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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-ergocryptine | 358 | None | 18 | Human | Binding | pKi | = | 8.09 | 8.09 | -6 | 21 | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | Drug Central | 575.3 | 5 | 3 | 6 | 2.43 | CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 | - | |
α-ergocryptine | 358 | None | 18 | Human | Binding | Ki | = | 8.22 | 8.09 | -6 | 21 | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | ChEMBL | 575.3 | 5 | 3 | 6 | 2.43 | CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 | - | |
α-ergocryptine | 358 | None | 18 | Human | Binding | IC50 | = | 13.00 | 7.89 | -6 | 21 | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | ChEMBL | 575.3 | 5 | 3 | 6 | 2.43 | CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 | - | |
α-methyl-5-HT | 364 | None | 24 | Human | Binding | pKi | None | - | 8.10 | 1 | 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/15322733 | |
α-methyl-5-HT | 364 | None | 24 | Human | Binding | pKi | None | - | 8.10 | 1 | 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/8078486 | |
α-methyl-5-HT | 364 | None | 24 | Human | Binding | pKi | None | - | 8.10 | 1 | 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 | Ki | = | 13.00 | 7.89 | 1 | 19 | Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand | ChEMBL | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1021/jm030205t | |
α-methyl-5-HT | 364 | None | 24 | Human | Binding | Ki | = | 13.00 | 7.89 | 1 | 19 | Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells | ChEMBL | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1021/jm050663x | |
α-methyl-5-HT | 364 | 3H-5HT | 24 | Human | Binding | pKi | = | 11.50 | 7.94 | 1 | 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 | Human | Binding | pKi | = | 11.90 | 7.92 | 1 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
α-methyl-5-HT | 364 | Functional | 24 | Human | Binding | pKi | = | 2.00 | 8.70 | 1 | 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 | Human | Binding | pKi | = | 6.92 | 8.16 | 1 | 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 | - | 8.00 | -1 | 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/8450835 | |
α-methyl-5-HT | 364 | 3H-5HT | 24 | Rat | Binding | pKi | = | 10.50 | 7.98 | -1 | 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 | = | 10.50 | 7.98 | -1 | 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 | = | 10.47 | 7.98 | -1 | 19 | - | PDSP KiDatabase | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | - | |
(+)-butaclamol | 746 | 3H-KETANSERIN | 9 | Bovine | Binding | pKi | = | 17.00 | 7.77 | -39 | 25 | - | PDSP KiDatabase | 361.2 | 0 | 1 | 2 | 4.84 | CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1 | - | |
(+)-chlorpheniramine | 918 | None | 42 | Human | Binding | AC50 | = | 4060.40 | 5.39 | -10 | 27 | Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration | ChEMBL | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | https://dx.doi.org/10.1038/s41467-023-40064-9 | |
(+)-chlorpheniramine | 918 | None | 42 | Human | Binding | pKi | = | 5.17 | 8.29 | -10 | 27 | None | Drug Central | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | - | |
(+)-DOI | 1458 | None | 4 | Human | Binding | pKi | None | - | 7.60 | -25 | 5 | Unclassified | Guide to Pharmacology | 321.0 | 4 | 1 | 3 | 2.20 | COc1cc(C[C@H](C)N)c(OC)cc1I | https://pubmed.ncbi.nlm.nih.gov/15322733 |
Showing 1 to 20 of 2,890 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 | |
α-methyl-5-HT | 364 | None | 24 | Rat | Functional | EC50 | = | 4.20 | 8.38 | -2 | 19 | Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats | ChEMBL | 190.1 | 2 | 3 | 2 | 1.76 | CC(N)Cc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1021/jm050663x | |
(+)-norfenfluramine | 2860 | None | 26 | Human | Functional | EC50 | = | 15.85 | 7.80 | 1 | 3 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | ChEMBL | 203.1 | 2 | 1 | 1 | 2.60 | C[C@H](N)Cc1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1021/jm0709034 | |
(+)-norfenfluramine | 2860 | None | 26 | Human | Functional | EC50 | = | 23.00 | 7.64 | 1 | 3 | Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of intracellular calcium level by calcium mobilization assay | ChEMBL | 203.1 | 2 | 1 | 1 | 2.60 | C[C@H](N)Cc1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.3c01178 | |
(+)-norfenfluramine | 2860 | None | 26 | Human | Functional | EC50 | = | 23.00 | 7.64 | 1 | 3 | Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of phospho-inositide hydrolysis by IP hydrolysis assay | ChEMBL | 203.1 | 2 | 1 | 1 | 2.60 | C[C@H](N)Cc1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.3c01178 | |
(+)-norfenfluramine | 2860 | None | 26 | Human | Functional | EC50 | = | 23.00 | 7.64 | 1 | 3 | Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of MAPK cascade by calcium mobilization assay | ChEMBL | 203.1 | 2 | 1 | 1 | 2.60 | C[C@H](N)Cc1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.3c01178 | |
(-)-propranolol | 3187 | None | 44 | Human | Functional | AC50 | = | 5000.00 | 5.30 | -389 | 34 | Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader | ChEMBL | 259.2 | 6 | 2 | 3 | 2.58 | CC(C)NC[C@H](O)COc1cccc2ccccc12 | https://dx.doi.org/10.1038/s41467-023-40064-9 | |
(R)-DOI | 2069 | None | 2 | Rat | Functional | EC50 | = | 11.90 | 7.92 | 2 | 6 | Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT | ChEMBL | 321.0 | 4 | 1 | 3 | 2.20 | COc1cc(C[C@@H](C)N)c(OC)cc1I | https://dx.doi.org/10.1016/j.bmcl.2007.03.073 | |
(R)-DOI | 2069 | None | 2 | Rat | Functional | EC50 | = | 11.90 | 7.92 | 2 | 6 | Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats | ChEMBL | 321.0 | 4 | 1 | 3 | 2.20 | COc1cc(C[C@@H](C)N)c(OC)cc1I | https://dx.doi.org/10.1021/jm050663x | |
17β-estradiol | 25 | None | 53 | Human | Functional | AC50 | = | 12000.00 | 4.92 | -7079 | 4 | Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader | ChEMBL | 272.2 | 0 | 2 | 2 | 3.61 | C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CC[C@@H]2O | https://dx.doi.org/10.1038/s41467-023-40064-9 | |
3-O-METHYL-ALPHA-METHYLDOPAMINE | 25080 | None | 22 | Rat | Functional | Kd | = | 6456.54 | 5.19 | - | 1 | Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation | ChEMBL | 181.1 | 3 | 2 | 3 | 1.29 | COc1cc(CC(C)N)ccc1O | https://dx.doi.org/10.1021/jm00183a006 | |
3-O-METHYL-ALPHA-METHYLDOPAMINE | 25080 | None | 22 | Rat | Functional | Kd | = | 3548.13 | 5.45 | - | 1 | Antagonistic against 5-hydroxytryptamine 2B receptor | ChEMBL | 181.1 | 3 | 2 | 3 | 1.29 | COc1cc(CC(C)N)ccc1O | https://dx.doi.org/10.1021/jm00183a006 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 1.50 | 8.82 | -2 | 61 | Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1016/j.bmcl.2003.05.001 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 25.12 | 7.60 | -2 | 61 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1021/jm0709034 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 5.80 | 8.24 | -2 | 61 | Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1016/j.bmc.2007.10.100 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 0.50 | 9.30 | -2 | 61 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1021/jm801354e | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 11.00 | 7.96 | -2 | 61 | Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1016/j.bmcl.2009.07.063 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 0.86 | 9.07 | -2 | 61 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1021/ml200206z | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 1.10 | 8.96 | -2 | 61 | Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1016/j.bmcl.2013.03.066 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 1.07 | 8.97 | -2 | 61 | Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1016/j.bmcl.2013.03.066 | |
5-hydroxytryptamine | 139 | None | 45 | Human | Functional | EC50 | = | 0.92 | 9.04 | -2 | 61 | Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | ChEMBL | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://dx.doi.org/10.1021/jm5019274 |
Showing 1 to 20 of 1,078 entries