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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
(+)-AJ76 | 322 | None | 18 | Human | Binding | Ki | = | 2331.00 | 5.63 | -51 | 8 | Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT ) | ChEMBL | 233.2 | 4 | 1 | 2 | 3.11 | CCCN[C@@H]1CCc2c(OC)cccc2[C@@H]1C | https://dx.doi.org/10.1016/S0960-894X(01)80181-5 | |
(-)-propranolol | 3187 | None | 44 | Human | Binding | pKi | None | - | 5.10 | -17378 | 34 | Unclassified | Guide to Pharmacology | 259.2 | 6 | 2 | 3 | 2.58 | CC(C)NC[C@H](O)COc1cccc2ccccc12 | https://pubmed.ncbi.nlm.nih.gov/7988681 | |
(1R,2S)-PHENYLPROPANOLAMINE | 27120 | 3H-LSD | 13 | Human | Binding | pKi | = | 10000.00 | 5.00 | -38 | 42 | - | PDSP KiDatabase | 151.1 | 2 | 2 | 2 | 1.07 | C[C@H](N)[C@H](O)c1ccccc1 | - | |
1-naphthylpiperazine | 35 | None | 37 | Human | Binding | Ki | = | 40.00 | 7.40 | -16 | 21 | Binding affinity for rodent 5-hydroxytryptamine 5A receptor | ChEMBL | 212.1 | 1 | 1 | 2 | 2.25 | c1ccc2c(N3CCNCC3)cccc2c1 | https://dx.doi.org/10.1021/jm030030n | |
1-naphthylpiperazine | 35 | 3H-LSD | 37 | Mouse | Binding | pKi | = | 40.00 | 7.40 | -16 | 21 | - | PDSP KiDatabase | 212.1 | 1 | 1 | 2 | 2.25 | c1ccc2c(N3CCNCC3)cccc2c1 | - | |
1-naphthylpiperazine | 35 | None | 37 | Mouse | Binding | Ki | = | 40.00 | 7.40 | -16 | 21 | Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand | ChEMBL | 212.1 | 1 | 1 | 2 | 2.25 | c1ccc2c(N3CCNCC3)cccc2c1 | https://dx.doi.org/10.1021/jm030030n | |
2-bromo-LSD | 56 | None | 11 | Mouse | Binding | Ki | = | 2.00 | 8.70 | 5 | 6 | Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand | ChEMBL | 401.1 | 3 | 1 | 2 | 3.67 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]c(Br)c(c34)C[C@H]2N(C)C1 | https://dx.doi.org/10.1021/jm030030n | |
5-CT | 134 | None | 25 | Human | Binding | pKi | None | - | 7.65 | -181 | 39 | Unclassified | Guide to Pharmacology | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://pubmed.ncbi.nlm.nih.gov/7988681 | |
5-CT | 134 | None | 25 | Human | Binding | pKi | None | - | 7.65 | -181 | 39 | Unclassified | Guide to Pharmacology | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://pubmed.ncbi.nlm.nih.gov/11343685 | |
5-CT | 134 | 3H-5CT | 25 | Human | Binding | pKi | = | 20.00 | 7.70 | -181 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | None | 25 | Human | Binding | Ki | = | 8.64 | 8.06 | -181 | 39 | PDSP Secondary Binding target: HTR5A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | ChEMBL | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://dx.doi.org/10.6019/CHEMBL5442175 | |
5-CT | 134 | None | 25 | Human | Binding | Ki | = | 20.00 | 7.70 | -181 | 39 | Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand | ChEMBL | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://dx.doi.org/10.1021/jm030030n | |
5-CT | 134 | None | 25 | Human | Binding | Ki | = | 20.00 | 7.70 | -181 | 39 | Binding affinity towards human 5-hydroxytryptamine 5A receptor | ChEMBL | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://dx.doi.org/10.1021/jm030030n | |
5-CT | 134 | 125I-LSD | 25 | Rat | Binding | pKi | = | 235.50 | 6.63 | -363 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | 125I-LSD | 25 | Rat | Binding | pKi | = | 12.58 | 7.90 | -363 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | None | 25 | Rat | Binding | pKi | None | - | 7.90 | -363 | 39 | Unclassified | Guide to Pharmacology | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://pubmed.ncbi.nlm.nih.gov/7682702 | |
5-CT | 134 | None | 25 | Mouse | Binding | pKi | None | - | 7.55 | -257 | 39 | Unclassified | Guide to Pharmacology | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://pubmed.ncbi.nlm.nih.gov/8450829 | |
5-CT | 134 | None | 25 | Mouse | Binding | pKi | None | - | 7.55 | -257 | 39 | Unclassified | Guide to Pharmacology | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://pubmed.ncbi.nlm.nih.gov/11343685 | |
5-CT | 134 | None | 25 | Mouse | Binding | pKi | None | - | 7.55 | -257 | 39 | Unclassified | Guide to Pharmacology | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | https://pubmed.ncbi.nlm.nih.gov/8549774 | |
5-CT | 134 | 125I-LSD | 25 | Mouse | Binding | pKi | = | 15.84 | 7.80 | -257 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - |
Showing 1 to 20 of 774 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
CHEMBL1169627 | 10559 | None | 31 | Human | Functional | EC50 | = | 79156.00 | 4.10 | -1 | 2 | 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 | 594.3 | 2 | 2 | 8 | 6.56 | COc1cc2c3cc1Oc1cc(ccc1O)C[C@@H]1c4c(cc(OC)c(O)c4Oc4ccc(cc4)C[C@H]3N(C)CC2)CCN1C | - | |
CHEMBL1487650 | 41061 | None | 4 | Human | Functional | EC50 | = | 47608.00 | 4.32 | 1 | 2 | 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 | 336.2 | 4 | 1 | 3 | 4.05 | COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C | - | |
CHEMBL1625496 | 56135 | None | 8 | Human | Functional | EC50 | = | 78366.00 | 4.11 | -1 | 2 | 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 | 324.2 | 7 | 2 | 3 | 3.83 | COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C | - | |
CHEMBL269964 | 97479 | None | 2 | Human | Functional | Kd | = | 7.41 | 8.13 | - | 5 | Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay | ChEMBL | 209.1 | 0 | 2 | 3 | 2.21 | CNC1=Nc2cccc(Cl)c2C(C)N1 | https://dx.doi.org/10.1016/j.bmcl.2007.10.080 | |
CHEMBL270177 | 97522 | None | 4 | Human | Functional | Kd | = | 3.02 | 8.52 | - | 6 | Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay | ChEMBL | 195.1 | 0 | 2 | 3 | 1.95 | CC1NC(N)=Nc2cccc(Cl)c21 | https://dx.doi.org/10.1016/j.bmcl.2007.10.080 | |
CHEMBL270177 | 97522 | None | 4 | Human | Functional | Kd | = | 3.16 | 8.50 | - | 6 | Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay | ChEMBL | 195.1 | 0 | 2 | 3 | 1.95 | CC1NC(N)=Nc2cccc(Cl)c21 | https://dx.doi.org/10.1016/j.bmcl.2007.10.078 | |
CHEMBL404511 | 155686 | None | 3 | Human | Functional | Kd | = | 38.90 | 7.41 | - | 5 | Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay | ChEMBL | 259.1 | 2 | 2 | 3 | 2.85 | CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 | https://dx.doi.org/10.1016/j.bmcl.2007.10.078 | |
CHEMBL5077128 | 216971 | None | 8 | Human | Functional | EC50 | = | 354.81 | 6.45 | - | 1 | 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 assay | ChEMBL | - | - | - | - | - | CS(=O)(=O)C1(CNCc2cccc3cccnc23)CC1 | https://dx.doi.org/10.1021/acs.jmedchem.1c02031 | |
CHEMBL5082447 | 217292 | None | 2 | Human | Functional | EC50 | = | 3630.78 | 5.44 | - | 1 | 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 assay | ChEMBL | - | - | - | - | - | CS(=O)(=O)C1(CNCc2ccc(Cl)c3cccnc23)CC1 | https://dx.doi.org/10.1021/acs.jmedchem.1c02031 | |
ethylisopropylamiloride | 1591 | None | 47 | Human | Functional | EC50 | = | 85847.00 | 4.07 | -10 | 5 | 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 | 299.1 | 4 | 3 | 5 | 0.36 | CCN(c1nc(N)c(C(=O)N=C(N)N)nc1Cl)C(C)C | - |
Showing 1 to 10 of 10 entries