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 nM 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 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C
CHEMBL1606743 5ht5a_human Human Yes 4.1 EC50 = 78366 nM 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]
324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C
CHEMBL1625496 5ht5a_human Human Yes 4.1 EC50 = 78366 nM 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]
324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C
CHEMBL1169627 5ht5a_human Human Yes 4.1 EC50 = 79156 nM 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]
594 2 2 8 6.6 COc1cc2c3cc1Oc1cc(ccc1O)C[C@@H]1c4c(cc(OC)c(O)c4Oc4ccc(cc4)C[C@H]3N(C)CC2)CCN1C
CHEMBL517986 5ht5a_human Human Yes 4.1 EC50 = 85847 nM 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]
299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C
CHEMBL1210154 5ht5a_human Human No 9.0 IC50 = 1 nM Bind
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 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1
CHEMBL102645 5ht5a_human Human No 6.0 IC50 = 1000 nM Bind
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 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3C(C)(C)CNS3(=O)=O)cc12
CHEMBL4128926 5ht5a_human Human No 7.0 IC50 = 106 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysis
583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12
CHEMBL103549 5ht5a_human Human No 6.9 IC50 = 125.9 nM Bind
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 3 1.0 CN(C)CCc1c[nH]c2ccc(CCN3CCNS3(=O)=O)cc12
CHEMBL321963 5ht5a_human Human No 6.9 IC50 = 125.9 nM Bind
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
364 7 1 3 1.7 CCN1CCN(CCc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O
CHEMBL323334 5ht5a_human Human No 6.9 IC50 = 125.9 nM Bind
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 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CCCN(C)S3(=O)=O)cc12
CHEMBL39 5ht5a_human Human Yes 6.8 IC50 = 160 nM Bind
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht5a_human Human Yes 6.8 IC50 = 180 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht5a_human Human Yes 6.8 IC50 = 180 nM Bind
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht5a_human Human Yes 6.8 IC50 = 180 nM Bind
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht5a_human Human Yes 6.7 IC50 = 184 nM Bind
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL103371 5ht5a_human Human No 6.7 IC50 = 199.5 nM Bind
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 3 1.3 CN(C)CCc1c[nH]c2ccc(CCN3CCN(C)S3(=O)=O)cc12
CHEMBL103388 5ht5a_human Human No 6.7 IC50 = 199.5 nM Bind
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
469 8 2 4 2.8 CC(=O)Nc1ccc(CN2CCN(Cc3ccc4[nH]cc(CCN(C)C)c4c3)S2(=O)=O)cc1
CHEMBL2111620 5ht5a_human Human No 5.7 IC50 = 1995.3 nM Bind
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 4 1.4 CN1CCN(Cc2ccc3scc(CCN)c3c2)S1(=O)=O
CHEMBL320412 5ht5a_human Human No 6.6 IC50 = 251.2 nM Bind
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 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CC(C)(C)NS3(=O)=O)cc12
CHEMBL39 5ht5a_human Human Yes 6.6 IC50 = 260 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL39 5ht5a_human Human Yes 6.6 IC50 = 280 nM Bind
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL326263 5ht5a_human Human No 5.5 IC50 = 3380 nM Bind
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1
CHEMBL128 5ht5a_human Human Yes 6.3 IC50 = 501.2 nM Bind
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 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2
CHEMBL318571 5ht5a_human Human No 6.3 IC50 = 501.2 nM Bind
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
364 6 1 3 2.0 CC(C)N1CCN(Cc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O
CHEMBL117537 5ht5a_human Human No 5.3 IC50 = 5520 nM Bind
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL103854 5ht5a_human Human No 6.2 IC50 = 631.0 nM Bind
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 3 0.7 CN1CCN(Cc2ccc3[nH]cc(CCN)c3c2)S1(=O)=O
CHEMBL319223 5ht5a_human Human No 6.2 IC50 = 631.0 nM Bind
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 3 1.3 CN(C)CCc1c[nH]c2ccc(N3CCN(C)S3(=O)=O)cc12
CHEMBL39 5ht5a_human Human Yes 7.1 IC50 = 79 nM Bind
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL101138 5ht5a_human Human No 7.1 IC50 = 79.4 nM Bind
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
398 6 1 3 2.8 CN(C)CCc1c[nH]c2ccc(N3CCN(Cc4ccccc4)S3(=O)=O)cc12
CHEMBL102548 5ht5a_human Human No 6.1 IC50 = 794.3 nM Bind
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 3 0.9 CN(C)CCc1c[nH]c2ccc(CN3CCNS3(=O)=O)cc12
CHEMBL102586 5ht5a_human Human No 6.1 IC50 = 794.3 nM Bind
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 3 0.9 CNCCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12
CHEMBL103205 5ht5a_human Human No 6.1 IC50 = 794.3 nM Bind
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 3 1.3 CN(C)CCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12
CHEMBL270177 5ht5a_human Human Yes 8.5 Kd = 3.0 nM 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
195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21
CHEMBL270177 5ht5a_human Human Yes 8.5 Kd = 3.2 nM 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
195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21
CHEMBL404511 5ht5a_human Human Yes 7.4 Kd = 38.9 nM 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
259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21
CHEMBL269964 5ht5a_human Human Yes 8.1 Kd = 7.4 nM 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
209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1
CHEMBL3654198 5ht5a_human Human No 9.2 Ki = 0.7 nM Bind
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 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cc(F)cc3F)c2C1
CHEMBL3654206 5ht5a_human Human No 9.1 Ki = 0.8 nM Bind
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 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3c(F)cccc3F)ccc(F)c2C2(CC2)C1
CHEMBL3654212 5ht5a_human Human No 9.1 Ki = 0.9 nM Bind
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 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(F)c2C2(CC2)C1
CHEMBL3654208 5ht5a_human Human No 9.1 Ki = 0.9 nM Bind
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 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3c(F)cc(F)cc3F)ccc(F)c2C2(CC2)C1
CHEMBL3654214 5ht5a_human Human No 9.0 Ki = 1.0 nM Bind
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 1 2.9 NC(N)=NC(=O)N1Cc2c(-c3ccccc3F)ccc(F)c2C2(CC2)C1
CHEMBL93240 5ht5a_human Human Yes 9.0 Ki = 1 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C
CHEMBL93240 5ht5a_human Human Yes 9.0 Ki = 1 nM Bind
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
356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C
CHEMBL3654197 5ht5a_human Human No 9.0 Ki = 1.1 nM Bind
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 1 3.2 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cc(F)cc3F)c2C1
CHEMBL3654199 5ht5a_human Human No 9.0 Ki = 1.1 nM Bind
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 1 2.5 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cccc3F)c2C1
CHEMBL3644535 5ht5a_human Human No 8.9 Ki = 1.2 nM Bind
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.
360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3c(F)cccc3F)c2c1
CHEMBL3654210 5ht5a_human Human No 8.9 Ki = 1.3 nM Bind
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 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3cc(F)c(F)cc3F)ccc(F)c2C2(CC2)C1
CHEMBL3644525 5ht5a_human Human No 8.9 Ki = 1.3 nM Bind
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.
360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2ncc(Cl)c(-c3ccc(F)cc3F)c2c1
CHEMBL3644530 5ht5a_human Human No 8.9 Ki = 1.3 nM Bind
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 2 3.0 Cc1cnc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc12
CHEMBL404372 5ht5a_rat Rat Yes 8.9 Ki = 1.3 nM Bind
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21
CHEMBL3644528 5ht5a_human Human No 8.9 Ki = 1.4 nM Bind
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 2 2.7 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3F)c2c1
CHEMBL3654207 5ht5a_human Human No 8.8 Ki = 1.6 nM Bind
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 1 3.1 CC1CN(C(=O)N=C(N)N)Cc2c(-c3c(F)cccc3F)ccc(F)c21
CHEMBL3644527 5ht5a_human Human No 8.8 Ki = 1.6 nM Bind
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.
360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3Cl)c2c1
CHEMBL404372 5ht5a_human Human Yes 8.8 Ki = 1.6 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21
CHEMBL3644540 5ht5a_human Human No 8.7 Ki = 1.8 nM Bind
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 2 2.8 Cc1cnc(-c2ccccc2F)c2cc(C(=O)N=C(N)N)ccc12
CHEMBL256694 5ht5a_human Human No 8.7 Ki = 1.8 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21
CHEMBL3654205 5ht5a_human Human No 8.7 Ki = 1.9 nM Bind
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).
381 1 2 2 2.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3Cl)c2C1
CHEMBL3644537 5ht5a_human Human No 8.7 Ki = 1.9 nM Bind
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 2 2.9 Cc1cnc(-c2c(F)cccc2F)c2cc(C(=O)N=C(N)N)ccc12
CHEMBL258075 5ht5a_human Human Yes 8.0 Ki = 10 nM Bind
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 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C
CHEMBL404511 5ht5a_human Human Yes 8.0 Ki = 10.1 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21
CHEMBL269964 5ht5a_human Human Yes 8.0 Ki = 10.7 nM Bind
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
209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1
CHEMBL269964 5ht5a_human Human Yes 8.0 Ki = 10.8 nM Bind
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
209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1
CHEMBL93240 5ht5a_human Human Yes 7.0 Ki = 100 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C
CHEMBL128099 5ht5a_human Human No 7.0 Ki = 100 nM Bind
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 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2
CHEMBL128848 5ht5a_human Human No 7.0 Ki = 100 nM Bind
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 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2
CHEMBL56 5ht5a_human Human Yes 6.0 Ki = 1000 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL13816 5ht5a_human Human No 6.0 Ki = 1000 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21
CHEMBL1112 5ht5a_human Human Yes 6.0 Ki = 1000 nM Bind
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL85 5ht5a_human Human Yes 6.0 Ki = 1000 nM Bind
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2
CHEMBL42 5ht5a_human Human Yes 6.0 Ki = 1000 nM Bind
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
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL1181632 5ht5a_human Human No 6.0 Ki = 1000 nM Bind
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
567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1
CHEMBL186261 5ht5a_human Human No 6.0 Ki = 1000 nM Bind
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
567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1
CHEMBL47050 5ht5a_human Human Yes 6.0 Ki = 1000 nM Bind
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL2442270 5ht5a_human Human No 7.0 Ki = 101 nM Bind
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 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1
CHEMBL272517 5ht5a_human Human Yes 7.0 Ki = 103 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
175 0 2 3 1.6 CNC1=Nc2ccccc2C(C)N1
CHEMBL7143 5ht5a_human Human Yes 5.0 Ki = 10450 nM Bind
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 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1
CHEMBL126666 5ht5a_human Human No 6.0 Ki = 1080 nM Bind
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 4.2 CN(CCCOc1ccc(F)cc1)Cc1cn(C)c2ccccc12
CHEMBL39 5ht5a_human Human Yes 7.0 Ki = 110 nM Bind
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL126021 5ht5a_mouse Mouse No 6.0 Ki = 1100 nM Bind
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 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2
CHEMBL2442274 5ht5a_human Human No 7.0 Ki = 112 nM Bind
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
304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1
CHEMBL126021 5ht5a_human Human No 6.0 Ki = 1120 nM Bind
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 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2
CHEMBL4215875 5ht5a_human Human No 6.0 Ki = 1135 nM Bind
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
228 1 1 3 2.3 CC1=CC=C(C=C1)C2=NOC3=C2CCNCC3
CHEMBL129230 5ht5a_mouse Mouse No 6.9 Ki = 115 nM Bind
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 4.3 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccc(F)cc1)CC2
CHEMBL1196896 5ht5a_human Human No 5.9 Ki = 1172 nM Bind
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 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21
CHEMBL558579 5ht5a_human Human No 5.9 Ki = 1172 nM Bind
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 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21
CHEMBL3326982 5ht5a_human Human No 5.9 Ki = 1178 nM Bind
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1
CHEMBL190382 5ht5a_human Human No 7.9 Ki = 12.6 nM Bind
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
512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)CCC1CCCC1
CHEMBL125417 5ht5a_mouse Mouse No 6.9 Ki = 120 nM Bind
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 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2
CHEMBL125745 5ht5a_rat Rat No 5.9 Ki = 1200 nM Bind
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 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1
CHEMBL402400 5ht5a_human Human No 6.9 Ki = 122 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
215 1 2 3 2.5 CC1NC(NC2CCC2)=Nc2ccccc21
CHEMBL128184 5ht5a_mouse Mouse No 5.9 Ki = 1220 nM Bind
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 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3
CHEMBL2442271 5ht5a_human Human No 6.9 Ki = 123 nM Bind
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
304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1
CHEMBL4218672 5ht5a_human Human No 5.9 Ki = 1231 nM Bind
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
232 1 1 3 2.2 C1CNCCC2=C1C(=NO2)C3=CC=C(C=C3)F
CHEMBL257302 5ht5a_human Human No 6.9 Ki = 124 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
271 3 2 3 3.9 CC1NC(NCCC2CCCCC2)=Nc2ccccc21
CHEMBL189262 5ht5a_human Human No 6.9 Ki = 125.9 nM Bind
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
489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3ccc(CNC4CCN(Cc5ccccc5)CC4)cc3)cc2)cc1
CHEMBL497963 5ht5a_human Human No 5.9 Ki = 1258.9 nM Bind
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1
CHEMBL39 5ht5a_human Human Yes 6.9 Ki = 126 nM Bind
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
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2442275 5ht5a_human Human No 5.9 Ki = 1282 nM Bind
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
318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O
CHEMBL3644524 5ht5a_human Human No 7.9 Ki = 13 nM Bind
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 2 3.0 Cc1cc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc2n1
CHEMBL138989 5ht5a_human Human No 7.9 Ki = 13 nM Bind
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1
CHEMBL96504 5ht5a_human Human No 7.9 Ki = 13 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2
CHEMBL96504 5ht5a_mouse Mouse No 7.9 Ki = 13 nM Bind
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 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2
CHEMBL129472 5ht5a_mouse Mouse No 6.9 Ki = 130 nM Bind
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 2 4.6 Cn1c2c(c3ccccc31)CN(CCCCc1ccccc1)CC2
CHEMBL39 5ht5a_human Human Yes 6.9 Ki = 130 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2058409 5ht5a_human Human No 5.9 Ki = 1323 nM Bind
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
318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12
CHEMBL129476 5ht5a_mouse Mouse No 6.9 Ki = 135 nM Bind
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 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2
CHEMBL1188516 5ht5a_human Human No 5.9 Ki = 1375 nM Bind
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
177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2
CHEMBL536561 5ht5a_human Human No 5.9 Ki = 1375 nM Bind
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
177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2
CHEMBL128184 5ht5a_human Human No 5.9 Ki = 1395 nM Bind
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 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3
CHEMBL442 5ht5a_human Human Yes 7.9 Ki = 14 nM Bind
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
581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL2058418 5ht5a_human Human No 5.9 Ki = 1425 nM Bind
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
332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C
CHEMBL1188759 5ht5a_human Human No 6.8 Ki = 145 nM Bind
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
161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2
CHEMBL537248 5ht5a_human Human No 6.8 Ki = 145 nM Bind
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
161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2
CHEMBL2058415 5ht5a_human Human No 5.8 Ki = 1454 nM Bind
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
332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C
CHEMBL270131 5ht5a_human Human No 5.8 Ki = 1472 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
259 2 2 3 2.8 C[C@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21
CHEMBL273921 5ht5a_human Human No 5.8 Ki = 1479.1 nM Bind
Binding affinity towards cloned human 5-HT5A receptor was determinedBinding affinity towards cloned human 5-HT5A receptor was determined
422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1
CHEMBL442 5ht5a_human Human Yes 7.8 Ki = 15.5 nM Bind
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL39 5ht5a_mouse Mouse Yes 6.8 Ki = 150 nM Bind
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL1829959 5ht5a_human Human No 5.8 Ki = 1525 nM Bind
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 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12
CHEMBL270658 5ht5a_human Human No 6.8 Ki = 153 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
203 2 2 3 2.3 CCCNC1=Nc2ccccc2C(C)N1
CHEMBL2442277 5ht5a_human Human No 5.8 Ki = 1550 nM Bind
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
318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O
CHEMBL516088 5ht5a_human Human No 5.8 Ki = 1584 nM Bind
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1
CHEMBL522708 5ht5a_human Human No 5.8 Ki = 1584.9 nM Bind
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1
CHEMBL137781 5ht5a_human Human No 7.8 Ki = 16 nM Bind
Binding affinities against 5-hydroxytryptamine 5A receptorBinding affinities against 5-hydroxytryptamine 5A receptor
335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1
CHEMBL442 5ht5a_human Human Yes 7.8 Ki = 16 nM Bind
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL126340 5ht5a_rat Rat No 5.8 Ki = 1600 nM Bind
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
432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1
CHEMBL18041 5ht5a_human Human Yes 4.8 Ki = 16000 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl
CHEMBL403102 5ht5a_human Human No 6.8 Ki = 163 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
245 2 2 4 2.1 CC1NC(NC[C@H]2CCCO2)=Nc2ccccc21
CHEMBL128185 5ht5a_human Human No 6.8 Ki = 165 nM Bind
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 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1
CHEMBL95104 5ht5a_human Human Yes 6.8 Ki = 168 nM Bind
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2
CHEMBL129476 5ht5a_human Human No 6.8 Ki = 168 nM Bind
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 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2
CHEMBL278751 5ht5a_human Human Yes 6.8 Ki = 168 nM Bind
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 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C
CHEMBL490632 5ht5a_human Human No 5.8 Ki = 1684 nM Bind
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1
CHEMBL34652 5ht5a_rat Rat No 7.8 Ki = 17 nM Bind
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 3.7 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1OC
CHEMBL39 5ht5a_human Human Yes 6.8 Ki = 170 nM Bind
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL2181166 5ht5a_human Human No 5.8 Ki = 1700 nM Bind
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12
CHEMBL129774 5ht5a_mouse Mouse No 5.8 Ki = 1710 nM Bind
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 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2
CHEMBL125417 5ht5a_human Human No 6.8 Ki = 174 nM Bind
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 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2
CHEMBL4165863 5ht5a_human Human No 5.8 Ki = 1747 nM Bind
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1
CHEMBL256049 5ht5a_human Human No 6.8 Ki = 176 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
247 5 2 4 2.4 CCOCCCNC1=Nc2ccccc2C(C)N1
CHEMBL129774 5ht5a_human Human No 5.8 Ki = 1775 nM Bind
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 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2
CHEMBL522691 5ht5a_human Human Yes 6.8 Ki = 178 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1
CHEMBL25163 5ht5a_human Human No 5.8 Ki = 1791 nM Bind
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
161 0 2 3 1.0 CNC1=Nc2ccccc2CN1
CHEMBL536557 5ht5a_human Human No 5.8 Ki = 1791 nM Bind
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
161 0 2 3 1.0 CNC1=Nc2ccccc2CN1
CHEMBL338095 5ht5a_mouse Mouse No 6.8 Ki = 180 nM Bind
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2
CHEMBL95104 5ht5a_human Human Yes 6.7 Ki = 182.0 nM Bind
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 )
487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2
CHEMBL2442273 5ht5a_human Human No 6.7 Ki = 184 nM Bind
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
304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1
CHEMBL446356 5ht5a_human Human No 6.7 Ki = 185 nM Bind
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 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2
CHEMBL132019 5ht5a_rat Rat No 6.7 Ki = 186 nM Bind
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 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(O)c1
CHEMBL402874 5ht5a_human Human No 6.7 Ki = 189 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
217 3 2 3 2.7 CCCCNC1=Nc2ccccc2C(C)N1
CHEMBL435814 5ht5a_human Human No 6.7 Ki = 190 nM Bind
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 4 3.6 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(N)cc1)CC2
CHEMBL340861 5ht5a_human Human No 5.7 Ki = 1920 nM Bind
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 3.0 Cn1ccc2c1CCN(CCCOc1ccc(F)cc1)C2
CHEMBL1188681 5ht5a_human Human No 6.7 Ki = 196 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1
CHEMBL537022 5ht5a_human Human No 6.7 Ki = 196 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1
CHEMBL3217984 5ht5a_human Human No 6.7 Ki = 199.5 nM Bind
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 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3
CHEMBL1179769 5ht5a_human Human No 6.7 Ki = 199.5 nM Bind
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
555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1
CHEMBL99071 5ht5a_human Human No 6.7 Ki = 199.5 nM Bind
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
555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1
CHEMBL187415 5ht5a_human Human No 6.7 Ki = 199.5 nM Bind
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
489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3cccc(CNC4CCN(Cc5ccccc5)CC4)c3)cc2)cc1
CHEMBL1190707 5ht5a_human Human Yes 5.7 Ki = 1990 nM Bind
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
165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1
CHEMBL541394 5ht5a_human Human Yes 5.7 Ki = 1990 nM Bind
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
165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1
CHEMBL4472703 5ht5a_human Human No 5.7 Ki = 1995.3 nM Bind
Displacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N
CHEMBL274384 5ht5a_mouse Mouse Yes 8.7 Ki = 2 nM Bind
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
401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC
CHEMBL273170 5ht5a_human Human Yes 8.7 Ki = 2 nM Bind
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
229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21
CHEMBL3644541 5ht5a_human Human No 8.6 Ki = 2.3 nM Bind
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.
360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3ccc(F)cc3F)c2c1
CHEMBL3654204 5ht5a_human Human No 8.6 Ki = 2.5 nM Bind
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 2 2.4 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cncc3F)c2C1
CHEMBL34653 5ht5a_rat Rat No 8.6 Ki = 2.6 nM Bind
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 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1cccc(O)c1
CHEMBL3654200 5ht5a_human Human No 8.6 Ki = 2.7 nM Bind
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).
364 1 2 1 3.0 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3ccc(F)cc3F)c2C1
CHEMBL3654209 5ht5a_human Human No 8.6 Ki = 2.7 nM Bind
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 1 1.9 NC(N)=NC(=O)N1Cc2c(C3CC3)ccc(F)c2C2(CC2)C1
CHEMBL541993 5ht5a_rat Rat No 8.5 Ki = 2.9 nM Bind
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21
CHEMBL18840 5ht5a_human Human Yes 7.7 Ki = 20 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N
CHEMBL18840 5ht5a_human Human Yes 7.7 Ki = 20 nM Bind
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
203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N
CHEMBL97518 5ht5a_human Human No 6.7 Ki = 200 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1
CHEMBL126897 5ht5a_human Human No 6.7 Ki = 200 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
388 5 0 3 5.3 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)c(Cl)c1)CC2
CHEMBL126898 5ht5a_human Human No 6.7 Ki = 200 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
354 5 0 3 4.7 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)cc1)CC2
CHEMBL51 5ht5a_human Human Yes 4.7 Ki = 20000 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2
CHEMBL51 5ht5a_human Human Yes 4.7 Ki = 20000 nM Bind
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
395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2
CHEMBL2111848 5ht5a_human Human No 6.7 Ki = 208 nM Bind
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 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2
CHEMBL3752900 5ht5a_human Human No 5.7 Ki = 2089.3 nM Bind
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12
CHEMBL278509 5ht5a_human Human Yes 5.7 Ki = 2100 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
212 1 1 2 2.2 c1ccc2cc(N3CCNCC3)ccc2c1
CHEMBL2413153 5ht5a_human Human Yes 5.7 Ki = 2128 nM Bind
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O
CHEMBL266250 5ht5a_mouse Mouse Yes 6.7 Ki = 215 nM Bind
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
178 1 2 3 0.8 Oc1ccccc1N1CCNCC1
CHEMBL442 5ht5a_human Human Yes 7.7 Ki = 22 nM Bind
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
581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL257744 5ht5a_human Human No 7.7 Ki = 22.2 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
289 3 2 4 2.9 COc1c(Cl)ccc2c1C(C)NC(NCC(F)F)=N2
CHEMBL446459 5ht5a_human Human No 7.7 Ki = 22.2 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
283 4 2 4 3.0 CC(C)Oc1cccc2c1N=C(NCC(F)F)NC2C
CHEMBL258073 5ht5a_human Human No 7.6 Ki = 22.9 nM Bind
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
225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2
CHEMBL2104993 5ht5a_human Human Yes 6.7 Ki = 220 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1
CHEMBL481153 5ht5a_human Human No 5.7 Ki = 2200 nM Bind
Antagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assay
340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21
CHEMBL467094 5ht5a_human Human Yes 5.7 Ki = 2224 nM Bind
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4
CHEMBL126737 5ht5a_human Human No 6.7 Ki = 225 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2
CHEMBL338696 5ht5a_mouse Mouse No 6.7 Ki = 225 nM Bind
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 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2
CHEMBL3770342 5ht5a_human Human No 6.6 Ki = 227 nM Bind
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
335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1
CHEMBL199824 5ht5a_human Human Yes 6.6 Ki = 228.6 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1
CHEMBL2068762 5ht5a_human Human Yes 6.6 Ki = 228.6 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1
CHEMBL27441 5ht5a_human Human Yes 5.6 Ki = 2331 nM Bind
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 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC
CHEMBL2442276 5ht5a_human Human No 5.6 Ki = 2332 nM Bind
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
318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O
CHEMBL134331 5ht5a_rat Rat No 6.6 Ki = 239 nM Bind
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 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1OC
CHEMBL3754166 5ht5a_human Human No 5.6 Ki = 2398.8 nM Bind
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12
CHEMBL270841 5ht5a_human Human No 7.6 Ki = 24 nM Bind
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 3 1.7 CCC1NC(N)=Nc2ccccc21
CHEMBL256048 5ht5a_human Human No 6.6 Ki = 241 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
247 5 2 4 2.4 CCCOCCNC1=Nc2ccccc2C(C)N1
CHEMBL269236 5ht5a_mouse Mouse Yes 5.6 Ki = 2470 nM Bind
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3
CHEMBL128848 5ht5a_mouse Mouse No 7.6 Ki = 25 nM Bind
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 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2
CHEMBL1181620 5ht5a_human Human No 7.6 Ki = 25.1 nM Bind
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
537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1
CHEMBL185676 5ht5a_human Human No 7.6 Ki = 25.1 nM Bind
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
537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1
CHEMBL1181680 5ht5a_human Human No 7.6 Ki = 25.1 nM Bind
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
517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1
CHEMBL188486 5ht5a_human Human No 7.6 Ki = 25.1 nM Bind
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
517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1
CHEMBL187621 5ht5a_human Human No 7.6 Ki = 25.1 nM Bind
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
518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)/C=C/c1ccccc1
CHEMBL402179 5ht5a_human Human Yes 7.6 Ki = 25.4 nM Bind
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 2 2 4 2.3 CNC1=Nc2c(OC(C)C)cccc2C(C)N1
CHEMBL39 5ht5a_human Human Yes 6.6 Ki = 250 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL130585 5ht5a_human Human No 6.6 Ki = 250 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
365 6 0 5 3.9 Cn1c2c(c3ccccc31)CN(CCCOc1ccc([N+](=O)[O-])cc1)CC2
CHEMBL126574 5ht5a_mouse Mouse No 6.6 Ki = 250 nM Bind
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 2 4.2 Cn1c2c(c3ccccc31)CN(CCCc1ccccc1)CC2
CHEMBL56 5ht5a_human Human Yes 5.6 Ki = 2500 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL56 5ht5a_human Human Yes 5.6 Ki = 2500 nM Bind
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 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL1181677 5ht5a_human Human No 6.6 Ki = 251.2 nM Bind
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
553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1
CHEMBL188440 5ht5a_human Human No 6.6 Ki = 251.2 nM Bind
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
553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1
CHEMBL1184719 5ht5a_human Human No 6.6 Ki = 251.2 nM Bind
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
523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1
CHEMBL365422 5ht5a_human Human No 6.6 Ki = 251.2 nM Bind
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
523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1
CHEMBL439240 5ht5a_human Human Yes 7.6 Ki = 26.5 nM Bind
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
243 1 2 3 3.0 CCC1NC(N)=Nc2ccc(Cl)c(Cl)c21
CHEMBL343755 5ht5a_human Human No 7.6 Ki = 27 nM Bind
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1
CHEMBL338095 5ht5a_human Human No 6.6 Ki = 270 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2
CHEMBL1188595 5ht5a_human Human Yes 6.6 Ki = 274 nM Bind
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
161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2
CHEMBL536789 5ht5a_human Human Yes 6.6 Ki = 274 nM Bind
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
161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2
CHEMBL403103 5ht5a_human Human No 6.6 Ki = 279 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
286 1 2 4 1.9 CC1NC(NC2CCCCN(C)C2=O)=Nc2ccccc21
CHEMBL404248 5ht5a_human Human No 7.6 Ki = 28.2 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
255 3 2 4 2.2 COc1cccc2c1N=C(NCC(F)F)NC2C
CHEMBL270409 5ht5a_human Human No 5.6 Ki = 2800 nM Bind
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 0 1 3 1.3 CN(C)C1=Nc2ccccc2CN1
CHEMBL338696 5ht5a_human Human No 6.5 Ki = 285 nM Bind
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 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2
CHEMBL161507 5ht5a_human Human No 6.5 Ki = 287 nM Bind
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 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C
CHEMBL338081 5ht5a_mouse Mouse No 6.5 Ki = 295 nM Bind
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 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOCc1ccccc1)CC2
CHEMBL24462 5ht5a_human Human Yes 8.5 Ki = 3 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
228 1 2 3 2.0 Oc1ccc2cccc(N3CCNCC3)c2c1
CHEMBL3644533 5ht5a_human Human No 8.5 Ki = 3.3 nM Bind
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 2 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3F)c2c1
CHEMBL3644534 5ht5a_human Human No 8.5 Ki = 3.4 nM Bind
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.
342 2 2 2 3.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3Cl)c2c1
CHEMBL3654196 5ht5a_human Human No 8.4 Ki = 3.6 nM Bind
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 1 2.5 NC(N)=NC(=O)N1CCc2cccc(-c3cc(F)c(F)cc3F)c2C1
CHEMBL3654211 5ht5a_human Human No 8.4 Ki = 3.7 nM Bind
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 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3cc(F)c(F)cc3F)c2C1
CHEMBL3644526 5ht5a_human Human No 8.4 Ki = 3.7 nM Bind
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 2 3.4 Cc1nc2ccc(C(=O)N=C(N)N)cc2c(-c2c(F)cc(F)cc2F)c1C
CHEMBL3654203 5ht5a_human Human No 8.4 Ki = 3.9 nM Bind
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 2 2.1 Cc1ccc(-c2ncc(F)cc2F)c2c1CCN(C(=O)N=C(N)N)C2
CHEMBL252258 5ht5a_human Human No 5.5 Ki = 3000 nM Bind
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2
CHEMBL349843 5ht5a_human Human No 5.5 Ki = 3067 nM Bind
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 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C
CHEMBL1181641 5ht5a_human Human No 7.5 Ki = 31.6 nM Bind
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
512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1
CHEMBL186849 5ht5a_human Human No 7.5 Ki = 31.6 nM Bind
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
512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1
CHEMBL189689 5ht5a_human Human No 7.5 Ki = 31.6 nM Bind
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
512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)CCC1CCCC1
CHEMBL336124 5ht5a_rat Rat No 6.5 Ki = 310 nM Bind
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 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(OC)c1
CHEMBL425190 5ht5a_human Human Yes 5.5 Ki = 3162.3 nM Bind
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2
CHEMBL1181669 5ht5a_human Human No 5.5 Ki = 3162.3 nM Bind
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
407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1
CHEMBL188050 5ht5a_human Human No 5.5 Ki = 3162.3 nM Bind
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
407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1
CHEMBL269236 5ht5a_human Human Yes 5.5 Ki = 3200 nM Bind
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 1.8 c1ccc2c3c([nH]c2c1)CNCC3
CHEMBL3753318 5ht5a_human Human No 5.5 Ki = 3235.9 nM Bind
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 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12
CHEMBL1200485 5ht5a_human Human Yes 5.5 Ki = 3296 nM Bind
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
464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1
CHEMBL1336 5ht5a_human Human Yes 5.5 Ki = 3296 nM Bind
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
464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1
CHEMBL271253 5ht5a_human Human No 7.5 Ki = 33.4 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2c(Cl)ccc(Cl)c21
CHEMBL2111848 5ht5a_mouse Mouse No 6.5 Ki = 330 nM Bind
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 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2
CHEMBL2391541 5ht5a_human Human Yes 5.5 Ki = 3311.3 nM Bind
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 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12
CHEMBL2058706 5ht5a_human Human No 5.5 Ki = 3324 nM Bind
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
318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1
CHEMBL424258 5ht5a_mouse Mouse No 6.5 Ki = 335 nM Bind
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 c1ccc(OCCCN2CCc3c([nH]c4ccccc34)C2)cc1
CHEMBL3764133 5ht5a_human Human No 6.5 Ki = 337 nM Bind
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21
CHEMBL3765875 5ht5a_human Human No 6.5 Ki = 337 nM Bind
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21
CHEMBL2058703 5ht5a_human Human No 5.5 Ki = 3372 nM Bind
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
318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1
CHEMBL126138 5ht5a_human Human No 6.5 Ki = 340 nM Bind
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 4.3 Cn1c2c(c3ccccc31)CN(CCC/C(=N/O)c1ccc(F)cc1)CC2
CHEMBL92139 5ht5a_rat Rat No 5.5 Ki = 3400 nM Bind
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 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1
CHEMBL13864 5ht5a_human Human No 6.5 Ki = 347 nM Bind
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
181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1
CHEMBL538340 5ht5a_human Human No 6.5 Ki = 347 nM Bind
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
181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1
CHEMBL340646 5ht5a_human Human No 6.5 Ki = 350 nM Bind
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 4 4.0 COc1ccc(OCCCN2CCc3c(c4ccccc4n3C)C2)cc1
CHEMBL446356 5ht5a_mouse Mouse No 6.5 Ki = 350 nM Bind
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 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2
CHEMBL126823 5ht5a_mouse Mouse No 6.4 Ki = 360 nM Bind
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 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2
CHEMBL256693 5ht5a_human Human No 7.4 Ki = 37 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
309 2 2 5 2.8 CC1NC(NCC2COc3ccccc3O2)=Nc2ccccc21
CHEMBL133433 5ht5a_rat Rat No 6.4 Ki = 379 nM Bind
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 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1O
CHEMBL1190709 5ht5a_human Human Yes 7.4 Ki = 38 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21
CHEMBL541396 5ht5a_human Human Yes 7.4 Ki = 38 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21
CHEMBL1190709 5ht5a_human Human Yes 7.4 Ki = 38 nM Bind
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
161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21
CHEMBL541396 5ht5a_human Human Yes 7.4 Ki = 38 nM Bind
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
161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21
CHEMBL133935 5ht5a_rat Rat No 6.4 Ki = 388 nM Bind
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 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(OC)c1
CHEMBL582877 5ht5a_human Human Yes 6.4 Ki = 389 nM Bind
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
295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1
CHEMBL257450 5ht5a_human Human No 6.4 Ki = 397 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
207 2 2 3 1.9 CC1NC(NCCF)=Nc2ccccc21
CHEMBL1181643 5ht5a_human Human No 6.4 Ki = 398.1 nM Bind
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
506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1
CHEMBL187029 5ht5a_human Human No 6.4 Ki = 398.1 nM Bind
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
506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1
CHEMBL3644529 5ht5a_human Human No 8.4 Ki = 4.1 nM Bind
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.
360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccc(F)cc3Cl)c2c1
CHEMBL3654213 5ht5a_human Human No 8.4 Ki = 4.2 nM Bind
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 2 1.8 NC(N)=NC(=O)N1CCc2cccc(-c3ncc(F)cc3F)c2C1
CHEMBL3654195 5ht5a_human Human No 8.4 Ki = 4.3 nM Bind
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 2 2.4 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3F)c2C1
CHEMBL3644539 5ht5a_human Human No 8.3 Ki = 4.6 nM Bind
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 2 3.5 NC(N)=NC(=O)c1ccc2c(C(F)F)cnc(-c3c(F)cccc3F)c2c1
CHEMBL3644536 5ht5a_human Human No 8.3 Ki = 4.7 nM Bind
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 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3Cl)c2c1
CHEMBL401745 5ht5a_human Human No 8.3 Ki = 4.7 nM Bind
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
239 1 2 4 2.3 COc1cc(Cl)c(C)c2c1N=C(N)NC2C
CHEMBL37844 5ht5a_rat Rat No 8.3 Ki = 4.9 nM Bind
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 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1O
CHEMBL277120 5ht5a_human Human Yes 7.4 Ki = 40 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2
CHEMBL442 5ht5a_human Human Yes 7.4 Ki = 40 nM Bind
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL277120 5ht5a_mouse Mouse Yes 7.4 Ki = 40 nM Bind
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 2.2 N1CCN(CC1)c1cccc2c1cccc2
CHEMBL126667 5ht5a_human Human No 6.4 Ki = 400 nM Bind
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 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1
CHEMBL3819366 5ht5a_human Human No 6.4 Ki = 400 nM Bind
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 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1
CHEMBL93868 5ht5a_rat Rat No 5.4 Ki = 4000 nM Bind
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 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12
CHEMBL441896 5ht5a_human Human No 6.4 Ki = 415 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
195 0 2 3 2.0 C[C@H]1NC(N)=Nc2cccc(Cl)c21
CHEMBL4278465 5ht5a_human Human No 5.4 Ki = 4152 nM Bind
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL3754496 5ht5a_human Human No 5.4 Ki = 4265.8 nM Bind
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 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12
CHEMBL1548 5ht5a_human Human Yes 7.4 Ki = 43 nM Bind
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
215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1
CHEMBL423527 5ht5a_rat Rat No 6.4 Ki = 431 nM Bind
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)C[C@H]1C[C@@H]1c1ccccc1OC
CHEMBL125361 5ht5a_mouse Mouse No 6.4 Ki = 435 nM Bind
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
346 7 0 2 5.3 Cn1c2c(c3ccccc31)CN(CCCCCCc1ccccc1)CC2
CHEMBL263700 5ht5a_rat Rat No 5.4 Ki = 4500 nM Bind
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 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12
CHEMBL3770106 5ht5a_human Human Yes 6.3 Ki = 457 nM Bind
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 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1
CHEMBL267615 5ht5a_human Human Yes 5.3 Ki = 4620 nM Bind
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 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC
CHEMBL1188440 5ht5a_human Human No 6.3 Ki = 463 nM Bind
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
161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2
CHEMBL536335 5ht5a_human Human No 6.3 Ki = 463 nM Bind
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
161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2
CHEMBL1188501 5ht5a_human Human No 6.3 Ki = 466 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL2436555 5ht5a_human Human No 6.3 Ki = 466 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL536539 5ht5a_human Human No 6.3 Ki = 466 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL2058428 5ht5a_human Human No 5.3 Ki = 4681 nM Bind
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
346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C
CHEMBL4209942 5ht5a_human Human No 5.3 Ki = 4700 nM Bind
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1
CHEMBL429925 5ht5a_human Human No 6.3 Ki = 488 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
243 1 2 3 2.5 CC1NC(NCC(F)(F)F)=Nc2ccccc21
CHEMBL4293307 5ht5a_human Human No 5.3 Ki = 4973 nM Bind
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1
CHEMBL3763779 5ht5a_human Human No 8.3 Ki = 5 nM Bind
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1
CHEMBL3765873 5ht5a_human Human No 8.3 Ki = 5 nM Bind
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1
CHEMBL270177 5ht5a_human Human Yes 8.3 Ki = 5.0 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21
CHEMBL361256 5ht5a_human Human No 8.3 Ki = 5.0 nM Bind
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
518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)/C=C/c1ccccc1
CHEMBL270177 5ht5a_human Human Yes 8.3 Ki = 5.1 nM Bind
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
195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21
CHEMBL270177 5ht5a_human Human Yes 8.3 Ki = 5.1 nM Bind
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
195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21
CHEMBL3644531 5ht5a_human Human No 8.3 Ki = 5.3 nM Bind
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 3 2.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3F)c2c1
CHEMBL429136 5ht5a_human Human No 8.2 Ki = 5.7 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21
CHEMBL1181665 5ht5a_human Human No 7.3 Ki = 50.1 nM Bind
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
537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1
CHEMBL187928 5ht5a_human Human No 7.3 Ki = 50.1 nM Bind
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
537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1
CHEMBL96729 5ht5a_human Human Yes 5.3 Ki = 5000 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1
CHEMBL96729 5ht5a_human Human Yes 5.3 Ki = 5000 nM Bind
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 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1
CHEMBL1181625 5ht5a_human Human No 6.3 Ki = 501.2 nM Bind
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
580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1
CHEMBL185996 5ht5a_human Human No 6.3 Ki = 501.2 nM Bind
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
580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1
CHEMBL1188501 5ht5a_human Human No 6.3 Ki = 501.2 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL2436555 5ht5a_human Human No 6.3 Ki = 501.2 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL536539 5ht5a_human Human No 6.3 Ki = 501.2 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL256047 5ht5a_human Human No 6.3 Ki = 504 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
293 2 2 3 3.5 C[C@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21
CHEMBL341373 5ht5a_rat Rat No 6.3 Ki = 506 nM Bind
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)C[C@H]1C[C@@H]1c1ccccc1O
CHEMBL2058426 5ht5a_human Human No 5.3 Ki = 5080 nM Bind
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
346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C
CHEMBL338091 5ht5a_mouse Mouse Yes 6.3 Ki = 512 nM Bind
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 2 4.3 O=C(CCCN1CCc2[nH]c3ccccc3c2C1)c1ccc(F)cc1
CHEMBL7318 5ht5a_human Human Yes 5.3 Ki = 5160 nM Bind
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 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1
CHEMBL3326993 5ht5a_human Human No 6.3 Ki = 517 nM Bind
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1
CHEMBL92879 5ht5a_mouse Mouse Yes 5.3 Ki = 5300 nM Bind
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 2 1.8 Cn1c2c(c3ccccc31)CNCC2
CHEMBL92879 5ht5a_mouse Mouse Yes 5.3 Ki = 5300 nM Bind
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2
CHEMBL511879 5ht5a_human Human No 5.3 Ki = 5355 nM Bind
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
318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O
CHEMBL96504 5ht5a_human Human No 7.3 Ki = 55 nM Bind
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2
CHEMBL96504 5ht5a_human Human No 7.3 Ki = 55 nM Bind
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 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2
CHEMBL129163 5ht5a_mouse Mouse No 6.3 Ki = 550 nM Bind
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 4.2 O=C(CCCN1CCc2c([nH]c3ccccc23)C1)c1ccccc1
CHEMBL1189631 5ht5a_human Human No 6.3 Ki = 550 nM Bind
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
165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1
CHEMBL539103 5ht5a_human Human No 6.3 Ki = 550 nM Bind
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
165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1
CHEMBL464099 5ht5a_human Human Yes 6.3 Ki = 566 nM Bind
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 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C
CHEMBL132123 5ht5a_rat Rat No 7.2 Ki = 58 nM Bind
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 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(O)c1
CHEMBL2181169 5ht5a_human Human No 5.2 Ki = 5805 nM Bind
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1
CHEMBL126737 5ht5a_mouse Mouse No 6.2 Ki = 590 nM Bind
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2
CHEMBL3770981 5ht5a_human Human No 6.2 Ki = 595 nM Bind
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 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1
CHEMBL3644538 5ht5a_human Human No 8.2 Ki = 6.2 nM Bind
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 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ncc(F)cc3Cl)c2c1
CHEMBL271298 5ht5a_human Human Yes 8.2 Ki = 6.3 nM Bind
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
243 0 2 3 2.9 CNC1=Nc2ccc(Cl)c(Cl)c2C(C)N1
CHEMBL408152 5ht5a_human Human Yes 8.2 Ki = 6.3 nM Bind
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 4 1.3 COc1cccc2c1N=C(N)NC2C
CHEMBL404511 5ht5a_human Human Yes 8.2 Ki = 6.3 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21
CHEMBL1181770 5ht5a_human Human Yes 8.2 Ki = 6.3 nM Bind
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
511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C
CHEMBL272781 5ht5a_human Human Yes 8.2 Ki = 6.5 nM Bind
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
229 0 2 3 2.6 CC1NC(N)=Nc2c(Cl)ccc(Cl)c21
CHEMBL3654202 5ht5a_human Human No 8.2 Ki = 6.6 nM Bind
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 1 3.5 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(Cl)c2C(F)C1
CHEMBL541993 5ht5a_human Human No 8.2 Ki = 6.8 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21
CHEMBL3654201 5ht5a_human Human No 8.2 Ki = 6.9 nM Bind
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 2 1.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(F)cc3F)c2C1
CHEMBL126438 5ht5a_mouse Mouse No 6.2 Ki = 600 nM Bind
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 c1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1
CHEMBL2429890 5ht5a_human Human No 5.2 Ki = 6060 nM Bind
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2
CHEMBL126823 5ht5a_human Human No 6.2 Ki = 620 nM Bind
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 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2
CHEMBL4466483 5ht5a_human Human No 5.2 Ki = 6200 nM Bind
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
411 3 0 5 6.4 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4SC=C5)C(F)(F)F
CHEMBL97518 5ht5a_mouse Mouse No 7.2 Ki = 63 nM Bind
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 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1
CHEMBL282199 5ht5a_human Human Yes 7.2 Ki = 63.1 nM Bind
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O
CHEMBL13816 5ht5a_human Human No 6.2 Ki = 630 nM Bind
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 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21
CHEMBL1184710 5ht5a_human Human No 6.2 Ki = 631.0 nM Bind
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
491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1
CHEMBL365084 5ht5a_human Human No 6.2 Ki = 631.0 nM Bind
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
491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1
CHEMBL267930 5ht5a_human Human Yes 4.2 Ki = 63000 nM Bind
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
395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1
CHEMBL1181634 5ht5a_human Human No 5.2 Ki = 6309.6 nM Bind
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
491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1
CHEMBL186450 5ht5a_human Human No 5.2 Ki = 6309.6 nM Bind
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
491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1
CHEMBL1188517 5ht5a_human Human No 6.2 Ki = 647 nM Bind
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
165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1
CHEMBL536562 5ht5a_human Human No 6.2 Ki = 647 nM Bind
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
165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1
CHEMBL282199 5ht5a_human Human Yes 7.2 Ki = 65 nM Bind
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O
CHEMBL126188 5ht5a_mouse Mouse No 6.2 Ki = 650 nM Bind
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 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1cccc3ccccc13)CC2
CHEMBL340511 5ht5a_mouse Mouse No 6.2 Ki = 655 nM Bind
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 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1ccc3ccccc3c1)CC2
CHEMBL25212 5ht5a_human Human Yes 6.2 Ki = 658 nM Bind
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
147 0 2 3 0.7 NC1=Nc2ccccc2CN1
CHEMBL557381 5ht5a_human Human Yes 6.2 Ki = 658 nM Bind
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
147 0 2 3 0.7 NC1=Nc2ccccc2CN1
CHEMBL1170237 5ht5a_human Human No 5.2 Ki = 6725 nM Bind
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
332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O
CHEMBL4204036 5ht5a_human Human No 5.2 Ki = 6800 nM Bind
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1
CHEMBL515472 5ht5a_human Human No 5.2 Ki = 6814 nM Bind
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1
CHEMBL2058429 5ht5a_human Human No 5.2 Ki = 6913 nM Bind
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
346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C
CHEMBL3644532 5ht5a_human Human No 8.2 Ki = 7.1 nM Bind
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 3 2.6 COc1cccc(F)c1-c1ncc(F)c2ccc(C(=O)N=C(N)N)cc12
CHEMBL334553 5ht5a_rat Rat No 6.1 Ki = 736 nM Bind
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 3.7 CCCN(CCC)[C@@H]1C[C@@H]1c1cccc(OC)c1
CHEMBL4469848 5ht5a_human Human No 5.1 Ki = 7400 nM Bind
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
395 3 0 5 6.0 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL3104091 5ht5a_human Human No 6.1 Ki = 741.3 nM Bind
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1
CHEMBL126724 5ht5a_mouse Mouse No 7.1 Ki = 75 nM Bind
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 2 4.1 Fc1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1
CHEMBL128099 5ht5a_mouse Mouse No 7.1 Ki = 75 nM Bind
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 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2
CHEMBL3104091 5ht5a_human Human No 6.1 Ki = 750 nM Bind
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1
CHEMBL2432039 5ht5a_human Human No 5.1 Ki = 7502 nM Bind
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42
CHEMBL133020 5ht5a_rat Rat No 6.1 Ki = 752 nM Bind
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 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1O
CHEMBL494675 5ht5a_human Human Yes 7.1 Ki = 76 nM Bind
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1
CHEMBL2205811 5ht5a_human Human No 5.1 Ki = 7815 nM Bind
Binding affinity to 5-HT5A receptorBinding affinity to 5-HT5A receptor
309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1
CHEMBL2058419 5ht5a_human Human No 5.1 Ki = 7828 nM Bind
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
332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O
CHEMBL1181776 5ht5a_human Human No 7.1 Ki = 79.4 nM Bind
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
531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1
CHEMBL191583 5ht5a_human Human No 7.1 Ki = 79.4 nM Bind
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
531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1
CHEMBL1184673 5ht5a_human Human No 7.1 Ki = 79.4 nM Bind
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
527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1
CHEMBL363678 5ht5a_human Human No 7.1 Ki = 79.4 nM Bind
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
527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1
CHEMBL270840 5ht5a_human Human Yes 6.1 Ki = 805 nM Bind
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 3 2.1 CCCC1NC(N)=Nc2ccccc21
CHEMBL1188501 5ht5a_human Human No 6.1 Ki = 807 nM Bind
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
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL2436555 5ht5a_human Human No 6.1 Ki = 807 nM Bind
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
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL536539 5ht5a_human Human No 6.1 Ki = 807 nM Bind
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
181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1
CHEMBL39 5ht5a_human Human Yes 7.1 Ki = 82 nM Bind
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2
CHEMBL4218679 5ht5a_human Human No 5.1 Ki = 8200 nM Bind
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO
CHEMBL270176 5ht5a_human Human Yes 7.1 Ki = 84.4 nM Bind
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
209 1 2 3 2.3 CCC1NC(N)=Nc2cccc(Cl)c21
CHEMBL1506260 5ht5a_human Human Yes 6.1 Ki = 845 nM Bind
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21
CHEMBL295234 5ht5a_human Human Yes 6.1 Ki = 845 nM Bind
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21
CHEMBL1258223 5ht5a_human Human No 5.1 Ki = 8589 nM Bind
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1
CHEMBL4541409 5ht5a_human Human No 5.1 Ki = 8690 nM Bind
Inhibition of 5HT5A (unknown origin)Inhibition of 5HT5A (unknown origin)
487 7 1 9 3.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12
CHEMBL272355 5ht5a_human Human No 7.1 Ki = 87 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
225 2 2 3 2.2 CC1NC(NCC(F)F)=Nc2ccccc21
CHEMBL478 5ht5a_mouse Mouse Yes 5.1 Ki = 8700 nM Bind
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
196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1
CHEMBL478 5ht5a_mouse Mouse Yes 5.1 Ki = 8700 nM Bind
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1
CHEMBL130586 5ht5a_mouse Mouse No 6.1 Ki = 875 nM Bind
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
396 7 0 3 5.5 c1ccc(Cn2c3c(c4ccccc42)CN(CCCOc2ccccc2)CC3)cc1
CHEMBL4167315 5ht5a_human Human No 6.1 Ki = 875 nM Bind
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1
CHEMBL1196644 5ht5a_human Human No 6.1 Ki = 882 nM Bind
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
161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2
CHEMBL557746 5ht5a_human Human No 6.1 Ki = 882 nM Bind
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
161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2
CHEMBL2442272 5ht5a_human Human No 7.1 Ki = 89 nM Bind
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
304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1
CHEMBL272752 5ht5a_human Human Yes 6.1 Ki = 892 nM Bind
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
181 0 2 3 1.4 NC1=Nc2c(Cl)cccc2CN1
CHEMBL1644978 5ht5a_human Human No 6.1 Ki = 894 nM Bind
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL263881 5ht5a_human Human Yes 8.1 Ki = 9 nM Bind
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC
CHEMBL128945 5ht5a_mouse Mouse No 7.1 Ki = 90 nM Bind
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 3 4.6 COc1ccc(CCCCN2CCc3c(c4ccccc4n3C)C2)cc1
CHEMBL1188596 5ht5a_human Human No 6.0 Ki = 911 nM Bind
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
165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1
CHEMBL536790 5ht5a_human Human No 6.0 Ki = 911 nM Bind
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
165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1
CHEMBL2058427 5ht5a_human Human No 5.0 Ki = 9118 nM Bind
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
346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C
CHEMBL126994 5ht5a_human Human No 6.0 Ki = 930 nM Bind
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 3.8 Cn1c2c(c3ccccc31)CN(CCOc1ccc(F)cc1)CC2
CHEMBL3764335 5ht5a_human Human No 6.0 Ki = 933 nM Bind
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21
CHEMBL3765876 5ht5a_human Human No 6.0 Ki = 933 nM Bind
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21
CHEMBL341506 5ht5a_mouse Mouse No 7.0 Ki = 95 nM Bind
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 Cn1c2c(c3ccccc31)CN(CCCCc1ccc(F)cc1)CC2
CHEMBL4572614 5ht5a_human Human No 5.0 Ki = 9500 nM Bind
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
410 3 0 6 5.7 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL404365 5ht5a_human Human No 7.0 Ki = 96 nM Bind
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
261 2 2 5 1.3 CC1NC(NCC2COCCO2)=Nc2ccccc21
CHEMBL463249 5ht5a_human Human No 5.0 Ki = 9621 nM Bind
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
332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O
CHEMBL1194499 5ht5a_human Human Yes 7.0 Ki = 97 nM Bind
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
177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2
CHEMBL552782 5ht5a_human Human Yes 7.0 Ki = 97 nM Bind
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
177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2
CHEMBL128185 5ht5a_mouse Mouse No 7.0 Ki = 98 nM Bind
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 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1
CHEMBL2164327 5ht5a_human Human Yes 7.0 Ki = 98.5 nM Bind
Displacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysis
283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C
CHEMBL401541 5ht5a_human Human Yes 7.0 Ki = 99 nM Bind
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
181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1
CHEMBL556983 5ht5a_human Human Yes 7.0 Ki = 99 nM Bind
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
181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1
CHEMBL3771331 5ht5a_human Human No 6.0 Ki = 994 nM Bind
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 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1
CHEMBL135894 5ht5a_rat Rat No 6.0 Ki = 998 nM Bind
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 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1OC