formatter': 'verbose', 'level': 'WARNING'}, 'protwis': {'class': 'logging.FileHandler', 'filename': 'logs/protwis.log', 'formatter': 'verbose', 'level': 'DEBUG'}}, 'loggers': {'build': {'handlers': ['build'], 'level': 'DEBUG'}, 'django': {'handlers': ['django'], 'level': 'WARNING', 'propagate': True}, 'protwis': {'handlers': ['protwis'], 'level': 'DEBUG'}}, 'version': 1}
LOGGING_CONFIG 'logging.config.dictConfig'
LOGIN_REDIRECT_URL '/accounts/profile/'
LOGIN_URL '/accounts/login/'
LOGOUT_REDIRECT_URL None
MANAGERS []
MEDIA_ROOT '/protwis/media/protwis'
MEDIA_URL '/media/'
MESSAGE_STORAGE 'django.contrib.messages.storage.fallback.FallbackStorage'
MIDDLEWARE ('common.middleware.stats.StatsMiddleware', 'debug_toolbar.middleware.DebugToolbarMiddleware', 'django.contrib.sessions.middleware.SessionMiddleware', 'django.middleware.common.CommonMiddleware', 'django.middleware.csrf.CsrfViewMiddleware', 'django.contrib.auth.middleware.AuthenticationMiddleware', 'django.contrib.messages.middleware.MessageMiddleware', 'django.middleware.clickjacking.XFrameOptionsMiddleware')
MIGRATION_MODULES {}
MONTH_DAY_FORMAT 'F j'
NUMBER_GROUPING 0
PASSWORD_HASHERS '********************'
PASSWORD_RESET_TIMEOUT_DAYS '********************'
PREPEND_WWW False
REFERENCE_POSITIONS {'D1S1': 'D1S1x50', 'D1S2': 'D1S2x50', 'D1T1': 'D1T1x50', 'D1e1': 'D1e1x50', 'ECL1': '23x50', 'ECL2': '45x50', 'H8': '8x50', 'ICL1': '12x50', 'ICL2': '34x50', 'TM1': '1x50', 'TM2': '2x50', 'TM3': '3x50', 'TM4': '4x50', 'TM5': '5x50', 'TM6': '6x50', 'TM7': '7x50'}
ROOT_URLCONF 'protwis.urls'
SECRET_KEY '********************'
SECURE_BROWSER_XSS_FILTER False
SECURE_CONTENT_TYPE_NOSNIFF False
SECURE_HSTS_INCLUDE_SUBDOMAINS False
SECURE_HSTS_PRELOAD False
SECURE_HSTS_SECONDS 0
SECURE_PROXY_SSL_HEADER None
SECURE_REDIRECT_EXEMPT []
SECURE_SSL_HOST None
SECURE_SSL_REDIRECT False
SERVER_EMAIL 'root@localhost'
SESSION_CACHE_ALIAS 'default'
SESSION_COOKIE_AGE 86400
SESSION_COOKIE_DOMAIN None
SESSION_COOKIE_HTTPONLY True
SESSION_COOKIE_NAME 'sessionid'
SESSION_COOKIE_PATH '/'
SESSION_COOKIE_SAMESITE 'Lax'
SESSION_COOKIE_SECURE False
SESSION_ENGINE 'django.contrib.sessions.backends.db'
SESSION_EXPIRE_AT_BROWSER_CLOSE False
SESSION_FILE_PATH None
SESSION_SAVE_EVERY_REQUEST False
SESSION_SERIALIZER 'django.contrib.sessions.serializers.PickleSerializer'
SETTINGS_MODULE 'protwis.settings'
SHORT_DATETIME_FORMAT 'm/d/Y P'
SHORT_DATE_FORMAT 'm/d/Y'
SIGNING_BACKEND 'django.core.signing.TimestampSigner'
SILENCED_SYSTEM_CHECKS []
SITE_NAME 'gpcr'
SITE_TITLE 'GPCRdb'
STATICFILES_DIRS ('/home/protwis/gpcrdb_test/static',)
STATICFILES_FINDERS ['django.contrib.staticfiles.finders.FileSystemFinder', 'django.contrib.staticfiles.finders.AppDirectoriesFinder']
STATICFILES_STORAGE 'django.contrib.staticfiles.storage.StaticFilesStorage'
STATIC_ROOT '/home/protwis/static_test/'
STATIC_URL '/static/'
SWAGGER_SETTINGS {'USE_SESSION_AUTH': False}
TEMPLATES [{'APP_DIRS': True, 'BACKEND': 'django.template.backends.django.DjangoTemplates', 'DIRS': [], 'OPTIONS': {'context_processors': ['django.contrib.auth.context_processors.auth', 'django.template.context_processors.debug', 'django.template.context_processors.i18n', 'django.template.context_processors.media', 'django.template.context_processors.static', 'django.template.context_processors.tz', 'django.contrib.messages.context_processors.messages', 'protwis.context_processors.current_site', 'protwis.context_processors.canonical_tag', 'protwis.context_processors.documentation_url', 'protwis.context_processors.google_analytics', 'protwis.context_processors.site_title'], 'debug': True}}]
TEST_NON_SERIALIZED_APPS []
TEST_RUNNER 'django.test.runner.DiscoverRunner'
THOUSAND_SEPARATOR ','
TIME_FORMAT 'P'
TIME_INPUT_FORMATS ['%H:%M:%S', '%H:%M:%S.%f', '%H:%M']
TIME_ZONE 'Europe/Copenhagen'
USE_I18N True
USE_L10N True
USE_THOUSAND_SEPARATOR False
USE_TZ True
USE_X_FORWARDED_HOST False
USE_X_FORWARDED_PORT False
WSGI_APPLICATION None
X_FRAME_OPTIONS 'SAMEORIGIN'
YEAR_MONTH_FORMAT 'F Y'

Headers

Request headers

Key Value
Accept text/html,application/xhtml+xml,application/xml;q=0.9,*/*;q=0.8
Accept-Encoding br,gzip
Accept-Language en-US,en;q=0.5
Connection close
Host test.gpcrdb.org
User-Agent CCBot/2.0 (https://commoncrawl.org/faq/)
X-Forwarded-For 35.168.110.128
X-Forwarded-Proto https
X-Real-Ip 35.168.110.128

Response headers

Key Value
Content-Length 691225
Content-Type text/html; charset=utf-8
Vary Cookie
X-Frame-Options SAMEORIGIN

WSGI environ

Since the WSGI environ inherits the environment of the server, only a significant subset is shown below.

Key Value
PATH_INFO /ligand/target/all/001_001_001_010/
QUERY_STRING
REMOTE_ADDR
REQUEST_METHOD GET
SCRIPT_NAME
SERVER_NAME test.gpcrdb.org
SERVER_PORT 443
SERVER_PROTOCOL HTTP/1.0
SERVER_SOFTWARE gunicorn/19.9.0

Request

View information

View function Arguments Keyword arguments URL name
ligand.views.TargetDetails () {'slug': '001_001_001_010'} ligand_target_detail

No cookies

No session data

No GET data

No POST data

SQL queries from 1 connection

  •   default 494.70 ms (411 queries including 409 similar and 296 duplicates )
  Query Timeline Time (ms) Action
  +
SELECT ••• "ligand_assayexperiment"."id", "ligand_assayexperiment"."ligand_id", "ligand_assayexperiment"."protein_id", "ligand_assayexperiment"."assay_id", "ligand_assayexperiment"."assay_type", "ligand_assayexperiment"."assay_description", "ligand_assayexperiment"."pchembl_value", "ligand_assayexperiment"."published_value", "ligand_assayexperiment"."published_relation", "ligand_assayexperiment"."published_type", "ligand_assayexperiment"."published_units", "ligand_assayexperiment"."standard_value", "ligand_assayexperiment"."standard_relation", "ligand_assayexperiment"."standard_type", "ligand_assayexperiment"."standard_units", "ligand_assayexperiment"."publication_id", "ligand_assayexperiment"."chembl", "ligand_assayexperiment"."smiles", "ligand_assayexperiment"."activity", "ligand_assayexperiment"."document_chembl_id", "ligand_assayexperiment"."cell_line" FROM "ligand_assayexperiment" INNER JOIN "ligand" ON ("ligand_assayexperiment"."ligand_id" = "ligand"."id") INNER JOIN "ligand_properities" ON ("ligand"."properities_id" = "ligand_properities"."id") INNER JOIN "ligand_properities_web_links" ON ("ligand_properities"."id" = "ligand_properities_web_links"."ligandproperities_id") INNER JOIN "web_link" ON ("ligand_properities_web_links"."weblink_id" = "web_link"."id") INNER JOIN "web_resource" ON ("web_link"."web_resource_id" = "web_resource"."id") INNER JOIN "protein" ON ("ligand_assayexperiment"."protein_id" = "protein"."id") INNER JOIN "protein_family" ON ("protein"."family_id" = "protein_family"."id") WHERE ("web_resource"."slug" = 'chembl_ligand' AND "protein_family"."slug" = '001_001_001_010')
28.480140882811643%
140.89

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(334)
  if not ps:
  +
SELECT ••• "ligand_assayexperiment"."standard_type", "ligand_assayexperiment"."standard_relation", "ligand_assayexperiment"."standard_value", "ligand_assayexperiment"."assay_description", "ligand_assayexperiment"."assay_type", "ligand_assayexperiment"."pchembl_value", "ligand_assayexperiment"."ligand_id", "ligand"."properities_id", "web_link"."index", "species"."common_name", "protein"."entry_name", "ligand_properities"."mw", "ligand_properities"."logp", "ligand_properities"."rotatable_bonds", "ligand_properities"."smiles", "ligand_properities"."hdon", "ligand_properities"."hacc", "ligand_assayexperiment"."protein_id", COUNT(DISTINCT "ligand_assayexperiment"."protein_id") AS "num_targets" FROM "ligand_assayexperiment" INNER JOIN "ligand" ON ("ligand_assayexperiment"."ligand_id" = "ligand"."id") INNER JOIN "ligand_properities" ON ("ligand"."properities_id" = "ligand_properities"."id") INNER JOIN "ligand_properities_web_links" ON ("ligand_properities"."id" = "ligand_properities_web_links"."ligandproperities_id") INNER JOIN "web_link" ON ("ligand_properities_web_links"."weblink_id" = "web_link"."id") INNER JOIN "web_resource" ON ("web_link"."web_resource_id" = "web_resource"."id") INNER JOIN "protein" ON ("ligand_assayexperiment"."protein_id" = "protein"."id") INNER JOIN "protein_family" ON ("protein"."family_id" = "protein_family"."id") INNER JOIN "species" ON ("protein"."species_id" = "species"."id") WHERE ("web_resource"."slug" = 'chembl_ligand' AND "protein_family"."slug" = '001_001_001_010') GROUP BY "ligand_assayexperiment"."standard_type", "ligand_assayexperiment"."standard_relation", "ligand_assayexperiment"."standard_value", "ligand_assayexperiment"."assay_description", "ligand_assayexperiment"."assay_type", "ligand_assayexperiment"."pchembl_value", "ligand_assayexperiment"."ligand_id", "ligand"."properities_id", "web_link"."index", "species"."common_name", "protein"."entry_name", "ligand_properities"."mw", "ligand_properities"."logp", "ligand_properities"."rotatable_bonds", "ligand_properities"."smiles", "ligand_properities"."hdon", "ligand_properities"."hacc", "ligand_assayexperiment"."protein_id"
2.5575493176591246%
12.65

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(357)
  for record in ps:
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 58152 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.3801117731994934%
1.88

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 58152 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.10010043780085555%
0.50

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 93054 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.3286880047192272%
1.63

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 93054 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.11643844859261772%
0.58

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 136011 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.12092055774787992%
0.60

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 136011 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.11648664331471731%
0.58

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 48745 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.2931202998097272%
1.45

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 48745 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.11296842860144701%
0.56

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 42315 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.31750682919212153%
1.57

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 8172 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.30102423423406055%
1.49

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 19349 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.11340218110034335%
0.56

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 45551 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.3278204997214345%
1.62

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 27038 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
2.0644691158581843%
10.21

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 44773 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.3110005417086764%
1.54

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 79297 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.09402790281630678%
0.47

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 16300 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.3385679227496438%
1.67

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 102618 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.3101330367108837%
1.53

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 3855 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.6026749998554158%
2.98

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 100818 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.11234189721415228%
0.56

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 49007 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.10038960613345312%
0.50

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 43980 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.33837514386124545%
1.67

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 99459 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.38729278679233275%
1.92

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 41994 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.29871088757328007%
1.48

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 5252 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.11455885443073359%
0.57

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 44137 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.11070327666276611%
0.55

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 45710 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.
0.11600469609372138%
0.57

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 34616 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 9 times.
0.2867104017704813%
1.42

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 34616 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 9 times.
0.11185994999315635%
0.55

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 34616 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 9 times.
0.10901646138928034%
0.54

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 34616 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 9 times.
0.1113298080500608%
0.55

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 126542 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 5 times.
0.10752242500419296%
0.53

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 126542 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 5 times.
0.10858270889038399%
0.54

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 91892 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 5 times.
0.11398051776553846%
0.56

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 91892 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 5 times.
0.10699228306109741%
0.53

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 113780 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.11181175527105675%
0.55

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 113780 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.11176356054895716%
0.55

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 113292 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.4104262534001376%
2.03

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 113292 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.11152258693845919%
0.55

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 114050 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.29581920424730446%
1.46

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 114050 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.11190814471525594%
0.55

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 113269 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.1122455077699531%
0.56

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 113269 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.10829354055778644%
0.54

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 113475 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.1136913494329409%
0.56

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 113475 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.09542554975719499%
0.47

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink"."url", "ligand_ligandvendorlink"."vendor_external_id", "ligand_ligandvendorlink"."sid" FROM "ligand_ligandvendorlink" INNER JOIN "ligand_ligandvendors" ON ("ligand_ligandvendorlink"."vendor_id" = "ligand_ligandvendors"."id") WHERE ("ligand_ligandvendorlink"."lp_id" = 13760 AND NOT ("ligand_ligandvendors"."name" IN ('ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem')))
  409 similar queries.   Duplicated 2 times.
0.11210092360365433%
0.55

Connection: default

/usr/lib/python3.6/concurrent/futures/thread.py in _worker(69)
  work_item.run()
/usr/lib/python3.6/concurrent/futures/thread.py in run(56)
  result = self.fn(*self.args, **self.kwargs)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle(279)
  keepalive = self.handle_request(req, conn)
/home/protwis/gpcrdb_env/lib/python3.6/site-packages/gunicorn/workers/gthread.py in handle_request(328)
  respiter = self.wsgi(environ, resp.start_response)
/home/protwis/gpcrdb_test/common/middleware/stats.py in __call__(34)
  response = self.get_response(request)
/home/protwis/gpcrdb_test/ligand/views.py in TargetDetails(359)
  vendor__name__in=['ZINC', 'ChEMBL', 'BindingDB', 'SureChEMBL', 'eMolecules', 'MolPort', 'PubChem'])) > 0 else 'No'
  +
SELECT ••• "ligand_ligandvendorlink"."id", "ligand_ligandvendorlink"."vendor_id", "ligand_ligandvendorlink"."lp_id", "ligand_ligandvendorlink".&quo