Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL5077128 214483 7 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assayAgonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assay
ChEMBL None None None CS(=O)(=O)C1(CNCc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5082447 214803 2 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assayAgonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assay
ChEMBL None None None CS(=O)(=O)C1(CNCc2ccc(Cl)c3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
785909 41048 7 None 1 2 Human 4.3 pEC50 = 4.3 Functional
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]
ChEMBL 336 4 1 3 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C nan
CHEMBL1487650 41048 7 None 1 2 Human 4.3 pEC50 = 4.3 Functional
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]
ChEMBL 336 4 1 3 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C nan
1765347 56119 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
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]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
CHEMBL1606743 56119 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
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]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
CHEMBL1625496 56119 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
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]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
253793 10556 45 None -1 2 Human 4.1 pEC50 = 4.1 Functional
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]
ChEMBL 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 nan
CHEMBL1169627 10556 45 None -1 2 Human 4.1 pEC50 = 4.1 Functional
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]
ChEMBL 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 nan
1795 1591 64 None -10 4 Human 4.1 pEC50 = 4.1 Functional
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]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
4186 1591 64 None -10 4 Human 4.1 pEC50 = 4.1 Functional
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]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
CHEMBL517986 1591 64 None -10 4 Human 4.1 pEC50 = 4.1 Functional
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]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
16006492 97469 7 None - 0 Human 8.5 pKd = 8.5 Functional
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
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 97469 7 None - 0 Human 8.5 pKd = 8.5 Functional
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
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
16006492 97469 7 None - 0 Human 8.5 pKd = 8.5 Functional
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
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270177 97469 7 None - 0 Human 8.5 pKd = 8.5 Functional
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
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458393 155596 4 None - 0 Human 7.4 pKd = 7.4 Functional
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
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 155596 4 None - 0 Human 7.4 pKd = 7.4 Functional
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
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458392 97426 5 None - 0 Human 8.1 pKd = 8.1 Functional
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
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 97426 5 None - 0 Human 8.1 pKd = 8.1 Functional
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
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
5329102 194726 86 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194726 86 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
1353 1911 93 None -77 83 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 93 None -77 83 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 93 None -77 83 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 93 None -77 83 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 93 None -77 83 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
1613 2348 53 None -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 53 None -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 53 None -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 53 None -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 53 None -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3158 56267 27 None - 20 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56267 27 None - 20 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
2247 505 81 None - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 81 None - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 81 None - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 81 None - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 81 None - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
135409453 3773 41 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 41 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 41 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
1427 2013 54 None - 27 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 54 None - 27 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 54 None - 27 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 54 None - 27 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 54 None - 27 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
135398745 2914 112 None -109 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 112 None -109 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 112 None -109 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 112 None -109 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
1400 1957 70 None - 3 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1957 70 None - 3 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1957 70 None - 3 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1957 70 None - 3 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1957 70 None - 3 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1957 70 None - 3 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
2726 919 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
43815 186920 64 None - 25 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 186920 64 None - 25 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 186920 64 None - 25 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
21722 17992 31 None - 6 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17992 31 None - 6 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
191 403 98 None - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 98 None - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 98 None - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 98 None - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 98 None - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
1224 1432 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1432 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1432 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1432 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1432 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1432 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
2284 3182 33 None - 29 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 33 None - 29 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 33 None - 29 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 33 None - 29 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 33 None - 29 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
44469677 15173 0 None - 0 Human 9.0 pIC50 = 9 Binding
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
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
CHEMBL1210154 15173 0 None - 0 Human 9.0 pIC50 = 9 Binding
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
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
10383252 4587 0 None - 0 Human 6.0 pIC50 = 6 Binding
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
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3C(C)(C)CNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102645 4587 0 None - 0 Human 6.0 pIC50 = 6 Binding
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
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3C(C)(C)CNS3(=O)=O)cc12 10.1021/jm00045a006
72548703 161567 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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
ChEMBL 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 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161567 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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
ChEMBL 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 10.1016/j.bmcl.2018.03.093
10404770 4716 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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
ChEMBL 336 6 2 3 1.0 CN(C)CCc1c[nH]c2ccc(CCN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103549 4716 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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
ChEMBL 336 6 2 3 1.0 CN(C)CCc1c[nH]c2ccc(CCN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
10021702 109392 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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
ChEMBL 364 7 1 3 1.7 CCN1CCN(CCc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL321963 109392 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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
ChEMBL 364 7 1 3 1.7 CCN1CCN(CCc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
10043491 109824 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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
ChEMBL 350 5 1 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CCCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL323334 109824 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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
ChEMBL 350 5 1 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CCCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
5 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5202 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
CHEMBL39 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
DB08839 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5202 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
CHEMBL39 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
DB08839 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 72 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5 139 72 None -323 54 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 139 72 None -323 54 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 139 72 None -323 54 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 139 72 None -323 54 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
10315894 4687 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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
ChEMBL 350 6 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CCN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103371 4687 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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
ChEMBL 350 6 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CCN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
10412397 4688 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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
ChEMBL 469 8 2 4 2.8 CC(=O)Nc1ccc(CN2CCN(Cc3ccc4[nH]cc(CCN(C)C)c4c3)S2(=O)=O)cc1 10.1021/jm00045a006
CHEMBL103388 4688 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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
ChEMBL 469 8 2 4 2.8 CC(=O)Nc1ccc(CN2CCN(Cc3ccc4[nH]cc(CCN(C)C)c4c3)S2(=O)=O)cc1 10.1021/jm00045a006
10404070 78448 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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
ChEMBL 325 4 1 4 1.4 CN1CCN(Cc2ccc3scc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL2111620 78448 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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
ChEMBL 325 4 1 4 1.4 CN1CCN(Cc2ccc3scc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
10337965 108591 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CC(C)(C)NS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL320412 108591 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CC(C)(C)NS3(=O)=O)cc12 10.1021/jm00045a006
5 139 72 None -323 54 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 72 None -323 54 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 72 None -323 54 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 72 None -323 54 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5 139 72 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
5202 139 72 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
CHEMBL39 139 72 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
DB08839 139 72 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
10885636 111016 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 111016 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
2543 3707 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
5358 3707 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
54 3707 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
CHEMBL128 3707 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
DB00669 3707 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
9998879 107500 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 364 6 1 3 2.0 CC(C)N1CCN(Cc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL318571 107500 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 364 6 1 3 2.0 CC(C)N1CCN(Cc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
11730467 11028 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 11028 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11722814 4762 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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
ChEMBL 308 4 2 3 0.7 CN1CCN(Cc2ccc3[nH]cc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL103854 4762 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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
ChEMBL 308 4 2 3 0.7 CN1CCN(Cc2ccc3[nH]cc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
10245588 107827 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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
ChEMBL 322 4 1 3 1.3 CN(C)CCc1c[nH]c2ccc(N3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL319223 107827 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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
ChEMBL 322 4 1 3 1.3 CN(C)CCc1c[nH]c2ccc(N3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
5 139 72 None -323 54 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
5202 139 72 None -323 54 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
CHEMBL39 139 72 None -323 54 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
DB08839 139 72 None -323 54 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
10340828 4364 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 398 6 1 3 2.8 CN(C)CCc1c[nH]c2ccc(N3CCN(Cc4ccccc4)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL101138 4364 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 398 6 1 3 2.8 CN(C)CCc1c[nH]c2ccc(N3CCN(Cc4ccccc4)S3(=O)=O)cc12 10.1021/jm00045a006
10471382 4572 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 322 5 2 3 0.9 CN(C)CCc1c[nH]c2ccc(CN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102548 4572 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 322 5 2 3 0.9 CN(C)CCc1c[nH]c2ccc(CN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
10471383 4578 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 322 5 2 3 0.9 CNCCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102586 4578 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 322 5 2 3 0.9 CNCCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
9819150 4668 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 336 5 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103205 4668 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 336 5 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
60152964 126790 0 None - 1 Human 9.2 pKi = 9.2 Binding
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).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
CHEMBL3654198 126790 0 None - 1 Human 9.2 pKi = 9.2 Binding
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).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
60151043 126798 0 None - 1 Human 9.1 pKi = 9.1 Binding
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).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3c(F)cccc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654206 126798 0 None - 1 Human 9.1 pKi = 9.1 Binding
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).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3c(F)cccc3F)ccc(F)c2C2(CC2)C1 nan
3233 3512 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3247 3512 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
6604889 3512 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
CHEMBL282199 3512 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
DB13988 3512 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
60151044 126804 0 None - 1 Human 9.1 pKi = 9.1 Binding
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).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654212 126804 0 None - 1 Human 9.1 pKi = 9.1 Binding
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).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
60151042 126800 0 None - 1 Human 9.1 pKi = 9.1 Binding
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).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3c(F)cc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654208 126800 0 None - 1 Human 9.1 pKi = 9.1 Binding
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).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3c(F)cc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
91819725 126806 0 None - 1 Human 9.0 pKi = 9.0 Binding
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).
ChEMBL 356 1 2 1 2.9 NC(N)=NC(=O)N1Cc2c(-c3ccccc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654214 126806 0 None - 1 Human 9.0 pKi = 9.0 Binding
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).
ChEMBL 356 1 2 1 2.9 NC(N)=NC(=O)N1Cc2c(-c3ccccc3F)ccc(F)c2C2(CC2)C1 nan
4106 2502 22 None -14 34 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 2502 22 None -14 34 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 2502 22 None -14 34 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 2502 22 None -14 34 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
4106 2502 22 None -14 34 Human 9.0 pKi = 9 Binding
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
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 2502 22 None -14 34 Human 9.0 pKi = 9 Binding
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
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 2502 22 None -14 34 Human 9.0 pKi = 9 Binding
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
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 2502 22 None -14 34 Human 9.0 pKi = 9 Binding
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
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
60150902 126789 0 None - 1 Human 9.0 pKi = 9.0 Binding
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).
ChEMBL 382 1 2 1 3.2 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
CHEMBL3654197 126789 0 None - 1 Human 9.0 pKi = 9.0 Binding
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).
ChEMBL 382 1 2 1 3.2 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
60152965 126791 0 None - 1 Human 9.0 pKi = 9.0 Binding
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).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cccc3F)c2C1 nan
CHEMBL3654199 126791 0 None - 1 Human 9.0 pKi = 9.0 Binding
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).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cccc3F)c2C1 nan
50923586 125160 0 None - 1 Human 8.9 pKi = 8.9 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644535 125160 0 None - 1 Human 8.9 pKi = 8.9 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3c(F)cccc3F)c2c1 nan
60150904 126802 0 None - 1 Human 8.9 pKi = 8.9 Binding
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).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3cc(F)c(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654210 126802 0 None - 1 Human 8.9 pKi = 8.9 Binding
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).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3cc(F)c(F)cc3F)ccc(F)c2C2(CC2)C1 nan
67961424 125150 0 None - 1 Human 8.9 pKi = 8.9 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2ncc(Cl)c(-c3ccc(F)cc3F)c2c1 nan
CHEMBL3644525 125150 0 None - 1 Human 8.9 pKi = 8.9 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2ncc(Cl)c(-c3ccc(F)cc3F)c2c1 nan
50923580 125155 0 None - 1 Human 8.9 pKi = 8.9 Binding
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.
ChEMBL 358 2 2 2 3.0 Cc1cnc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644530 125155 0 None - 1 Human 8.9 pKi = 8.9 Binding
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.
ChEMBL 358 2 2 2 3.0 Cc1cnc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
44456033 155567 3 None 1 8 Rat 8.9 pKi = 8.9 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404372 155567 3 None 1 8 Rat 8.9 pKi = 8.9 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
50923443 125153 0 None - 1 Human 8.9 pKi = 8.9 Binding
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.
ChEMBL 344 2 2 2 2.7 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644528 125153 0 None - 1 Human 8.9 pKi = 8.9 Binding
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.
ChEMBL 344 2 2 2 2.7 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL5093295 215421 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNC[C@H]2CCn3ccnc3C2)c2ncccc12 10.1021/acs.jmedchem.1c02031
91819723 126799 0 None - 1 Human 8.8 pKi = 8.8 Binding
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).
ChEMBL 362 1 2 1 3.1 CC1CN(C(=O)N=C(N)N)Cc2c(-c3c(F)cccc3F)ccc(F)c21 nan
CHEMBL3654207 126799 0 None - 1 Human 8.8 pKi = 8.8 Binding
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).
ChEMBL 362 1 2 1 3.1 CC1CN(C(=O)N=C(N)N)Cc2c(-c3c(F)cccc3F)ccc(F)c21 nan
50923442 125152 0 None - 1 Human 8.8 pKi = 8.8 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3Cl)c2c1 nan
CHEMBL3644527 125152 0 None - 1 Human 8.8 pKi = 8.8 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3Cl)c2c1 nan
44456033 155567 3 None -1 8 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404372 155567 3 None -1 8 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
50923723 125165 0 None - 1 Human 8.7 pKi = 8.7 Binding
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.
ChEMBL 322 2 2 2 2.8 Cc1cnc(-c2ccccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644540 125165 0 None - 1 Human 8.7 pKi = 8.7 Binding
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.
ChEMBL 322 2 2 2 2.8 Cc1cnc(-c2ccccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
136152971 95357 0 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL256694 95357 0 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
60150901 126797 0 None - 1 Human 8.7 pKi = 8.7 Binding
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).
ChEMBL 381 1 2 2 2.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3Cl)c2C1 nan
CHEMBL3654205 126797 0 None - 1 Human 8.7 pKi = 8.7 Binding
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).
ChEMBL 381 1 2 2 2.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3Cl)c2C1 nan
50923720 125162 0 None - 1 Human 8.7 pKi = 8.7 Binding
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.
ChEMBL 340 2 2 2 2.9 Cc1cnc(-c2c(F)cccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644537 125162 0 None - 1 Human 8.7 pKi = 8.7 Binding
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.
ChEMBL 340 2 2 2 2.9 Cc1cnc(-c2c(F)cccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
16006607 95672 4 None -10 5 Human 8.0 pKi = 8 Binding
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
ChEMBL 219 2 2 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL258075 95672 4 None -10 5 Human 8.0 pKi = 8 Binding
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
ChEMBL 219 2 2 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
135458393 155596 4 None 2 5 Human 8.0 pKi = 8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 155596 4 None 2 5 Human 8.0 pKi = 8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458392 97426 5 None 1 5 Human 8.0 pKi = 8.0 Binding
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
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 97426 5 None 1 5 Human 8.0 pKi = 8.0 Binding
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
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
135458392 97426 5 None 1 5 Human 8.0 pKi = 8.0 Binding
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
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 97426 5 None 1 5 Human 8.0 pKi = 8.0 Binding
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
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
4106 2502 22 None -14 34 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 2502 22 None -14 34 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 2502 22 None -14 34 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 2502 22 None -14 34 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL5285512 194299 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 327 2 1 3 4.9 COc1ccc2[nH]c3c(-c4cn(C)c5ccccc45)nccc3c2c1 10.1021/acs.jmedchem.0c01887
44351139 18844 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128099 18844 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
44351140 19041 0 None -3 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128848 19041 0 None -3 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
1220 187 55 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 187 55 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 187 55 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 187 55 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
22857296 29150 0 None -123 4 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL13816 29150 0 None -123 4 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL5083607 214873 0 None -83 9 Human 6.0 pKi = 6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
242 470 124 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 470 124 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 470 124 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 470 124 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 470 124 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
2389 3331 118 None -346 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3331 118 None -346 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3331 118 None -346 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3331 118 None -346 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3331 118 None -346 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
135398737 958 93 None -173 89 Human 6.0 pKi = 6 Binding
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
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
38 958 93 None -173 89 Human 6.0 pKi = 6 Binding
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
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
722 958 93 None -173 89 Human 6.0 pKi = 6 Binding
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
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
CHEMBL42 958 93 None -173 89 Human 6.0 pKi = 6 Binding
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
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
DB00363 958 93 None -173 89 Human 6.0 pKi = 6 Binding
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
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
44397431 11757 0 None - 1 Human 6.0 pKi = 6 Binding
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
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181632 11757 0 None - 1 Human 6.0 pKi = 6 Binding
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
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL186261 11757 0 None - 1 Human 6.0 pKi = 6 Binding
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
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
33630 178957 99 None -13 28 Human 6.0 pKi = 6 Binding
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
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178957 99 None -13 28 Human 6.0 pKi = 6 Binding
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
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
135514796 93058 0 None 2 3 Human 7.0 pKi = 7 Binding
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
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442270 93058 0 None 2 3 Human 7.0 pKi = 7 Binding
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
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
136152962 97920 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 175 0 2 3 1.6 CNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL272517 97920 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 175 0 2 3 1.6 CNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
49756 204312 13 None -138 8 Human 5.0 pKi = 5.0 Binding
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
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL7143 204312 13 None -138 8 Human 5.0 pKi = 5.0 Binding
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
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL4520788 213975 10 None -48 25 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR5ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR5A
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
CHEMBL5078567 214565 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)C1(CNCc2ccc(Cl)c3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
11088692 18074 0 None - 1 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 326 7 0 3 4.2 CN(CCCOc1ccc(F)cc1)Cc1cn(C)c2ccccc12 10.1021/jm030080s
CHEMBL126666 18074 0 None - 1 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 326 7 0 3 4.2 CN(CCCOc1ccc(F)cc1)Cc1cn(C)c2ccccc12 10.1021/jm030080s
5 139 72 None -323 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 72 None -323 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 72 None -323 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 72 None -323 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
44351116 17950 1 None 1 2 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
CHEMBL126021 17950 1 None 1 2 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
136118729 93062 0 None 4 4 Human 7.0 pKi = 7.0 Binding
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
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442274 93062 0 None 4 4 Human 7.0 pKi = 7.0 Binding
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
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
44351116 17950 1 None -1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
CHEMBL126021 17950 1 None -1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
135367857 164604 0 None -69 8 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 164604 0 None -69 8 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
71918568 119554 4 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL3459329 119554 4 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
44351511 19382 0 None -1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 5 0 3 4.3 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL129230 19382 0 None -1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 5 0 3 4.3 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccc(F)cc1)CC2 10.1021/jm030080s
44455980 13982 0 None - 1 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL1196896 13982 0 None - 1 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL558579 13982 0 None - 1 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
72550642 114078 0 None -134 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326982 114078 0 None -134 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
71918568 119554 4 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL3459329 119554 4 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5074821 214336 1 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnn(C[C@H](C)NCc2cccc(OCc3ccccn3)c2)c1 10.1021/acs.jmedchem.1c02031
CHEMBL5087322 215085 6 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnc(NCc2ccccc2-n2ccnc2)nc1N(C)C 10.1021/acs.jmedchem.1c02031
CHEMBL5092728 215384 1 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CC(C)(C)c1ccc2c(c1)CN(C[C@@H](O)COC1CCOCC1)CC2 10.1021/acs.jmedchem.1c02031
CHEMBL5093652 215437 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None N#CC1(c2ccccc2)CCC(NCCc2nnc3ccccn23)CC1 10.1021/acs.jmedchem.1c02031
44397618 67622 0 None - 1 Human 7.9 pKi = 7.9 Binding
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
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL190382 67622 0 None - 1 Human 7.9 pKi = 7.9 Binding
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
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL5081379 214746 0 None -18 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44351102 17012 0 None 1 3 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125417 17012 0 None 1 3 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
9817810 17372 1 None -501 8 Rat 5.9 pKi = 5.9 Binding
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
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL125745 17372 1 None -501 8 Rat 5.9 pKi = 5.9 Binding
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
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
44455963 155186 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 215 1 2 3 2.5 CC1NC(NC2CCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL402400 155186 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 215 1 2 3 2.5 CC1NC(NC2CCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44351183 18860 0 None -5 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
CHEMBL128184 18860 0 None -5 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
117209962 184869 1 None -46 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184869 1 None -46 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
136118716 93059 0 None 3 3 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442271 93059 0 None 3 3 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
135367820 164821 0 None -23 5 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 164821 0 None -23 5 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
136152965 95496 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 271 3 2 3 3.9 CC1NC(NCCC2CCCCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL257302 95496 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 271 3 2 3 3.9 CC1NC(NCCC2CCCCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
11443218 67478 0 None - 1 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3ccc(CNC4CCN(Cc5ccccc5)CC4)cc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL189262 67478 0 None - 1 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3ccc(CNC4CCN(Cc5ccccc5)CC4)cc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
24865725 188084 0 None -2511 12 Human 5.9 pKi = 5.9 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL497963 188084 0 None -2511 12 Human 5.9 pKi = 5.9 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
5 139 72 None -323 54 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 72 None -323 54 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 72 None -323 54 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 72 None -323 54 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
136118613 93063 0 None -5 4 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442275 93063 0 None -5 4 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL5087322 215085 6 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnc(NCc2ccccc2-n2ccnc2)nc1N(C)C 10.1021/acs.jmedchem.1c02031
50923441 125149 0 None - 1 Human 7.9 pKi = 7.9 Binding
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.
ChEMBL 358 2 2 2 3.0 Cc1cc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc2n1 nan
CHEMBL3644524 125149 0 None - 1 Human 7.9 pKi = 7.9 Binding
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.
ChEMBL 358 2 2 2 3.0 Cc1cc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc2n1 nan
11121216 30139 0 None -6 14 Human 7.9 pKi = 7.9 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm020153s
CHEMBL138989 30139 0 None -6 14 Human 7.9 pKi = 7.9 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm020153s
10382508 207865 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
CHEMBL96504 207865 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
10382508 207865 0 None 2 3 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL96504 207865 0 None 2 3 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
44351059 19429 0 None - 1 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 0 2 4.6 Cn1c2c(c3ccccc31)CN(CCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129472 19429 0 None - 1 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 0 2 4.6 Cn1c2c(c3ccccc31)CN(CCCCc1ccccc1)CC2 10.1021/jm030080s
5 139 72 None -323 54 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 72 None -323 54 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 72 None -323 54 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 72 None -323 54 Human 6.9 pKi = 6.9 Binding
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
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
136118732 76246 0 None 1 3 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058409 76246 0 None 1 3 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
44351342 19431 0 None 1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
CHEMBL129476 19431 0 None 1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
44456251 12836 0 None - 1 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188516 12836 0 None - 1 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536561 12836 0 None - 1 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
44351183 18860 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
CHEMBL128184 18860 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
1043 1582 14 None -169 28 Human 7.9 pKi = 7.9 Binding
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
ChEMBL 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 10.1016/j.bmc.2011.08.033
149 1582 14 None -169 28 Human 7.9 pKi = 7.9 Binding
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
ChEMBL 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 10.1016/j.bmc.2011.08.033
8223 1582 14 None -169 28 Human 7.9 pKi = 7.9 Binding
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
ChEMBL 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 10.1016/j.bmc.2011.08.033
CHEMBL442 1582 14 None -169 28 Human 7.9 pKi = 7.9 Binding
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
ChEMBL 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 10.1016/j.bmc.2011.08.033
DB00696 1582 14 None -169 28 Human 7.9 pKi = 7.9 Binding
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
ChEMBL 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 10.1016/j.bmc.2011.08.033
854531 152994 30 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 244 1 1 1 4.4 c1ccc(-c2nccc3c2[nH]c2ccccc23)cc1 10.1021/acs.jmedchem.0c01887
CHEMBL3975325 152994 30 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 244 1 1 1 4.4 c1ccc(-c2nccc3c2[nH]c2ccccc23)cc1 10.1021/acs.jmedchem.0c01887
136118619 76251 0 None -2 4 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058418 76251 0 None -2 4 Human 5.9 pKi = 5.9 Binding
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
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
44456487 12873 0 None - 1 Human 6.8 pKi = 6.8 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL1188759 12873 0 None - 1 Human 6.8 pKi = 6.8 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL537248 12873 0 None - 1 Human 6.8 pKi = 6.8 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
136118616 76248 0 None -14 5 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058415 76248 0 None -14 5 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
136152963 97455 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270131 97455 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
9888494 98171 0 None -660 13 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human 5-HT5A receptor was determinedBinding affinity towards cloned human 5-HT5A receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL273921 98171 0 None -660 13 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human 5-HT5A receptor was determinedBinding affinity towards cloned human 5-HT5A receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
1043 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
149 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
8223 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
CHEMBL442 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
DB00696 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
5 139 72 None -891 54 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 72 None -891 54 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 72 None -891 54 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 72 None -891 54 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL5280298 194059 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 294 1 1 1 5.5 c1ccc2cc(-c3nccc4c3[nH]c3ccccc34)ccc2c1 10.1021/acs.jmedchem.0c01887
53381002 65465 0 None -17 4 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
CHEMBL1829959 65465 0 None -17 4 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
136152981 97567 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 203 2 2 3 2.3 CCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL270658 97567 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 203 2 2 3 2.3 CCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
136118615 93065 0 None -2 4 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442277 93065 0 None -2 4 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
44582676 189779 0 None -12 17 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189779 0 None -12 17 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
24865727 193113 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL522708 193113 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
10947658 28702 0 None -14 16 Human 7.8 pKi = 7.8 Binding
Binding affinities against 5-hydroxytryptamine 5A receptorBinding affinities against 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm020153s
CHEMBL137781 28702 0 None -14 16 Human 7.8 pKi = 7.8 Binding
Binding affinities against 5-hydroxytryptamine 5A receptorBinding affinities against 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm020153s
1043 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
149 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
8223 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
CHEMBL442 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
DB00696 1582 14 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 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 10.1016/j.bmcl.2013.12.024
9867475 18013 0 None -524 9 Rat 5.8 pKi = 5.8 Binding
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
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126340 18013 0 None -524 9 Rat 5.8 pKi = 5.8 Binding
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
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
108182 4131 22 None -51 16 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
245 4131 22 None -51 16 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
CHEMBL18041 4131 22 None -51 16 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
CHEMBL4802043 214057 11 None - 1 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CCOc1ccc(S(=O)(=O)Nc2ccc(Cl)cc2C#Cc2cnc(C(=O)O)cc2OC)c2ncccc12 10.6019/CHEMBL4800726
CHEMBL4802043 214057 11 None - 1 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CCOc1ccc(S(=O)(=O)Nc2ccc(Cl)cc2C#Cc2cnc(C(=O)O)cc2OC)c2ncccc12 10.6019/CHEMBL4800726
136152968 155324 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 245 2 2 4 2.1 CC1NC(NC[C@H]2CCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL403102 155324 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 245 2 2 4 2.1 CC1NC(NC[C@H]2CCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44351184 18861 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
CHEMBL128185 18861 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
10028436 3532 5 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
3237 3532 5 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
CHEMBL95104 3532 5 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
44351342 19431 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
CHEMBL129476 19431 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
6604756 98831 18 None -28 7 Human 6.8 pKi = 6.8 Binding
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 )
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL278751 98831 18 None -28 7 Human 6.8 pKi = 6.8 Binding
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 )
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
44582705 186996 0 None -10 13 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186996 0 None -10 13 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
13972207 119617 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
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
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL34652 119617 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
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
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
10334023 112882 5 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 283 1 2 1 4.9 c1ccc2c(-c3nccc4c3[nH]c3ccccc34)c[nH]c2c1 10.1021/acs.jmedchem.0c01887
CHEMBL3309924 112882 5 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 283 1 2 1 4.9 c1ccc2c(-c3nccc4c3[nH]c3ccccc34)c[nH]c2c1 10.1021/acs.jmedchem.0c01887
CHEMBL5268604 193574 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 299 1 3 2 4.6 Oc1ccc2[nH]c3c(-c4c[nH]c5ccccc45)nccc3c2c1 10.1021/acs.jmedchem.0c01887
5 139 72 None -323 54 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
5202 139 72 None -323 54 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
CHEMBL39 139 72 None -323 54 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
DB08839 139 72 None -323 54 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
71459269 82960 0 None -7413 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
CHEMBL2181166 82960 0 None -7413 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
44351063 19466 0 None 1 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129774 19466 0 None 1 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
44351102 17012 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125417 17012 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
132060776 162402 0 None -5 16 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 162402 0 None -5 16 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
136152974 95226 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCOCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL256049 95226 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCOCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
168268877 189970 0 None -38 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189970 0 None -38 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
44351063 19466 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129774 19466 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
25107716 2351 43 None -309 7 Human 6.8 pKi = 6.8 Binding
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
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
8436 2351 43 None -309 7 Human 6.8 pKi = 6.8 Binding
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
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
CHEMBL522691 2351 43 None -309 7 Human 6.8 pKi = 6.8 Binding
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
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
136100333 94515 0 None - 1 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL25163 94515 0 None - 1 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536557 94515 0 None - 1 Human 5.8 pKi = 5.8 Binding
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
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
44351193 116852 0 None 1 3 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338095 116852 0 None 1 3 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL5074880 214339 0 None -186 9 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
10028436 3532 5 None -87 12 Human 6.7 pKi = 6.7 Binding
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 )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3532 5 None -87 12 Human 6.7 pKi = 6.7 Binding
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 )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3532 5 None -87 12 Human 6.7 pKi = 6.7 Binding
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 )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
136118728 93061 0 None 1 3 Human 6.7 pKi = 6.7 Binding
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
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442273 93061 0 None 1 3 Human 6.7 pKi = 6.7 Binding
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
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
44351100 171471 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL446356 171471 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
44355204 21900 0 None - 1 Rat 6.7 pKi = 6.7 Binding
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
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL132019 21900 0 None - 1 Rat 6.7 pKi = 6.7 Binding
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
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
136152980 155279 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 217 3 2 3 2.7 CCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL402874 155279 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 217 3 2 3 2.7 CCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
11035049 168578 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 335 5 1 4 3.6 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(N)cc1)CC2 10.1021/jm030080s
CHEMBL435814 168578 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 335 5 1 4 3.6 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(N)cc1)CC2 10.1021/jm030080s
10924201 118165 0 None - 1 Human 5.7 pKi = 5.7 Binding
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
ChEMBL 288 5 0 3 3.0 Cn1ccc2c1CCN(CCCOc1ccc(F)cc1)C2 10.1021/jm030080s
CHEMBL340861 118165 0 None - 1 Human 5.7 pKi = 5.7 Binding
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
ChEMBL 288 5 0 3 3.0 Cn1ccc2c1CCN(CCCOc1ccc(F)cc1)C2 10.1021/jm030080s
136179599 12859 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL1188681 12859 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL537022 12859 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
75306277 109254 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 109254 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
11168912 11370 1 None - 1 Human 6.7 pKi = 6.7 Binding
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
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1179769 11370 1 None - 1 Human 6.7 pKi = 6.7 Binding
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
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL99071 11370 1 None - 1 Human 6.7 pKi = 6.7 Binding
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
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
44397486 67112 0 None - 1 Human 6.7 pKi = 6.7 Binding
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
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3cccc(CNC4CCN(Cc5ccccc5)CC4)c3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL187415 67112 0 None - 1 Human 6.7 pKi = 6.7 Binding
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
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3cccc(CNC4CCN(Cc5ccccc5)CC4)c3)cc2)cc1 10.1016/j.bmcl.2005.06.024
44456170 13151 1 None - 1 Human 5.7 pKi = 5.7 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1190707 13151 1 None - 1 Human 5.7 pKi = 5.7 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL541394 13151 1 None - 1 Human 5.7 pKi = 5.7 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
155536080 172114 0 None -13 10 Human 5.7 pKi = 5.7 Binding
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
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4472703 172114 0 None -13 10 Human 5.7 pKi = 5.7 Binding
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
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
10171 56 18 None 5 6 Mouse 8.7 pKi = 8.7 Binding
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
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
272 56 18 None 5 6 Mouse 8.7 pKi = 8.7 Binding
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
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
CHEMBL274384 56 18 None 5 6 Mouse 8.7 pKi = 8.7 Binding
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
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
16093484 98060 6 None 3 6 Human 8.7 pKi = 8.7 Binding
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
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL273170 98060 6 None 3 6 Human 8.7 pKi = 8.7 Binding
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
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
50923724 125166 0 None - 1 Human 8.6 pKi = 8.6 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3ccc(F)cc3F)c2c1 nan
CHEMBL3644541 125166 0 None - 1 Human 8.6 pKi = 8.6 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3ccc(F)cc3F)c2c1 nan
CHEMBL5079273 214611 4 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNCCc2cccnc2)c2ncccc12 10.1021/acs.jmedchem.1c02031
91819722 126796 0 None - 1 Human 8.6 pKi = 8.6 Binding
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).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cncc3F)c2C1 nan
CHEMBL3654204 126796 0 None - 1 Human 8.6 pKi = 8.6 Binding
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).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cncc3F)c2C1 nan
13972256 119618 1 None 1 2 Rat 8.6 pKi = 8.6 Binding
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
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL34653 119618 1 None 1 2 Rat 8.6 pKi = 8.6 Binding
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
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
91819720 126792 0 None - 1 Human 8.6 pKi = 8.6 Binding
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).
ChEMBL 364 1 2 1 3.0 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3ccc(F)cc3F)c2C1 nan
CHEMBL3654200 126792 0 None - 1 Human 8.6 pKi = 8.6 Binding
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).
ChEMBL 364 1 2 1 3.0 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3ccc(F)cc3F)c2C1 nan
60150905 126801 0 None - 1 Human 8.6 pKi = 8.6 Binding
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).
ChEMBL 302 1 2 1 1.9 NC(N)=NC(=O)N1Cc2c(C3CC3)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654209 126801 0 None - 1 Human 8.6 pKi = 8.6 Binding
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).
ChEMBL 302 1 2 1 1.9 NC(N)=NC(=O)N1Cc2c(C3CC3)ccc(F)c2C2(CC2)C1 nan
136152964 194939 0 None 2 8 Rat 8.5 pKi = 8.5 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL541993 194939 0 None 2 8 Rat 8.5 pKi = 8.5 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
1809 134 32 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 134 32 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 134 32 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
1809 134 32 None -229 36 Human 7.7 pKi = 7.7 Binding
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
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 134 32 None -229 36 Human 7.7 pKi = 7.7 Binding
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
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 134 32 None -229 36 Human 7.7 pKi = 7.7 Binding
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
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
44327952 208044 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm030030n
CHEMBL97518 208044 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm030030n
10872812 18113 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 388 5 0 3 5.3 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)c(Cl)c1)CC2 10.1021/jm030080s
CHEMBL126897 18113 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 388 5 0 3 5.3 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)c(Cl)c1)CC2 10.1021/jm030080s
10882775 18114 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 354 5 0 3 4.7 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)cc1)CC2 10.1021/jm030080s
CHEMBL126898 18114 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 354 5 0 3 4.7 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)cc1)CC2 10.1021/jm030080s
1524 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
197 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
3822 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
88 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
CHEMBL51 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
DB12465 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
1524 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
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
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
197 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
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
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
3822 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
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
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
88 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
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
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
CHEMBL51 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
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
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
DB12465 2181 96 None -1862 52 Human 4.7 pKi = 4.7 Binding
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
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
71452650 78496 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL2111848 78496 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL5082151 214788 1 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1ccc(Cl)c2cccnc12 10.1021/acs.jmedchem.1c02031
127036932 137348 0 None -69 22 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 137348 0 None -69 22 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL5074821 214336 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnn(C[C@H](C)NCc2cccc(OCc3ccccn3)c2)c1 10.1021/acs.jmedchem.1c02031
2760172 98809 32 None 1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 c1ccc2cc(N3CCNCC3)ccc2c1 10.1021/jm030030n
CHEMBL278509 98809 32 None 1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 c1ccc2cc(N3CCNCC3)ccc2c1 10.1021/jm030030n
CHEMBL5084249 214905 0 None -251 8 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCN(CC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
73346042 91834 5 None -21379 17 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91834 5 None -21379 17 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL5092728 215384 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CC(C)(C)c1ccc2c(c1)CN(C[C@@H](O)COC1CCOCC1)CC2 10.1021/acs.jmedchem.1c02031
70530 96957 104 None -6 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm030030n
CHEMBL266250 96957 104 None -6 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm030030n
1043 1582 14 None -169 28 Human 7.7 pKi = 7.7 Binding
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
ChEMBL 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 10.1021/jm990550b
149 1582 14 None -169 28 Human 7.7 pKi = 7.7 Binding
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
ChEMBL 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 10.1021/jm990550b
8223 1582 14 None -169 28 Human 7.7 pKi = 7.7 Binding
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
ChEMBL 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 10.1021/jm990550b
CHEMBL442 1582 14 None -169 28 Human 7.7 pKi = 7.7 Binding
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
ChEMBL 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 10.1021/jm990550b
DB00696 1582 14 None -169 28 Human 7.7 pKi = 7.7 Binding
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
ChEMBL 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 10.1021/jm990550b
136152966 95593 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 289 3 2 4 2.9 COc1c(Cl)ccc2c1C(C)NC(NCC(F)F)=N2 10.1016/j.bmcl.2007.10.078
CHEMBL257744 95593 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 289 3 2 4 2.9 COc1c(Cl)ccc2c1C(C)NC(NCC(F)F)=N2 10.1016/j.bmcl.2007.10.078
135458427 171553 0 None -5 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 283 4 2 4 3.0 CC(C)Oc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
CHEMBL446459 171553 0 None -5 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 283 4 2 4 3.0 CC(C)Oc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
44456395 95671 0 None -1 5 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL258073 95671 0 None -1 5 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2 10.1016/j.bmcl.2007.10.080
134138168 147691 0 None -19 10 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147691 0 None -19 10 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
4806 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
24841480 183899 0 None -1096 20 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183899 0 None -1096 20 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
181743 178572 5 None -1122 22 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 178572 5 None -1122 22 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL4576555 214017 5 None -2 19 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
44351180 18084 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126737 18084 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
44351077 116970 0 None 1 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338696 116970 0 None 1 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
118464420 138245 0 None -38 8 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 138245 0 None -38 8 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
10324985 76781 8 None -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76781 8 None -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76781 8 None -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
168293874 192179 0 None -52 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 192179 0 None -52 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5090584 215271 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1cccc2cccnc12 10.1021/acs.jmedchem.1c02031
CHEMBL5071978 214272 0 None -3 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
117209858 184554 1 None -147 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 184554 1 None -147 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
122334 322 23 None -51 8 Human 5.6 pKi = 5.6 Binding
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 )
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
970 322 23 None -51 8 Human 5.6 pKi = 5.6 Binding
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 )
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
CHEMBL27441 322 23 None -51 8 Human 5.6 pKi = 5.6 Binding
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 )
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
136118614 93064 0 None -25 5 Human 5.6 pKi = 5.6 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442276 93064 0 None -25 5 Human 5.6 pKi = 5.6 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
155770281 177747 0 None -2 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A (unknown origin)Binding affinity to 5HT5A (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4642592 177747 0 None -2 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A (unknown origin)Binding affinity to 5HT5A (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
44355141 24646 0 None - 1 Rat 6.6 pKi = 6.6 Binding
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
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL134331 24646 0 None - 1 Rat 6.6 pKi = 6.6 Binding
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
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
127036953 137515 0 None -239 22 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 137515 0 None -239 22 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
44455986 97596 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 175 1 2 3 1.7 CCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL270841 97596 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 175 1 2 3 1.7 CCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL5093342 215564 0 None -28 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 215564 0 None -28 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5090884 215577 0 None -37 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096072 215577 0 None -37 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
136152973 95225 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCCOCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL256048 95225 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCCOCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
107838 97323 112 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030030n
CHEMBL269236 97323 112 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030030n
CHEMBL4576555 214017 5 None -2 19 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
CHEMBL4576555 214017 5 None -2 19 Human 5.6 pKi = 5.6 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HTR5ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HTR5A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL5212743
44351140 19041 0 None 3 3 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128848 19041 0 None 3 3 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
11444050 11754 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
CHEMBL1181620 11754 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
CHEMBL185676 11754 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
9827938 11771 0 None 6 12 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 11771 0 None 6 12 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 11771 0 None 6 12 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
11352884 67158 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL187621 67158 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
135966709 155155 4 None -10 5 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 233 2 2 4 2.3 CNC1=Nc2c(OC(C)C)cccc2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL402179 155155 4 None -10 5 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 233 2 2 4 2.3 CNC1=Nc2c(OC(C)C)cccc2C(C)N1 10.1016/j.bmcl.2007.10.080
5 139 72 None -323 54 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 72 None -323 54 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 72 None -323 54 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 72 None -323 54 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
10893866 20308 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 6 0 5 3.9 Cn1c2c(c3ccccc31)CN(CCCOc1ccc([N+](=O)[O-])cc1)CC2 10.1021/jm030080s
CHEMBL130585 20308 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 6 0 5 3.9 Cn1c2c(c3ccccc31)CN(CCCOc1ccc([N+](=O)[O-])cc1)CC2 10.1021/jm030080s
44351099 18055 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 304 4 0 2 4.2 Cn1c2c(c3ccccc31)CN(CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL126574 18055 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 304 4 0 2 4.2 Cn1c2c(c3ccccc31)CN(CCCc1ccccc1)CC2 10.1021/jm030080s
1220 187 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 187 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 187 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 187 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
1220 187 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 187 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 187 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 187 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
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
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
44397593 11769 0 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181677 11769 0 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188440 11769 0 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
44397513 12266 0 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1184719 12266 0 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL365422 12266 0 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44455943 169002 5 None 2 5 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 243 1 2 3 3.0 CCC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL439240 169002 5 None 2 5 Human 7.6 pKi = 7.6 Binding
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
ChEMBL 243 1 2 3 3.0 CCC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
10472143 119277 0 None -60 16 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm020153s
CHEMBL343755 119277 0 None -60 16 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm020153s
44351193 116852 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338095 116852 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL5092524 215375 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1ccc(F)c2cccnc12 10.1021/acs.jmedchem.1c02031
44456284 12845 1 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188595 12845 1 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536789 12845 1 None - 1 Human 6.6 pKi = 6.6 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
136152969 155325 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 286 1 2 4 1.9 CC1NC(NC2CCCCN(C)C2=O)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL403103 155325 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 286 1 2 4 1.9 CC1NC(NC2CCCCN(C)C2=O)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
135458428 155534 0 None 1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 255 3 2 4 2.2 COc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
CHEMBL404248 155534 0 None 1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 255 3 2 4 2.2 COc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
12683497 97520 0 None - 1 Human 5.6 pKi = 5.6 Binding
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
ChEMBL 175 0 1 3 1.3 CN(C)C1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL270409 97520 0 None - 1 Human 5.6 pKi = 5.6 Binding
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
ChEMBL 175 0 1 3 1.3 CN(C)C1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
4407909 192866 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192866 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192866 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
44351077 116970 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338696 116970 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
44374431 54952 0 None -1 4 Human 6.5 pKi = 6.5 Binding
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 )
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL161507 54952 0 None -1 4 Human 6.5 pKi = 6.5 Binding
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 )
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
90469115 185842 4 None -954 17 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 185842 4 None -954 17 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL5093652 215437 2 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None N#CC1(c2ccccc2)CCC(NCCc2nnc3ccccn23)CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5094493 215499 0 None -144 7 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCN(CCC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44351171 116849 0 None 2 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL338081 116849 0 None 2 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOCc1ccccc1)CC2 10.1021/jm030080s
44275750 93213 39 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 228 1 2 3 2.0 Oc1ccc2cccc(N3CCNCC3)c2c1 10.1021/jm030030n
CHEMBL24462 93213 39 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 228 1 2 3 2.0 Oc1ccc2cccc(N3CCNCC3)c2c1 10.1021/jm030030n
CHEMBL5075486 214376 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CCC[C@@H](CNCc2ccc(Cl)c3cccnc23)C1 10.1021/acs.jmedchem.1c02031
50923584 125158 0 None - 1 Human 8.5 pKi = 8.5 Binding
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.
ChEMBL 326 2 2 2 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3F)c2c1 nan
CHEMBL3644533 125158 0 None - 1 Human 8.5 pKi = 8.5 Binding
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.
ChEMBL 326 2 2 2 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3F)c2c1 nan
50923585 125159 0 None - 1 Human 8.5 pKi = 8.5 Binding
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.
ChEMBL 342 2 2 2 3.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3Cl)c2c1 nan
CHEMBL3644534 125159 0 None - 1 Human 8.5 pKi = 8.5 Binding
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.
ChEMBL 342 2 2 2 3.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3Cl)c2c1 nan
91819719 126788 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2cccc(-c3cc(F)c(F)cc3F)c2C1 nan
CHEMBL3654196 126788 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2cccc(-c3cc(F)c(F)cc3F)c2C1 nan
60150903 126803 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3cc(F)c(F)cc3F)c2C1 nan
CHEMBL3654211 126803 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3cc(F)c(F)cc3F)c2C1 nan
50923581 125151 0 None - 1 Human 8.4 pKi = 8.4 Binding
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.
ChEMBL 372 2 2 2 3.4 Cc1nc2ccc(C(=O)N=C(N)N)cc2c(-c2c(F)cc(F)cc2F)c1C nan
CHEMBL3644526 125151 0 None - 1 Human 8.4 pKi = 8.4 Binding
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.
ChEMBL 372 2 2 2 3.4 Cc1nc2ccc(C(=O)N=C(N)N)cc2c(-c2c(F)cc(F)cc2F)c1C nan
60150900 126795 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 345 1 2 2 2.1 Cc1ccc(-c2ncc(F)cc2F)c2c1CCN(C(=O)N=C(N)N)C2 nan
CHEMBL3654203 126795 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 345 1 2 2 2.1 Cc1ccc(-c2ncc(F)cc2F)c2c1CCN(C(=O)N=C(N)N)C2 nan
24936155 94622 0 None -501 7 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
CHEMBL252258 94622 0 None -501 7 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
44374648 119972 0 None -18 4 Human 5.5 pKi = 5.5 Binding
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 )
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL349843 119972 0 None -18 4 Human 5.5 pKi = 5.5 Binding
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 )
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
4106 2502 22 None -14 34 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
5358812 2502 22 None -14 34 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
89 2502 22 None -14 34 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
CHEMBL93240 2502 22 None -14 34 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
11272242 11762 0 None - 1 Human 7.5 pKi = 7.5 Binding
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
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1181641 11762 0 None - 1 Human 7.5 pKi = 7.5 Binding
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
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL186849 11762 0 None - 1 Human 7.5 pKi = 7.5 Binding
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
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
11364267 67539 0 None - 1 Human 7.5 pKi = 7.5 Binding
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
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL189689 67539 0 None - 1 Human 7.5 pKi = 7.5 Binding
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
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44355165 116470 0 None - 1 Rat 6.5 pKi = 6.5 Binding
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
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL336124 116470 0 None - 1 Rat 6.5 pKi = 6.5 Binding
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
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
10287730 3536 40 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
77 3536 40 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
CHEMBL425190 3536 40 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
44397511 11768 0 None - 1 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1181669 11768 0 None - 1 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL188050 11768 0 None - 1 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
107838 97323 112 None -1 2 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030080s
CHEMBL269236 97323 112 None -1 2 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030080s
127036186 137414 0 None -102 19 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 137414 0 None -102 19 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
216239 23795 118 None -6 7 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1200485 23795 118 None -6 7 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1336 23795 118 None -6 7 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
136116062 97680 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL271253 97680 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.078
71452650 78496 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL2111848 78496 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
50878551 90745 61 None -85 18 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 90745 61 None -85 18 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
136118651 76324 0 None -9 4 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058706 76324 0 None -9 4 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
10892139 165587 0 None -1 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3c([nH]c4ccccc34)C2)cc1 10.1021/jm030080s
CHEMBL424258 165587 0 None -1 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3c([nH]c4ccccc34)C2)cc1 10.1021/jm030080s
122483275 138110 0 None -15 8 Human 6.5 pKi = 6.5 Binding
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
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764133 138110 0 None -15 8 Human 6.5 pKi = 6.5 Binding
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
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765875 138110 0 None -15 8 Human 6.5 pKi = 6.5 Binding
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
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
136118648 76321 0 None -67 5 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058703 76321 0 None -67 5 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
44351361 17968 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 5 1 4 4.3 Cn1c2c(c3ccccc31)CN(CCC/C(=N/O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126138 17968 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 5 1 4 4.3 Cn1c2c(c3ccccc31)CN(CCC/C(=N/O)c1ccc(F)cc1)CC2 10.1021/jm030080s
9862256 207120 0 None -2238 9 Rat 5.5 pKi = 5.5 Binding
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
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL92139 207120 0 None -2238 9 Rat 5.5 pKi = 5.5 Binding
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
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
10035245 29694 0 None - 1 Human 6.5 pKi = 6.5 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL13864 29694 0 None - 1 Human 6.5 pKi = 6.5 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL538340 29694 0 None - 1 Human 6.5 pKi = 6.5 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
10926167 118093 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 6 0 4 4.0 COc1ccc(OCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL340646 118093 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 6 0 4 4.0 COc1ccc(OCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
44351100 171471 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL446356 171471 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL5094680 215510 0 None -23 8 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11726973 18101 0 None 1 3 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
CHEMBL126823 18101 0 None 1 3 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
136152970 95356 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 309 2 2 5 2.8 CC1NC(NCC2COc3ccccc3O2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL256693 95356 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 309 2 2 5 2.8 CC1NC(NCC2COc3ccccc3O2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44355425 23588 0 None - 1 Rat 6.4 pKi = 6.4 Binding
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
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL133433 23588 0 None - 1 Rat 6.4 pKi = 6.4 Binding
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
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
44455985 13152 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL1190709 13152 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL541396 13152 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44455985 13152 1 None - 1 Human 7.4 pKi = 7.4 Binding
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
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL1190709 13152 1 None - 1 Human 7.4 pKi = 7.4 Binding
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
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL541396 13152 1 None - 1 Human 7.4 pKi = 7.4 Binding
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
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL5074190 214314 0 None -151 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
44355426 24179 0 None - 1 Rat 6.4 pKi = 6.4 Binding
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
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL133935 24179 0 None - 1 Rat 6.4 pKi = 6.4 Binding
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
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
752521 198737 8 None -19 9 Human 6.4 pKi = 6.4 Binding
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
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 198737 8 None -19 9 Human 6.4 pKi = 6.4 Binding
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
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
136152978 95526 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 207 2 2 3 1.9 CC1NC(NCCF)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL257450 95526 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 207 2 2 3 1.9 CC1NC(NCCF)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44397435 11763 0 None - 1 Human 6.4 pKi = 6.4 Binding
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
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181643 11763 0 None - 1 Human 6.4 pKi = 6.4 Binding
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
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL187029 11763 0 None - 1 Human 6.4 pKi = 6.4 Binding
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
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL5089996 215235 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN1CC[C@H](CNCc2ccc(Cl)c3cccnc23)CC1=O 10.1021/acs.jmedchem.1c02031
50923444 125154 0 None - 1 Human 8.4 pKi = 8.4 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccc(F)cc3Cl)c2c1 nan
CHEMBL3644529 125154 0 None - 1 Human 8.4 pKi = 8.4 Binding
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.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccc(F)cc3Cl)c2c1 nan
91819724 126805 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 331 1 2 2 1.8 NC(N)=NC(=O)N1CCc2cccc(-c3ncc(F)cc3F)c2C1 nan
CHEMBL3654213 126805 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 331 1 2 2 1.8 NC(N)=NC(=O)N1CCc2cccc(-c3ncc(F)cc3F)c2C1 nan
91819718 126787 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3F)c2C1 nan
CHEMBL3654195 126787 0 None - 1 Human 8.4 pKi = 8.4 Binding
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).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3F)c2C1 nan
50923722 125164 0 None - 1 Human 8.3 pKi = 8.3 Binding
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.
ChEMBL 376 3 2 2 3.5 NC(N)=NC(=O)c1ccc2c(C(F)F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644539 125164 0 None - 1 Human 8.3 pKi = 8.3 Binding
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.
ChEMBL 376 3 2 2 3.5 NC(N)=NC(=O)c1ccc2c(C(F)F)cnc(-c3c(F)cccc3F)c2c1 nan
50923719 125161 0 None - 1 Human 8.3 pKi = 8.3 Binding
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.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3Cl)c2c1 nan
CHEMBL3644536 125161 0 None - 1 Human 8.3 pKi = 8.3 Binding
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.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3Cl)c2c1 nan
16093485 155063 0 None -1 5 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 239 1 2 4 2.3 COc1cc(Cl)c(C)c2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL401745 155063 0 None -1 5 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 239 1 2 4 2.3 COc1cc(Cl)c(C)c2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
13972211 138937 1 None 28 2 Rat 8.3 pKi = 8.3 Binding
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
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL37844 138937 1 None 28 2 Rat 8.3 pKi = 8.3 Binding
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
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
1342 35 49 None -16 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
3 35 49 None -16 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
CHEMBL277120 35 49 None -16 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
1043 1582 14 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm030030n
149 1582 14 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm030030n
8223 1582 14 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm030030n
CHEMBL442 1582 14 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm030030n
DB00696 1582 14 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 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 10.1021/jm030030n
1342 35 49 None -16 19 Mouse 7.4 pKi = 7.4 Binding
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
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
3 35 49 None -16 19 Mouse 7.4 pKi = 7.4 Binding
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
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
CHEMBL277120 35 49 None -16 19 Mouse 7.4 pKi = 7.4 Binding
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
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
11808247 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
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
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
CHEMBL126667 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
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
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
CHEMBL3819366 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
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
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
9927441 207394 0 None -1174 9 Rat 5.4 pKi = 5.4 Binding
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
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
CHEMBL93868 207394 0 None -1174 9 Rat 5.4 pKi = 5.4 Binding
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
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
44455962 169346 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL441896 169346 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
145980271 166492 0 None -8 16 Human 5.4 pKi = 5.4 Binding
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
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 166492 0 None -8 16 Human 5.4 pKi = 5.4 Binding
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
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
92042876 151336 0 None -79 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 151336 0 None -79 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
127026052 137553 0 None -257 19 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137553 0 None -257 19 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
9904281 47749 28 None 4 7 Human 7.4 pKi = 7.4 Binding
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
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1548 47749 28 None 4 7 Human 7.4 pKi = 7.4 Binding
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
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
44355180 165334 0 None - 1 Rat 6.4 pKi = 6.4 Binding
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
ChEMBL 233 6 0 2 3.1 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL423527 165334 0 None - 1 Rat 6.4 pKi = 6.4 Binding
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
ChEMBL 233 6 0 2 3.1 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
44351101 16949 0 None 1 2 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 346 7 0 2 5.3 Cn1c2c(c3ccccc31)CN(CCCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125361 16949 0 None 1 2 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 346 7 0 2 5.3 Cn1c2c(c3ccccc31)CN(CCCCCCc1ccccc1)CC2 10.1021/jm030080s
9796627 96653 0 None -154 7 Rat 5.4 pKi = 5.4 Binding
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
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL263700 96653 0 None -154 7 Rat 5.4 pKi = 5.4 Binding
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
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
3649661 138219 7 None -63 8 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 138219 7 None -63 8 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
12 1553 17 None -208 7 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
6918513 1553 17 None -208 7 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
CHEMBL267615 1553 17 None -208 7 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
44456246 12832 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188440 12832 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536335 12832 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
44456400 12834 0 None -2 10 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12834 0 None -2 10 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12834 0 None -2 10 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12834 0 None -2 10 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
136118660 76256 0 None -3 3 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058428 76256 0 None -3 3 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
145963830 164123 0 None -46 7 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 164123 0 None -46 7 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
136152976 167471 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 243 1 2 3 2.5 CC1NC(NCC(F)(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL429925 167471 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 243 1 2 3 2.5 CC1NC(NCC(F)(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
145986752 167276 0 None -12 17 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 167276 0 None -12 17 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
122483281 138108 0 None 6 8 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763779 138108 0 None 6 8 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765873 138108 0 None 6 8 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
16006492 97469 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270177 97469 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
44397364 123160 0 None - 1 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL361256 123160 0 None - 1 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
16006492 97469 7 None 3 6 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 97469 7 None 3 6 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
16006492 97469 7 None 3 6 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 97469 7 None 3 6 Human 8.3 pKi = 8.3 Binding
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
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
50923582 125156 2 None - 1 Human 8.3 pKi = 8.3 Binding
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.
ChEMBL 345 2 2 3 2.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3F)c2c1 nan
CHEMBL3644531 125156 2 None - 1 Human 8.3 pKi = 8.3 Binding
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.
ChEMBL 345 2 2 3 2.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3F)c2c1 nan
135458410 167189 0 None 3 6 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL429136 167189 0 None 3 6 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
11191906 11767 0 None 6 12 Human 7.3 pKi = 7.3 Binding
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
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 11767 0 None 6 12 Human 7.3 pKi = 7.3 Binding
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
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 11767 0 None 6 12 Human 7.3 pKi = 7.3 Binding
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
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
4713248 207907 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL96729 207907 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
4713248 207907 3 None -5 3 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL96729 207907 3 None -5 3 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
44397427 11756 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
CHEMBL1181625 11756 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
CHEMBL185996 11756 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
44456400 12834 0 None -2 10 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12834 0 None -2 10 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12834 0 None -2 10 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12834 0 None -2 10 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
136152972 95224 0 None -2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL256047 95224 0 None -2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
44355128 118482 0 None - 1 Rat 6.3 pKi = 6.3 Binding
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
ChEMBL 219 5 1 2 2.8 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL341373 118482 0 None - 1 Rat 6.3 pKi = 6.3 Binding
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
ChEMBL 219 5 1 2 2.8 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
136118658 76254 0 None -5 6 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058426 76254 0 None -5 6 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
379995 116851 2 None - 1 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 1 2 4.3 O=C(CCCN1CCc2[nH]c3ccccc3c2C1)c1ccc(F)cc1 10.1021/jm030080s
CHEMBL338091 116851 2 None - 1 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 1 2 4.3 O=C(CCCN1CCc2[nH]c3ccccc3c2C1)c1ccc(F)cc1 10.1021/jm030080s
CHEMBL4748908 214035 1 None -64 12 Human 5.3 pKi = 5.3 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
6918515 2612 38 None -158 7 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
71 2612 38 None -158 7 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
CHEMBL7318 2612 38 None -158 7 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
72550645 114089 0 None -72 8 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326993 114089 0 None -72 8 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
18677411 207244 11 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030080s
CHEMBL92879 207244 11 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030080s
18677411 207244 11 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030030n
CHEMBL92879 207244 11 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030030n
135474338 189271 0 None -28 3 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL511879 189271 0 None -28 3 Human 5.3 pKi = 5.3 Binding
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
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
10382508 207865 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
CHEMBL96504 207865 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
10382508 207865 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL96504 207865 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
11045379 19371 0 None -4 2 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 1 2 4.2 O=C(CCCN1CCc2c([nH]c3ccccc23)C1)c1ccccc1 10.1021/jm030080s
CHEMBL129163 19371 0 None -4 2 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 1 2 4.2 O=C(CCCN1CCc2c([nH]c3ccccc23)C1)c1ccccc1 10.1021/jm030080s
44456443 12991 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1189631 12991 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL539103 12991 0 None - 1 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
16573 177619 34 None -28 6 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 177619 34 None -28 6 Human 6.3 pKi = 6.3 Binding
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
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL5085238 214958 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CC[C@@H](CNCc2cccc3cccnc23)C1 10.1021/acs.jmedchem.1c02031
44355424 22026 0 None - 1 Rat 7.2 pKi = 7.2 Binding
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
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL132123 22026 0 None - 1 Rat 7.2 pKi = 7.2 Binding
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
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
71462776 82963 0 None -4786 6 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181169 82963 0 None -4786 6 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
44351180 18084 0 None -2 3 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126737 18084 0 None -2 3 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
118464425 138309 0 None -15 9 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 138309 0 None -15 9 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
50923721 125163 0 None - 1 Human 8.2 pKi = 8.2 Binding
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.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ncc(F)cc3Cl)c2c1 nan
CHEMBL3644538 125163 0 None - 1 Human 8.2 pKi = 8.2 Binding
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.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ncc(F)cc3Cl)c2c1 nan
135458394 97691 5 None 2 5 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 243 0 2 3 2.9 CNC1=Nc2ccc(Cl)c(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL271298 97691 5 None 2 5 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 243 0 2 3 2.9 CNC1=Nc2ccc(Cl)c(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
16006606 157661 3 None 1 5 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 191 1 2 4 1.3 COc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL408152 157661 3 None 1 5 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 191 1 2 4 1.3 COc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
135458393 155596 4 None 2 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 155596 4 None 2 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
11168182 3534 25 None 50 13 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 3534 25 None 50 13 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 3534 25 None 50 13 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
16006605 97992 3 None -2 5 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL272781 97992 3 None -2 5 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.080
91819721 126794 0 None - 1 Human 8.2 pKi = 8.2 Binding
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).
ChEMBL 382 1 2 1 3.5 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(Cl)c2C(F)C1 nan
CHEMBL3654202 126794 0 None - 1 Human 8.2 pKi = 8.2 Binding
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).
ChEMBL 382 1 2 1 3.5 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(Cl)c2C(F)C1 nan
CHEMBL5093969 215461 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNCC[C@@H]2CCOC2)c2ncccc12 10.1021/acs.jmedchem.1c02031
CHEMBL5094012 215463 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=C1C[C@H](CNCc2ccc(Cl)c3cccnc23)CN1C1CC1 10.1021/acs.jmedchem.1c02031
136152964 194939 0 None -2 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL541993 194939 0 None -2 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
60150899 126793 0 None - 1 Human 8.2 pKi = 8.2 Binding
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).
ChEMBL 349 1 2 2 1.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(F)cc3F)c2C1 nan
CHEMBL3654201 126793 0 None - 1 Human 8.2 pKi = 8.2 Binding
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).
ChEMBL 349 1 2 2 1.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(F)cc3F)c2C1 nan
22980542 18031 0 None -3 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
CHEMBL126438 18031 0 None -3 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
73353884 92322 0 None -5 8 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2429890 92322 0 None -5 8 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL4748908 214035 1 None -64 12 Human 5.2 pKi = 5.2 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
11726973 18101 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
CHEMBL126823 18101 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
146025727 171685 0 None -229 27 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171685 0 None -229 27 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44327952 208044 0 None 1 5 Mouse 7.2 pKi = 7.2 Binding
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
ChEMBL 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 10.1021/jm030030n
CHEMBL97518 208044 0 None 1 5 Mouse 7.2 pKi = 7.2 Binding
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
ChEMBL 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 10.1021/jm030030n
3233 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
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.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
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.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
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.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
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.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
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.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
22857296 29150 0 None -123 4 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL13816 29150 0 None -123 4 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
44397433 12265 0 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1184710 12265 0 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL365084 12265 0 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
2470 3653 50 None -77624 59 Human 4.2 pKi = 4.2 Binding
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
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 3653 50 None -77624 59 Human 4.2 pKi = 4.2 Binding
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
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 3653 50 None -77624 59 Human 4.2 pKi = 4.2 Binding
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
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 3653 50 None -77624 59 Human 4.2 pKi = 4.2 Binding
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
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 3653 50 None -77624 59 Human 4.2 pKi = 4.2 Binding
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
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
44397429 11758 0 None - 1 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181634 11758 0 None - 1 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL186450 11758 0 None - 1 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
44456253 12837 0 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188517 12837 0 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536562 12837 0 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
3233 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
3247 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
6604889 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
CHEMBL282199 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
DB13988 3512 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
44350898 17980 0 None -1 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1cccc3ccccc13)CC2 10.1021/jm030080s
CHEMBL126188 17980 0 None -1 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1cccc3ccccc13)CC2 10.1021/jm030080s
44350897 118073 0 None -2 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1ccc3ccccc3c1)CC2 10.1021/jm030080s
CHEMBL340511 118073 0 None -2 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1ccc3ccccc3c1)CC2 10.1021/jm030080s
12628906 94596 28 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL25212 94596 28 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL557381 94596 28 None - 1 Human 6.2 pKi = 6.2 Binding
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
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
135508617 136016503 10630 0 None -12 4 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL1170237 10630 0 None -12 4 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
145977799 163643 0 None -9 6 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204036 163643 0 None -9 6 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
44582675 189701 0 None -114 15 Human 5.2 pKi = 5.2 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189701 0 None -114 15 Human 5.2 pKi = 5.2 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
117209965 185247 1 None -29 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 185247 1 None -29 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
4376990 193009 5 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 193009 5 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 193009 5 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
136118661 76257 0 None -7 5 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058429 76257 0 None -7 5 Human 5.2 pKi = 5.2 Binding
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
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
50923583 125157 0 None - 1 Human 8.2 pKi = 8.2 Binding
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.
ChEMBL 356 3 2 3 2.6 COc1cccc(F)c1-c1ncc(F)c2ccc(C(=O)N=C(N)N)cc12 nan
CHEMBL3644532 125157 0 None - 1 Human 8.2 pKi = 8.2 Binding
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.
ChEMBL 356 3 2 3 2.6 COc1cccc(F)c1-c1ncc(F)c2ccc(C(=O)N=C(N)N)cc12 nan
CHEMBL5094234 215573 0 None -331 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 215573 0 None -331 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5091270 215301 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CCC[C@@H](CNCc2cccc3cccnc23)C1 10.1021/acs.jmedchem.1c02031
44355201 115218 0 None - 1 Rat 6.1 pKi = 6.1 Binding
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
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL334553 115218 0 None - 1 Rat 6.1 pKi = 6.1 Binding
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
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
130442572 171908 0 None -158 24 Human 5.1 pKi = 5.1 Binding
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
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171908 0 None -158 24 Human 5.1 pKi = 5.1 Binding
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
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
21509921 104458 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104458 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
44351047 18082 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 5 1 2 4.1 Fc1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
CHEMBL126724 18082 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 5 1 2 4.1 Fc1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
44351139 18844 0 None 1 3 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128099 18844 0 None 1 3 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
21509921 104458 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104458 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
73355415 92533 0 None -38 13 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 92533 0 None -38 13 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
44355164 23041 0 None - 1 Rat 6.1 pKi = 6.1 Binding
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
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL133020 23041 0 None - 1 Rat 6.1 pKi = 6.1 Binding
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
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
2737389 187586 28 None -53 5 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
CHEMBL494675 187586 28 None -53 5 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
71459604 83793 0 None -13 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT5A receptorBinding affinity to 5-HT5A receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83793 0 None -13 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT5A receptorBinding affinity to 5-HT5A receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
136118620 76252 0 None -24 5 Human 5.1 pKi = 5.1 Binding
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
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2058419 76252 0 None -24 5 Human 5.1 pKi = 5.1 Binding
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
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
44397669 11787 0 None - 1 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181776 11787 0 None - 1 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL191583 11787 0 None - 1 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
44397362 12259 0 None - 1 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1184673 12259 0 None - 1 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL363678 12259 0 None - 1 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44455983 97595 1 None - 1 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 189 2 2 3 2.1 CCCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL270840 97595 1 None - 1 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 189 2 2 3 2.1 CCCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
44456400 12834 0 None -2 10 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188501 12834 0 None -2 10 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL2436555 12834 0 None -2 10 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536539 12834 0 None -2 10 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
5 139 72 None -323 54 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 72 None -323 54 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 72 None -323 54 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 72 None -323 54 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
145967795 164823 0 None -5 3 Human 5.1 pKi = 5.1 Binding
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
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4218679 164823 0 None -5 3 Human 5.1 pKi = 5.1 Binding
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
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
44455973 97468 7 None 1 4 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 209 1 2 3 2.3 CCC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270176 97468 7 None 1 4 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 209 1 2 3 2.3 CCC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
160510 101127 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL1506260 101127 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL295234 101127 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
160510 101127 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
CHEMBL1506260 101127 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
CHEMBL295234 101127 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
49783209 17609 0 None -4265 26 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17609 0 None -4265 26 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
155551348 173957 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5HT5A (unknown origin)Inhibition of 5HT5A (unknown origin)
ChEMBL 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 10.1021/acs.jmedchem.8b01662
CHEMBL4541409 173957 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5HT5A (unknown origin)Inhibition of 5HT5A (unknown origin)
ChEMBL 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 10.1021/acs.jmedchem.8b01662
136152977 97885 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 225 2 2 3 2.2 CC1NC(NCC(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL272355 97885 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 225 2 2 3 2.2 CC1NC(NCC(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
1355 2011 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
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
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
142 2011 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
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
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
CHEMBL478 2011 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
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
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
DB12110 2011 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
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
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
1355 2011 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
142 2011 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
CHEMBL478 2011 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
DB12110 2011 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
44351103 20309 0 None -9 2 Mouse 6.1 pKi = 6.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 396 7 0 3 5.5 c1ccc(Cn2c3c(c4ccccc42)CN(CCCOc2ccccc2)CC3)cc1 10.1021/jm030080s
CHEMBL130586 20309 0 None -9 2 Mouse 6.1 pKi = 6.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 396 7 0 3 5.5 c1ccc(Cn2c3c(c4ccccc42)CN(CCCOc2ccccc2)CC3)cc1 10.1021/jm030080s
132060720 162489 0 None -2 9 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4167315 162489 0 None -2 9 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
44456398 13950 0 None - 1 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL1196644 13950 0 None - 1 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL557746 13950 0 None - 1 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
135464118 93060 0 None -2 5 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442272 93060 0 None -2 5 Human 7.1 pKi = 7.1 Binding
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
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
44456244 97985 1 None - 1 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2c(Cl)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL272752 97985 1 None - 1 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2c(Cl)cccc2CN1 10.1016/j.bmcl.2007.10.080
53325242 57070 0 None -4 17 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 57070 0 None -4 17 Human 6.1 pKi = 6.1 Binding
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
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
1621 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
10405482 19142 0 None 11 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 348 6 0 3 4.6 COc1ccc(CCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL128945 19142 0 None 11 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 348 6 0 3 4.6 COc1ccc(CCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL5091373 215567 0 None -436 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 215567 0 None -436 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44456286 12846 0 None - 1 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188596 12846 0 None - 1 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536790 12846 0 None - 1 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
136118659 76255 0 None -5 5 Human 5.0 pKi = 5.0 Binding
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
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058427 76255 0 None -5 5 Human 5.0 pKi = 5.0 Binding
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
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
10881882 18192 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 4 0 3 3.8 Cn1c2c(c3ccccc31)CN(CCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126994 18192 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 4 0 3 3.8 Cn1c2c(c3ccccc31)CN(CCOc1ccc(F)cc1)CC2 10.1021/jm030080s
122483292 138111 0 None -33 7 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764335 138111 0 None -33 7 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765876 138111 0 None -33 7 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
44351499 118553 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(CCCCc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL341506 118553 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(CCCCc1ccc(F)cc1)CC2 10.1021/jm030080s
130442480 175270 0 None -117 24 Human 5.0 pKi = 5.0 Binding
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
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 175270 0 None -117 24 Human 5.0 pKi = 5.0 Binding
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
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
136152967 155565 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 261 2 2 5 1.3 CC1NC(NCC2COCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL404365 155565 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 261 2 2 5 1.3 CC1NC(NCC2COCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
135433933 177038 1 None -8 4 Human 5.0 pKi = 5.0 Binding
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
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL463249 177038 1 None -8 4 Human 5.0 pKi = 5.0 Binding
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
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
44456207 13646 7 None - 1 Human 7.0 pKi = 7.0 Binding
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
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1194499 13646 7 None - 1 Human 7.0 pKi = 7.0 Binding
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
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL552782 13646 7 None - 1 Human 7.0 pKi = 7.0 Binding
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
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL5077293 214491 0 None -346 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
44351184 18861 0 None 1 3 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
CHEMBL128185 18861 0 None 1 3 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
23642275 482 31 None -60 3 Human 7.0 pKi = 7.0 Binding
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
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
8433 482 31 None -60 3 Human 7.0 pKi = 7.0 Binding
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
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
CHEMBL2164327 482 31 None -60 3 Human 7.0 pKi = 7.0 Binding
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
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
13702393 155025 2 None 6 6 Human 7.0 pKi = 7 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL401541 155025 2 None 6 6 Human 7.0 pKi = 7 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL556983 155025 2 None 6 6 Human 7.0 pKi = 7 Binding
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
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
118464427 138334 0 None -36 7 Human 6.0 pKi = 6 Binding
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
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 138334 0 None -36 7 Human 6.0 pKi = 6 Binding
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
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
44355200 26338 0 None - 1 Rat 6.0 pKi = 6 Binding
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
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL135894 26338 0 None - 1 Rat 6.0 pKi = 6 Binding
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
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
2543 3707 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
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
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
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
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
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
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
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
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
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
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
4106 2502 22 3H-5CT -14 34 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-5CT -14 34 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-5CT -14 34 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-5CT -14 34 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 22 125I-LSD -269 34 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 125I-LSD -269 34 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 125I-LSD -269 34 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 125I-LSD -269 34 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1220 187 55 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
10257 738 31 125I-LSD -741 19 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 738 31 125I-LSD -741 19 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 738 31 125I-LSD -741 19 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 738 31 125I-LSD -741 19 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
135398737 958 93 3H-5CT -173 89 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-5CT -173 89 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-5CT -173 89 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-5CT -173 89 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-5CT -173 89 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11957541 1459 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1459 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1459 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1459 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1459 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
681 1465 72 125I-LSD -199 39 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 125I-LSD -199 39 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 125I-LSD -199 39 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 125I-LSD -199 39 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 125I-LSD -199 39 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1357 2485 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2485 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2485 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2485 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2485 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2485 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
206 2493 16 125I-LSD -676 25 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 16 125I-LSD -676 25 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 16 125I-LSD -676 25 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
133 2496 52 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
134 2514 24 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
484 2858 51 125I-LSD -7 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2858 51 125I-LSD -7 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2858 51 125I-LSD -7 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
1243 3618 34 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
944 3618 34 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
CHEMBL324017 3618 34 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
102 4127 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 4127 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
108182 4131 22 125I-LSD -3 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 4131 22 125I-LSD -3 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 4131 22 125I-LSD -3 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
None 216379 0 UNDEFINED -1122 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
179 400 115 3H-LSD -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 115 3H-LSD -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 115 3H-LSD -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 115 3H-LSD -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 115 3H-LSD -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
681 1465 72 125I-LSD -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 125I-LSD -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 125I-LSD -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 125I-LSD -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 125I-LSD -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1524 2181 96 125I-LSD -7585 52 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 125I-LSD -7585 52 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 125I-LSD -7585 52 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 125I-LSD -7585 52 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 125I-LSD -7585 52 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 125I-LSD -7585 52 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
134 2514 24 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
484 2858 51 125I-LSD -24 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
484 2858 51 3H-KETANSERIN -7 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2858 51 125I-LSD -24 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2858 51 3H-KETANSERIN -7 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2858 51 125I-LSD -24 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2858 51 3H-KETANSERIN -7 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
15897 2862 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
119570 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
243 3202 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3202 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3202 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3202 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3202 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
173 3262 95 3H-LSD -114 23 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 95 3H-LSD -114 23 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 95 3H-LSD -114 23 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
2402 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
128563 3464 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3464 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3464 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3464 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
2543 3707 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3707 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
185 4006 60 3H-LSD -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4006 60 3H-LSD -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4006 60 3H-LSD -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4006 60 3H-LSD -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
102 4127 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2662 11384 131 3H-Alpha-Me-histamine -41 30 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11384 131 3H-Alpha-Me-histamine -41 30 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
5090 15561 106 3H-Alpha-Me-histamine -1348 30 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15561 106 3H-Alpha-Me-histamine -1348 30 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
10297 27112 30 3H-LSD -38 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27112 30 3H-LSD -38 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 46800 99 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46800 99 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46800 99 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
21830793 91835 10 3H-8-OH-DPAT -66069 45 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91835 10 3H-8-OH-DPAT -66069 45 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
2244 94233 100 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 94233 100 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
3663 99967 83 3H-LSD -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99967 83 3H-LSD -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
446220 133521 14 3H-LSD -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 133521 14 3H-LSD -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 167791 24 3H-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167791 24 3H-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
5280343 188275 124 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 188275 124 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 188275 124 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
54676228 193615 112 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 193615 112 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 196535 92 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 196535 92 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 200551 115 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 200551 115 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 200551 115 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 202274 22 3H-LSD -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 22 3H-LSD -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 22 3H-LSD -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 203025 92 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203025 92 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
1973 203483 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 203483 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 203483 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
202478 204687 20 3H-LSD -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 204687 20 3H-LSD -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
3821 204718 17 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
CHEMBL742 204718 17 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
5311189 204841 11 3H-LSD -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 204841 11 3H-LSD -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 205341 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 205341 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 205341 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
119607 206203 113 3H-Alpha-Me-histamine -97 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 206203 113 3H-Alpha-Me-histamine -97 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
3337 206367 27 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 27 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 27 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 27 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 27 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
165193 215945 0 125I-LSD -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 0 125I-LSD -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 0 125I-LSD -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
None 215993 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
25137849 216179 0 3H-LSD -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216179 0 3H-LSD -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 216239 0 3H-LSD -95499 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 216311 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 216312 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216313 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216314 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216315 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 216316 0 3H-LSD -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216317 0 3H-LSD -1 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216318 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 216325 0 3H-LSD -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 216326 0 3H-LSD -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 216327 0 3H-LSD -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 216328 0 3H-LSD -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 216329 0 3H-LSD -3 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 216330 0 3H-LSD -281 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 216331 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
135269 216389 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 216390 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 216391 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 216392 0 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 216393 0 3H-Alpha-Me-histamine -1412 26 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 216394 0 3H-Alpha-Me-histamine -1 29 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 216395 0 3H-Alpha-Me-histamine -7 28 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
5 139 72 3H-LSD -891 54 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-LSD -891 54 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-LSD -891 54 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-LSD -891 54 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2726 919 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1809 134 32 UNDEFINED -257 36 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 134 32 125I-LSD -363 36 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 UNDEFINED -257 36 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 125I-LSD -363 36 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 UNDEFINED -257 36 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 125I-LSD -363 36 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
135398745 2914 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
242 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
4106 2502 22 UNDEFINED -269 34 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 UNDEFINED -269 34 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 UNDEFINED -269 34 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 UNDEFINED -269 34 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1220 187 55 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
5 139 72 3H-5CT -323 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5CT -323 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5CT -323 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5CT -323 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 72 125I-LSD -999 54 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 125I-LSD -999 54 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 125I-LSD -999 54 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 125I-LSD -999 54 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
103 4153 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
7153 98020 77 3H-LSD -70 34 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 77 3H-LSD -70 34 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
135398745 2914 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11954224 215953 0 3H-LSD -147 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1212 1662 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
4106 2502 22 125I-LSD -128 34 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 125I-LSD -128 34 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 125I-LSD -128 34 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 125I-LSD -128 34 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
11954224 215953 0 125I-LSD -131 58 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1809 134 32 125I-LSD -257 36 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 125I-LSD -257 36 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 125I-LSD -257 36 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4452 2762 19 3H-LSD -52480 19 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2762 19 3H-LSD -52480 19 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2762 19 3H-LSD -52480 19 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
1220 187 55 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
None 216135 0 3H-LSD -1819 24 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
134 2514 24 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2389 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1809 134 32 3H-5CT -229 36 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5CT -229 36 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5CT -229 36 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
6971132 216009 0 3H-LSD -512 14 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
1524 2181 96 3H-5CT -1862 52 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 3H-5CT -1862 52 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 3H-5CT -1862 52 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 3H-5CT -1862 52 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 3H-5CT -1862 52 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 3H-5CT -1862 52 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2389 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -346 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1353 1911 93 3H-LSD -77 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -77 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -77 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -77 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -77 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
242 470 124 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2337 3256 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1809 134 32 125I-LSD -363 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 125I-LSD -363 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 125I-LSD -363 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
5 139 72 125I-LSD -999 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 125I-LSD -999 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 125I-LSD -999 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 125I-LSD -999 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1220 187 55 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
5 139 72 125I-LSD -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 72 UNDEFINED -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 125I-LSD -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 UNDEFINED -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 125I-LSD -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 UNDEFINED -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 125I-LSD -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 UNDEFINED -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
115 3791 80 125I-LSD -61 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 80 125I-LSD -61 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 80 125I-LSD -61 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
145 140 49 3H-LSD -53 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 49 3H-LSD -53 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 49 3H-LSD -53 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 49 3H-LSD -53 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115237 55585 119 3H-LSD -181 54 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 3H-LSD -181 54 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
4106 2502 22 125I-LSD -128 34 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 125I-LSD -128 34 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 125I-LSD -128 34 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 125I-LSD -128 34 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
103 4153 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
10257 738 31 3H-LSD -741 19 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 738 31 3H-LSD -741 19 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 738 31 3H-LSD -741 19 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 738 31 3H-LSD -741 19 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
2865 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1588 2325 27 3H-LSD -8 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 3H-LSD -8 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 3H-LSD -8 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 3H-LSD -8 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 3H-LSD -8 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11954224 215953 0 125I-LSD -131 58 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
2865 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2337 3256 77 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 215946 0 125I-LSD -223 24 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 216278 0 3H-LSD -3630 12 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
11954259 215979 0 3H-LSD -1202 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
100 3805 58 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
11954224 215953 0 3H-LSD -131 58 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
135398737 958 93 3H-LSD -173 89 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -173 89 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -173 89 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -173 89 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -173 89 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3294 2006 111 3H-LSD -676 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-LSD -676 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-LSD -676 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-LSD -676 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-LSD -676 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2470 3653 50 None -77624 59 Human 8.4 pKi = 8.4 Binding
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
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 None -77624 59 Human 8.4 pKi = 8.4 Binding
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
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 None -77624 59 Human 8.4 pKi = 8.4 Binding
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
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 None -77624 59 Human 8.4 pKi = 8.4 Binding
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
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 None -77624 59 Human 8.4 pKi = 8.4 Binding
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
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1524 2181 96 None -1862 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 None -1862 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 None -1862 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 None -1862 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 None -1862 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 None -1862 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2543 3707 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1342 35 49 3H-LSD -16 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 49 3H-LSD -16 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 49 3H-LSD -16 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
135398737 958 93 None -67 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -67 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -67 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -67 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -67 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
102 4127 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
216239 23795 118 None -6 7 Human 8.3 pKi = 8.3 Binding
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
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1200485 23795 118 None -6 7 Human 8.3 pKi = 8.3 Binding
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
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1336 23795 118 None -6 7 Human 8.3 pKi = 8.3 Binding
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
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
2337 3256 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1353 1911 93 None -77 83 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 None -77 83 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 None -77 83 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 None -77 83 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 None -77 83 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
242 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
134 2514 24 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2543 3707 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2435 3590 83 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1809 134 32 3H-LSD -257 36 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-LSD -257 36 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-LSD -257 36 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
3294 2006 111 3H-LSD -676 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-LSD -676 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-LSD -676 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-LSD -676 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-LSD -676 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
277 1301 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
135398737 958 93 None -173 89 Human 8.2 pKi = 8.2 Binding
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
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -173 89 Human 8.2 pKi = 8.2 Binding
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
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -173 89 Human 8.2 pKi = 8.2 Binding
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
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -173 89 Human 8.2 pKi = 8.2 Binding
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
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -173 89 Human 8.2 pKi = 8.2 Binding
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
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
33630 178957 99 None -13 28 Human 8.2 pKi = 8.2 Binding
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
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178957 99 None -13 28 Human 8.2 pKi = 8.2 Binding
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
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
102 4127 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
5022 1651 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
6918248 1651 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
8182 1651 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
CHEMBL231068 1651 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
DB04908 1651 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
1613 2348 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
133 2496 52 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
11954224 215953 0 UNDEFINED -131 58 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 215953 0 125I-LSD -131 58 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
100 3805 58 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
212 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2865 4143 73 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
115237 55585 119 None -181 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 None -181 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
4806 4008 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 4008 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 4008 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 4008 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 4008 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
2389 3331 118 None -346 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 None -346 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 None -346 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 None -346 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 None -346 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
134 2514 24 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1212 1662 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3389 217711 0 None -1 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
11978813 721 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 721 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 721 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 721 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 721 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
22530 56130 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
CHEMBL1600878 56130 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
CHEMBL1625607 56130 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
2726 919 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
141 1427 35 3H-LSD -7 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1427 35 3H-LSD -7 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1427 35 3H-LSD -7 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1427 35 3H-LSD -7 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
134 2514 24 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2514 24 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
133 2496 52 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
102 4127 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2470 3653 50 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
107780 1844 54 3H-5HT -6760 17 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 54 3H-5HT -6760 17 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 54 3H-5HT -6760 17 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
134 2514 24 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2514 24 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
103 4153 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
11954224 215953 0 None -147 58 Human 8.1 pKi = 8.1 Binding
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
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1613 2348 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
134 2514 24 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1621 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 None -27 45 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11954224 215953 0 None -131 58 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 215953 0 None -131 58 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
46780481 107531 20 None -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 None -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 None -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 None -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1621 2429 17 3H-LSD -28 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-LSD -28 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-LSD -28 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-LSD -28 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-LSD -28 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
6971132 216009 0 3H-LSD -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
4806 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
7351 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
9966051 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
CHEMBL2104993 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
DB09068 4008 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
11168182 3534 25 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
264 3534 25 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
CHEMBL1181770 3534 25 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
135398745 2914 112 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1524 2181 96 None -1862 52 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
197 2181 96 None -1862 52 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
3822 2181 96 None -1862 52 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
88 2181 96 None -1862 52 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
CHEMBL51 2181 96 None -1862 52 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
DB12465 2181 96 None -1862 52 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
2543 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
2543 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
5358 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
5358 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
54 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
54 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
CHEMBL128 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
CHEMBL128 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
DB00669 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
DB00669 3707 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
2303 3187 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
4946 3187 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
564 3187 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
63 3187 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
91536 3187 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
CHEMBL27 3187 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
CHEMBL452861 3187 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
DB00571 3187 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
135398737 958 93 None -67 89 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
38 958 93 None -67 89 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
722 958 93 None -67 89 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
CHEMBL42 958 93 None -67 89 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
DB00363 958 93 None -67 89 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
12 1553 17 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
6918513 1553 17 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
CHEMBL267615 1553 17 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
6918515 2612 38 None -158 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
71 2612 38 None -158 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
CHEMBL7318 2612 38 None -158 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
2543 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
2543 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
5358 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
5358 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
54 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
54 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
CHEMBL128 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
CHEMBL128 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
DB00669 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
DB00669 3707 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
102 4127 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
3659 4127 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
8969 4127 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
CHEMBL15245 4127 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
DB01392 4127 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
102 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
102 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
3659 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
3659 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
8969 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
8969 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
CHEMBL15245 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
CHEMBL15245 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
DB01392 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
DB01392 4127 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
115 3791 80 None -61 27 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
4296 3791 80 None -61 27 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
CHEMBL274866 3791 80 None -61 27 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
10257 738 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
10257 738 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
144 738 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
144 738 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
CHEMBL416526 738 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
CHEMBL416526 738 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
DB01445 738 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
DB01445 738 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
1220 187 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
1220 187 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
31 187 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
31 187 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
7 187 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
7 187 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
CHEMBL56 187 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
CHEMBL56 187 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
122130461 2428 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
139 2428 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
6717 2428 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
1220 187 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
1220 187 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
31 187 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
31 187 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
7 187 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
7 187 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
CHEMBL56 187 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
CHEMBL56 187 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
108029 3414 57 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
23 3414 57 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
CHEMBL18785 3414 57 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
197706 1464 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 1464 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 1464 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
133 2496 52 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
1723 2496 52 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
28693 2496 52 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
CHEMBL19215 2496 52 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
DB13520 2496 52 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
135398737 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
135398737 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
38 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
38 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
722 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
722 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
CHEMBL42 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
CHEMBL42 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
DB00363 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
DB00363 958 93 None -173 89 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
5 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
5 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
5202 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5202 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
5202 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
CHEMBL39 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
CHEMBL39 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
CHEMBL39 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
DB08839 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
DB08839 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
DB08839 139 72 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
108029 3414 57 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
23 3414 57 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
CHEMBL18785 3414 57 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
5 139 72 None -999 54 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
5202 139 72 None -999 54 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
CHEMBL39 139 72 None -999 54 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
DB08839 139 72 None -999 54 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
134 2514 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
1775 2514 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
9681 2514 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
CHEMBL1065 2514 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
DB00247 2514 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
134 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
134 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
1775 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
1775 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
9681 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
9681 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
CHEMBL1065 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
CHEMBL1065 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
DB00247 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
DB00247 2514 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
5 139 72 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5 139 72 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
5202 139 72 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5202 139 72 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
CHEMBL39 139 72 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
CHEMBL39 139 72 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
DB08839 139 72 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
DB08839 139 72 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
4106 2502 22 None -269 34 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
4106 2502 22 None -269 34 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
5358812 2502 22 None -269 34 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
5358812 2502 22 None -269 34 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
89 2502 22 None -269 34 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
89 2502 22 None -269 34 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
CHEMBL93240 2502 22 None -269 34 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
CHEMBL93240 2502 22 None -269 34 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
134 2514 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
1775 2514 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
9681 2514 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
CHEMBL1065 2514 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
DB00247 2514 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
5074 3332 80 None -69 30 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
97 3332 80 None -69 30 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
CHEMBL267777 3332 80 None -69 30 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
DB12693 3332 80 None -69 30 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
4106 2502 22 None -128 34 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
5358812 2502 22 None -128 34 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
89 2502 22 None -128 34 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
CHEMBL93240 2502 22 None -128 34 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
1809 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
1809 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
1809 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
4 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
4 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
4 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
CHEMBL18840 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
CHEMBL18840 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
CHEMBL18840 134 32 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
5074 3332 80 None -43 30 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
97 3332 80 None -43 30 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
CHEMBL267777 3332 80 None -43 30 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
DB12693 3332 80 None -43 30 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
1809 134 32 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
1809 134 32 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
4 134 32 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
4 134 32 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
CHEMBL18840 134 32 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
CHEMBL18840 134 32 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
1043 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
1043 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8450829
1043 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8549774
149 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
149 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8450829
149 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8549774
8223 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
8223 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8450829
8223 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8549774
CHEMBL442 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
CHEMBL442 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8450829
CHEMBL442 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8549774
DB00696 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
DB00696 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8450829
DB00696 1582 14 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 8549774
1809 134 32 None -363 36 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
4 134 32 None -363 36 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
CHEMBL18840 134 32 None -363 36 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
1043 1582 14 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7682702
149 1582 14 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7682702
8223 1582 14 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7682702
CHEMBL442 1582 14 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7682702
DB00696 1582 14 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7682702
1043 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
1043 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7988681
149 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
149 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7988681
8223 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
8223 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7988681
CHEMBL442 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
CHEMBL442 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7988681
DB00696 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 11343685
DB00696 1582 14 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 7988681
4106 2502 22 None -14 34 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
4106 2502 22 None -14 34 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
5358812 2502 22 None -14 34 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
5358812 2502 22 None -14 34 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
89 2502 22 None -14 34 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
89 2502 22 None -14 34 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
CHEMBL93240 2502 22 None -14 34 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
CHEMBL93240 2502 22 None -14 34 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681