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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 | = | 5.73 | 8.24 | -79 | 21 | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | 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 | = | 1872.00 | 5.73 | -79 | 21 | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | 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 | = | 2496.00 | 5.60 | -79 | 21 | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | 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 | - | |
(±)-adrenaline | 3139 | None | 60 | Human | Binding | pKi | None | - | 4.30 | -10000 | 14 | Unclassified | Guide to Pharmacology | 183.1 | 3 | 4 | 4 | 0.35 | CNCC(O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/8719421 | |
(±)-adrenaline | 3139 | None | 60 | Human | Binding | pKi | None | - | 4.30 | -10000 | 14 | Unclassified | Guide to Pharmacology | 183.1 | 3 | 4 | 4 | 0.35 | CNCC(O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/7903415 | |
(±)-adrenaline | 3139 | None | 60 | Human | Binding | pKi | None | - | 4.30 | -10000 | 14 | Unclassified | Guide to Pharmacology | 183.1 | 3 | 4 | 4 | 0.35 | CNCC(O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/14730417 | |
(±)-adrenaline | 3139 | None | 60 | Rat | Binding | pKi | None | - | 5.30 | -1000 | 14 | Unclassified | Guide to Pharmacology | 183.1 | 3 | 4 | 4 | 0.35 | CNCC(O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/8719421 | |
(±)-adrenaline | 3139 | None | 60 | Mouse | Binding | pKi | None | - | 5.30 | -1000 | 14 | Unclassified | Guide to Pharmacology | 183.1 | 3 | 4 | 4 | 0.35 | CNCC(O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/8719421 | |
(-)-adrenaline | 291 | None | 40 | Human | Binding | pKi | = | - | 4.30 | -4168 | 35 | Unclassified | Guide to Pharmacology | 183.1 | 3 | 4 | 4 | 0.35 | CNC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/14730417 | |
(-)-adrenaline | 291 | None | 40 | Human | Binding | pKi | = | - | 4.30 | -4168 | 35 | Unclassified | Guide to Pharmacology | 183.1 | 3 | 4 | 4 | 0.35 | CNC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/20590599 | |
(-)-adrenaline | 291 | 125I-CYP | 40 | Human | Binding | pKi | = | 10000.00 | 5.00 | -4168 | 35 | - | PDSP KiDatabase | 183.1 | 3 | 4 | 4 | 0.35 | CNC[C@H](O)c1ccc(O)c(O)c1 | - | |
(-)-noradrenaline | 2857 | None | 46 | Human | Binding | pKi | = | - | 5.50 | -26 | 32 | Unclassified | Guide to Pharmacology | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/9131260 | |
(-)-noradrenaline | 2857 | None | 46 | Human | Binding | pKi | = | - | 5.50 | -26 | 32 | Unclassified | Guide to Pharmacology | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/14730417 | |
(-)-noradrenaline | 2857 | None | 46 | Human | Binding | pKi | = | - | 5.50 | -26 | 32 | Unclassified | Guide to Pharmacology | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/14744619 | |
(-)-noradrenaline | 2857 | None | 46 | Human | Binding | pKi | None | 5.37 | 8.27 | -26 | 32 | None | Drug Central | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | - | |
(-)-noradrenaline | 2857 | None | 46 | Rat | Binding | pKi | = | - | 4.20 | -12882 | 32 | Unclassified | Guide to Pharmacology | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/14744619 | |
(-)-noradrenaline | 2857 | None | 46 | Mouse | Binding | pKi | = | - | 3.80 | -32359 | 32 | Unclassified | Guide to Pharmacology | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/14744619 | |
(-)-pindolol | 3126 | None | 37 | Human | Binding | Ki | = | 36.00 | 7.44 | -83 | 15 | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | ChEMBL | 248.2 | 6 | 3 | 3 | 1.91 | CC(C)NC[C@H](O)COc1cccc2[nH]ccc12 | - | |
(-)-pindolol | 3126 | None | 37 | Human | Binding | IC50 | = | 48.00 | 7.32 | -83 | 15 | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | ChEMBL | 248.2 | 6 | 3 | 3 | 1.91 | CC(C)NC[C@H](O)COc1cccc2[nH]ccc12 | - | |
(-)-propranolol | 3187 | None | 44 | Human | Binding | pKi | = | - | 6.75 | -213 | 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/10079020 |
Showing 1 to 20 of 726 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 | |
(-)-adrenaline | 291 | None | 40 | Human | Functional | pEC50 | = | - | 6.50 | -4 | 35 | Unclassified | Guide to Pharmacology | 183.1 | 3 | 4 | 4 | 0.35 | CNC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/20590599 | |
(-)-adrenaline | 291 | None | 40 | Human | Functional | EC50 | = | 31.00 | 7.51 | -4 | 35 | Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method | ChEMBL | 183.1 | 3 | 4 | 4 | 0.35 | CNC[C@H](O)c1ccc(O)c(O)c1 | https://dx.doi.org/10.1016/j.bmc.2007.11.060 | |
(-)-adrenaline | 291 | None | 40 | Human | Functional | EC50 | = | 49.00 | 7.31 | -4 | 35 | Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay | ChEMBL | 183.1 | 3 | 4 | 4 | 0.35 | CNC[C@H](O)c1ccc(O)c(O)c1 | https://dx.doi.org/10.1016/j.bmc.2007.11.060 | |
(-)-noradrenaline | 2857 | None | 46 | Human | Functional | pEC50 | = | - | 7.20 | -1 | 32 | Unclassified | Guide to Pharmacology | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://pubmed.ncbi.nlm.nih.gov/20590599 | |
(-)-noradrenaline | 2857 | None | 46 | Human | Functional | EC50 | = | 6.30 | 8.20 | -1 | 32 | Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay | ChEMBL | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://dx.doi.org/10.1016/j.bmc.2007.11.060 | |
(-)-noradrenaline | 2857 | None | 46 | Human | Functional | EC50 | = | 5.50 | 8.26 | -1 | 32 | Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method | ChEMBL | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://dx.doi.org/10.1016/j.bmc.2007.11.060 | |
(-)-noradrenaline | 2857 | None | 46 | Rat | Functional | EC50 | = | 1580.00 | 5.80 | -1000 | 32 | Effective dose for contraction of reserpine-pretreated rat vas deferens | ChEMBL | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://dx.doi.org/10.1021/jm00019a001 | |
(-)-noradrenaline | 2857 | None | 46 | Rat | Functional | EC50 | = | 100000.00 | 4.00 | -1000 | 32 | Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes. | ChEMBL | 169.1 | 2 | 4 | 4 | 0.09 | NC[C@H](O)c1ccc(O)c(O)c1 | https://dx.doi.org/10.1021/jm00019a001 | |
(-)-propranolol | 3187 | None | 44 | Human | Functional | Kd | = | 162.18 | 6.79 | -158 | 34 | Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis | ChEMBL | 259.2 | 6 | 2 | 3 | 2.58 | CC(C)NC[C@H](O)COc1cccc2ccccc12 | https://dx.doi.org/10.1021/jm2008562 | |
abediterol | 221 | None | 18 | Human | Functional | pIC50 | = | - | 5.52 | -3388 | 3 | Unclassified | Guide to Pharmacology | 460.2 | 13 | 4 | 5 | 4.23 | O=c1ccc2c([C@@H](O)CNCCCCCCOCC(F)(F)c3ccccc3)ccc(O)c2[nH]1 | https://pubmed.ncbi.nlm.nih.gov/22588259 | |
alprenolol | 370 | None | 37 | Human | Functional | Kd | = | 75.86 | 7.12 | - | 16 | Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis | ChEMBL | 249.2 | 8 | 2 | 3 | 2.15 | C=CCc1ccccc1OCC(O)CNC(C)C | https://dx.doi.org/10.1021/jm2008562 | |
ARFORMOTEROL | 26817 | None | 34 | Human | Functional | EC50 | = | 25.12 | 7.60 | -16 | 7 | Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins | ChEMBL | 344.2 | 9 | 4 | 5 | 2.22 | COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 | https://dx.doi.org/10.1021/jm100326d | |
ARFORMOTEROL | 26817 | None | 34 | Human | Functional | EC50 | = | 25.12 | 7.60 | -16 | 7 | Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation | ChEMBL | 344.2 | 9 | 4 | 5 | 2.22 | COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 | https://dx.doi.org/10.1016/j.bmc.2011.08.043 | |
ARFORMOTEROL | 26817 | None | 34 | Human | Functional | pEC50 | = | 7.60 | 8.12 | -16 | 7 | Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay | Drug Central | 344.2 | 9 | 4 | 5 | 2.22 | COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 | - | |
ARFORMOTEROL | 26817 | None | 34 | Human | Functional | pEC50 | = | 7.60 | 8.12 | -16 | 7 | Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay | Drug Central | 344.2 | 9 | 4 | 5 | 2.22 | COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 | - | |
BRL 37344 | 725 | None | 16 | Human | Functional | pEC50 | = | - | 7.50 | -2 | 8 | Unclassified | Guide to Pharmacology | 363.1 | 9 | 3 | 4 | 3.06 | C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 | https://pubmed.ncbi.nlm.nih.gov/20590599 | |
BRL 37344 | 725 | None | 16 | Human | Functional | EC50 | = | 5.90 | 8.23 | -2 | 8 | Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay | ChEMBL | 363.1 | 9 | 3 | 4 | 3.06 | C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 | https://dx.doi.org/10.1016/j.bmc.2007.11.060 | |
BRL 37344 | 725 | None | 16 | Human | Functional | EC50 | = | 1.10 | 8.96 | -2 | 8 | Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method | ChEMBL | 363.1 | 9 | 3 | 4 | 3.06 | C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 | https://dx.doi.org/10.1016/j.bmc.2007.11.060 | |
BRL 37344 | 725 | None | 16 | Human | Functional | EC50 | = | 25.12 | 7.60 | -2 | 8 | Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production | ChEMBL | 363.1 | 9 | 3 | 4 | 3.06 | C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 | https://dx.doi.org/10.1021/jm0509445 | |
BRL 37344 | 725 | None | 16 | Human | Functional | EC50 | = | 680.00 | 6.17 | -2 | 8 | Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane. | ChEMBL | 363.1 | 9 | 3 | 4 | 3.06 | C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 | https://dx.doi.org/10.1016/0960-894X(96)00417-9 |
Showing 1 to 20 of 1,561 entries