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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 | |
α-methyl-5-HT | 364 | None | 24 | Human | Binding | pKi | None | - | 5.80 | -208 | 19 | Unclassified | Guide to Pharmacology | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | https://pubmed.ncbi.nlm.nih.gov/15466450 | |
α-methyl-5-HT | 364 | None | 24 | Human | Binding | pKi | None | - | 5.80 | -208 | 19 | Unclassified | Guide to Pharmacology | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | https://pubmed.ncbi.nlm.nih.gov/7796807 | |
α-methyl-5-HT | 364 | 3H-GR-113808 | 24 | Guinea pig | Binding | pKi | = | 1584.89 | 5.80 | -208 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
α-methyl-5-HT | 364 | 3H-GR-113808 | 24 | Guinea pig | Binding | pKi | = | 1584.89 | 5.80 | -208 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
α-methyl-5-HT | 364 | 3H-GR-113808 | 24 | Guinea pig | Binding | pKi | = | 1584.89 | 5.80 | -208 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
α-methyl-5-HT | 364 | 3H-GR-113808 | 24 | Guinea pig | Binding | pKi | = | 1584.89 | 5.80 | -208 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
α-methyl-5-HT | 364 | 3H-GR-113808 | 24 | Rat | Binding | pKi | = | 1450.00 | 5.84 | -89 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
α-methyl-5-HT | 364 | 3H-GR-113808 | 24 | Rat | Binding | pKi | = | 1450.00 | 5.84 | -89 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
α-methyl-5-HT | 364 | 3H-5HT | 24 | Rat | Binding | pKi | = | 263.00 | 6.58 | -89 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
α-methyl-5-HT | 364 | None | 24 | Rat | Binding | pKi | None | - | 6.10 | -89 | 19 | Unclassified | Guide to Pharmacology | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | https://pubmed.ncbi.nlm.nih.gov/8813606 | |
α-methyl-5-HT | 364 | None | 24 | Rat | Binding | pKi | None | - | 6.10 | -89 | 19 | Unclassified | Guide to Pharmacology | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | https://pubmed.ncbi.nlm.nih.gov/9225293 | |
(R)ZACOPRIDE | 98858 | None | 2 | Rat | Binding | Ki | = | 1510.00 | 5.82 | - | 1 | Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand | ChEMBL | 309.1 | 3 | 2 | 4 | 1.75 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 | https://dx.doi.org/10.1021/jm960320m | |
(R)ZACOPRIDE | 98858 | None | 2 | Rat | Binding | ED50 | = | 505.00 | 6.30 | - | 1 | Relaxation of carbachol induced contractions of rat tunica muscularis mucosae | ChEMBL | 309.1 | 3 | 2 | 4 | 1.75 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 | https://dx.doi.org/10.1021/jm00086a019 | |
5-CT | 134 | 3H-GR-113808 | 25 | Human | Binding | pKi | = | 10000.00 | 5.00 | -109647 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | 3H-GR-113808 | 25 | Guinea pig | Binding | pKi | = | 10000.00 | 5.00 | -87096 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | 3H-GR-113808 | 25 | Guinea pig | Binding | pKi | = | 6309.57 | 5.20 | -87096 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | 3H-GR-113808 | 25 | Guinea pig | Binding | pKi | = | 10000.00 | 5.00 | -87096 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | 3H-GR-113808 | 25 | Guinea pig | Binding | pKi | = | 6309.57 | 5.20 | -87096 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | 3H-GR-113808 | 25 | Rat | Binding | pKi | = | 3162.27 | 5.50 | -46773 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - | |
5-CT | 134 | 3H-RS 57639 | 25 | Rat | Binding | pKi | = | 5011.87 | 5.30 | -46773 | 39 | - | PDSP KiDatabase | 203.1 | 3 | 3 | 2 | 0.77 | NCCc1c[nH]c2ccc(C(N)=O)cc12 | - |
Showing 1 to 20 of 1,323 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 | |
(R)ZACOPRIDE | 98858 | None | 2 | Rat | Functional | EC50 | = | 501.19 | 6.30 | - | 1 | 5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae | ChEMBL | 309.1 | 3 | 2 | 4 | 1.75 | COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CN2CCC1CC2 | https://dx.doi.org/10.1016/S0960-894X(00)80352-2 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 100.00 | 7.00 | -138 | 61 | Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1038/nature05991 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 12.00 | 7.92 | -138 | 61 | Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1021/jm801327q | |
5-hydroxytryptamine | 139 | None | 45 | Rat | Functional | EC50 | = | 6.31 | 8.20 | -29 | 61 | 5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1016/S0960-894X(00)80352-2 | |
5-hydroxytryptamine | 139 | None | 45 | Rat | Functional | EC50 | = | 17.10 | 7.77 | -29 | 61 | In vitro relaxation of carbachol pre-contracted rat oesophageal TMM. | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1016/0960-894X(96)00002-9 | |
5-hydroxytryptamine | 139 | None | 45 | Rat | Functional | IC50 | = | 3.70 | 8.43 | -29 | 61 | 5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1016/S0960-894X(01)80508-4 | |
CHEMBL1162955 | 10417 | None | 0 | Human | Functional | Ki | = | 15.00 | 7.82 | - | 1 | Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells | ChEMBL | 1178.6 | 30 | 4 | 14 | 8.72 | COc1cc(N)c(Cl)cc1C(=O)OCCN1CCC(CNC(=O)CCCN(CCCc2ccc(CCCN(CCCC(=O)NCC3CCN(CCOC(=O)c4cc(Cl)c(N)cc4OC)CC3)C(=O)C(C)(C)C)cc2)C(=O)C(C)(C)C)CC1 | https://dx.doi.org/10.1021/jm070552t | |
CHEMBL116913 | 10535 | None | 0 | Rat | Functional | Ki | = | 29.70 | 7.53 | - | 1 | Tested for potency against 5-hydroxytryptamine 4 receptor agonist in rat brain | ChEMBL | 339.1 | 0 | 2 | 5 | 1.52 | Nc1cc2c(cc1Cl)C(=O)NC1CCN(CCOCCO2)CC1 | https://dx.doi.org/10.1021/jm020099f | |
CHEMBL1181147 | 11679 | None | 0 | Rat | Functional | EC50 | = | 9.55 | 8.02 | - | 1 | Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae | ChEMBL | 380.2 | 6 | 2 | 3 | 3.46 | CCCC[N+]12CCCC(C1)C(NC(=O)c1cc(Cl)c(N)cc1OC)CC2 | https://dx.doi.org/10.1016/S0960-894X(01)81243-9 | |
CHEMBL1181946 | 11812 | None | 0 | Rat | Functional | EC50 | = | 129.00 | 6.89 | - | 1 | Agonism at 5HT4 receptor in rat tunica muscularis mucosa | ChEMBL | 338.2 | 4 | 2 | 3 | 2.29 | COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CC[N@@+]2(C)CCC[C@@H]12 | https://dx.doi.org/10.1021/jm0509501 | |
CHEMBL1183709 | 12076 | None | 0 | Rat | Functional | EC50 | = | 1360.00 | 5.87 | - | 1 | In vitro relaxation of carbachol pre-contracted rat oesophageal TMM. | ChEMBL | 378.2 | 5 | 2 | 3 | 3.00 | CCCC[N+]12CCC(CC1)[C@@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 | https://dx.doi.org/10.1016/0960-894X(96)00002-9 | |
CHEMBL1185621 | 12389 | None | 0 | Rat | Functional | EC50 | = | 8.50 | 8.07 | - | 1 | In vitro relaxation of carbachol pre-contracted rat oesophageal TMM. | ChEMBL | 378.2 | 5 | 2 | 3 | 3.00 | CCCC[N+]12CCC(CC1)[C@H](NC(=O)c1cc(Cl)c(N)c3c1OCC3)C2 | https://dx.doi.org/10.1016/0960-894X(96)00002-9 | |
CHEMBL121913 | 15557 | None | 0 | Human | Functional | Kd | = | 0.70 | 9.15 | - | 1 | ,Antagonism of stimulation of 5-hydroxytryptamine receptor on the L-type calcium current (I Ca) in isolated human atrial myocytes | ChEMBL | 391.1 | 6 | 1 | 8 | 1.70 | COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ncccn2)CC1 | https://dx.doi.org/10.1021/jm0009538 | |
CHEMBL1258109 | 17585 | None | 0 | Human | Functional | EC50 | = | 8.91 | 8.05 | - | 1 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay | ChEMBL | 362.2 | 7 | 1 | 6 | 3.17 | CCCCN1CCC(COC(=O)c2ccc(NC)c3c2OCCO3)CC1 | https://dx.doi.org/10.1021/jm100668r | |
CHEMBL1258223 | 17616 | None | 0 | Human | Functional | EC50 | = | 14.13 | 7.85 | - | 26 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay | ChEMBL | 396.2 | 7 | 1 | 6 | 3.82 | CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 | https://dx.doi.org/10.1021/jm100668r | |
CHEMBL1258338 | 17646 | None | 0 | Human | Functional | EC50 | = | 10.00 | 8.00 | - | 1 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay | ChEMBL | 440.1 | 7 | 1 | 6 | 3.93 | CCCCN1CCC(COC(=O)c2cc(Br)c(NC)c3c2OCCO3)CC1 | https://dx.doi.org/10.1021/jm100668r | |
CHEMBL1258339 | 17647 | None | 0 | Human | Functional | EC50 | = | 19.95 | 7.70 | - | 1 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay | ChEMBL | 488.1 | 7 | 1 | 6 | 3.77 | CCCCN1CCC(COC(=O)c2cc(I)c(NC)c3c2OCCO3)CC1 | https://dx.doi.org/10.1021/jm100668r | |
CHEMBL1258450 | 17683 | None | 0 | Human | Functional | EC50 | = | 15.85 | 7.80 | - | 1 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay | ChEMBL | 387.2 | 7 | 1 | 7 | 3.04 | CCCCN1CCC(COC(=O)c2cc(C#N)c(NC)c3c2OCCO3)CC1 | https://dx.doi.org/10.1021/jm100668r | |
CHEMBL1258451 | 17684 | None | 0 | Human | Functional | EC50 | = | 0.18 | 9.75 | - | 1 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay | ChEMBL | 320.2 | 7 | 1 | 5 | 2.95 | CCCCN1CCC(COC(=O)c2ccc(N)cc2OC)CC1 | https://dx.doi.org/10.1021/jm100668r | |
CHEMBL1258671 | 17756 | None | 0 | Human | Functional | EC50 | = | 5.89 | 8.23 | - | 12 | Agonist activity at 5HT4 receptor expressed in HEK293/L9 cells by cAMP assay | ChEMBL | 366.2 | 6 | 1 | 6 | 2.85 | CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 | https://dx.doi.org/10.1021/jm100668r |
Showing 1 to 20 of 371 entries