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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 | Ki | = | 24.00 | 7.62 | -10 | 21 | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | 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 | pKi | = | 8.37 | 8.08 | -10 | 21 | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | 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 | IC50 | = | 48.00 | 7.32 | -10 | 21 | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | 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 | = | 6.00 | 8.22 | -1 | 14 | None | Drug Central | 183.1 | 3 | 4 | 4 | 0.35 | CNCC(O)c1ccc(O)c(O)c1 | - | |
| (±)-adrenaline | 3139 | 125I-HEAT | 60 | Rat | Binding | pKi | = | 10000.00 | 5.00 | -1995 | 14 | - | PDSP KiDatabase | 183.1 | 3 | 4 | 4 | 0.35 | CNCC(O)c1ccc(O)c(O)c1 | - | |
| (+)-adrenaline | 290 | None | 26 | Human | Binding | pKi | = | - | 6.00 | 3 | 5 | 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/7651358 | |
| (+)-chlorpheniramine | 918 | None | 42 | Human | Binding | Ki | = | 16575.00 | 4.78 | -602 | 27 | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | ChEMBL | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | - | |
| (+)-chlorpheniramine | 918 | None | 42 | Human | Binding | IC50 | = | 33721.00 | 4.47 | -602 | 27 | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | ChEMBL | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | - | |
| (+)-chlorpheniramine | 918 | None | 42 | Human | Binding | pKi | = | 4.78 | 8.32 | -602 | 27 | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | Drug Central | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | - | |
| (+)-cyclazosin | 1278 | None | 10 | Human | Binding | Ki | = | 31.62 | 7.50 | -5 | 9 | Binding affinity was tested on cloned rat Alpha-1D adrenergic receptor | ChEMBL | 437.2 | 4 | 1 | 8 | 3.10 | COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC | https://dx.doi.org/10.1021/jm960697s | |
| (+)-cyclazosin | 1278 | None | 10 | Human | Binding | Ki | = | 0.17 | 9.77 | -5 | 9 | Displacement of [3H]prazosin from human Alpha-1D adrenoceptor expressed in CHO cells | ChEMBL | 437.2 | 4 | 1 | 8 | 3.10 | COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC | https://dx.doi.org/10.1021/jm8016046 | |
| (+)-CYCLAZOSIN | 85391 | None | 0 | Human | Binding | Ki | = | 3.24 | 8.49 | -15 | 5 | Displacement of [3H]prazosin from Homo sapiens (human) alpha1D adrenergic receptor | ChEMBL | 437.2 | 4 | 1 | 8 | 3.10 | COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@@H]43)nc(N)c2cc1OC | https://dx.doi.org/10.1007/s00044-004-0024-8 | |
| (+)-cyclazosin | 1278 | None | 10 | Human | Binding | Ki | = | 3.24 | 8.49 | -5 | 9 | Displacement of [3H]prazosin from human alpha1D adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method | ChEMBL | 437.2 | 4 | 1 | 8 | 3.10 | COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC | https://dx.doi.org/10.1016/j.bmc.2018.05.023 | |
| (+)-cyclazosin | 1278 | None | 10 | Human | Binding | Ki | = | 3.24 | 8.49 | -5 | 9 | Displacement of [3H]prazosin from human adrenergic alpha-1d receptor expressed in CHO cells | ChEMBL | 437.2 | 4 | 1 | 8 | 3.10 | COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC | https://dx.doi.org/10.1016/j.bmc.2007.01.028 | |
| (+)-cyclazosin | 1278 | None | 10 | Human | Binding | pKi | = | - | 9.20 | -5 | 9 | Unclassified | Guide to Pharmacology | 437.2 | 4 | 1 | 8 | 3.10 | COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC | https://pubmed.ncbi.nlm.nih.gov/8917649 | |
| (+)-cyclazosin | 1278 | None | 10 | Human | Binding | pKi | = | - | 9.20 | -5 | 9 | Unclassified | Guide to Pharmacology | 437.2 | 4 | 1 | 8 | 3.10 | COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC | https://pubmed.ncbi.nlm.nih.gov/32608144 | |
| (+)-cyclazosin | 1278 | None | 10 | Rat | Binding | pKi | None | - | 7.60 | -79 | 9 | Unclassified | Guide to Pharmacology | 437.2 | 4 | 1 | 8 | 3.10 | COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H]4CCCC[C@H]43)nc(N)c2cc1OC | https://pubmed.ncbi.nlm.nih.gov/8917649 | |
| (-)-adrenaline | 291 | None | 40 | Human | Binding | pKi | = | - | 6.25 | -17 | 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/7651358 | |
| (-)-adrenaline | 291 | None | 40 | Human | Binding | pKi | = | - | 6.25 | -17 | 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/8564227 | |
| (-)-adrenaline | 291 | None | 40 | Human | Binding | pKi | = | - | 6.25 | -17 | 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/34355529 | |
Showing 1 to 20 of 2,216 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 | = | - | 7.20 | -9 | 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/34355529 | |
| (-)-noradrenaline | 2857 | None | 46 | Human | Functional | pEC50 | = | - | 7.20 | -5 | 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/34355529 | |
| CHEMBL100198 | 4205 | None | 0 | Human | Functional | EC50 | = | 199.53 | 6.70 | -10 | 3 | Potency against cloned human alpha 1D-adrenoceptor expressed in rat-1 fibroblasts. | ChEMBL | 246.1 | 4 | 2 | 4 | 0.80 | CN(C)C(=O)c1ccccc1NCC1=NCCN1 | https://dx.doi.org/10.1016/s0960-894x(01)00569-8 | |
| CHEMBL114669 | 9954 | None | 0 | Human | Functional | EC50 | = | 31.62 | 7.50 | -5 | 2 | Activation of human Alpha-1D adrenergic receptors expressed in rat-1 fibroblasts | ChEMBL | 241.1 | 3 | 3 | 4 | 1.96 | Oc1ccc2cccc(NCC3=NCCN3)c2c1 | https://dx.doi.org/10.1016/s0960-894x(02)00753-9 | |
| CHEMBL117248 | 10876 | None | 0 | Human | Functional | EC50 | = | 8.91 | 8.05 | -1 | 6 | Agonist potency at Alpha-1D adrenergic receptor assayed in rat-1 fibroblasts | ChEMBL | 221.1 | 4 | 2 | 4 | 1.82 | CSc1ccccc1NCC1=NCCN1 | https://dx.doi.org/10.1021/jm000542r | |
| CHEMBL117248 | 10876 | None | 0 | Human | Functional | EC50 | = | 7.94 | 8.10 | -1 | 6 | Activation of human Alpha-1D adrenergic receptors expressed in rat-1 fibroblasts | ChEMBL | 221.1 | 4 | 2 | 4 | 1.82 | CSc1ccccc1NCC1=NCCN1 | https://dx.doi.org/10.1016/s0960-894x(02)00753-9 | |
| CHEMBL118055 | 11559 | None | 1 | Human | Functional | EC50 | = | 19.95 | 7.70 | 1 | 3 | Activation of human Alpha-1D adrenergic receptors expressed in rat-1 fibroblasts | ChEMBL | 219.1 | 4 | 2 | 3 | 2.74 | CSc1ccccc1NCc1c[nH]cn1 | https://dx.doi.org/10.1016/s0960-894x(02)00753-9 | |
| CHEMBL1190038 | 13057 | None | 0 | Human | Functional | EC50 | = | 51.29 | 7.29 | -15 | 6 | Agonist potency at Alpha-1D adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1D adrenergic receptor | ChEMBL | 235.1 | 5 | 2 | 4 | 2.21 | CCSc1ccccc1NCC1=NCCN1 | https://dx.doi.org/10.1021/jm000542r | |
| CHEMBL142387 | 33940 | None | 0 | Human | Functional | EC50 | = | 25.12 | 7.60 | -5 | 3 | Activation of recombinant human adrenergic, alpha-1D receptor expressed in rat-1 fibroblasts assayed via calcium mobilization through Gq coupled PLC pathway | ChEMBL | 259.1 | 4 | 1 | 5 | 2.19 | c1ccc(-c2ccns2)c(OCC2=NCCN2)c1 | https://dx.doi.org/10.1016/s0960-894x(01)00764-8 | |
| CHEMBL142784 | 34391 | None | 0 | Human | Functional | EC50 | = | 5.01 | 8.30 | -10 | 3 | Activation of recombinant human adrenergic, alpha-1D receptor expressed in rat-1 fibroblasts assayed via calcium mobilization through Gq coupled PLC pathway | ChEMBL | 242.1 | 4 | 1 | 4 | 2.33 | c1ccc(-c2ccoc2)c(OCC2=NCCN2)c1 | https://dx.doi.org/10.1016/s0960-894x(01)00764-8 | |
| CHEMBL142871 | 34497 | None | 0 | Human | Functional | EC50 | = | 31.62 | 7.50 | -12 | 3 | Activation of recombinant human adrenergic, alpha-1D receptor expressed in rat-1 fibroblasts assayed via calcium mobilization through Gq coupled PLC pathway | ChEMBL | 259.1 | 4 | 1 | 5 | 2.19 | c1ccc(-c2nccs2)c(OCC2=NCCN2)c1 | https://dx.doi.org/10.1016/s0960-894x(01)00764-8 | |
| CHEMBL143801 | 35442 | None | 0 | Human | Functional | EC50 | = | 15.85 | 7.80 | -15 | 3 | Activation of recombinant human adrenergic, alpha-1D receptor expressed in rat-1 fibroblasts assayed via calcium mobilization through Gq coupled PLC pathway | ChEMBL | 258.1 | 4 | 1 | 4 | 2.80 | c1csc(-c2ccccc2OCC2=NCCN2)c1 | https://dx.doi.org/10.1016/s0960-894x(01)00764-8 | |
| CHEMBL152155 | 44771 | None | 0 | Human | Functional | EC50 | = | 16.22 | 7.79 | -34 | 3 | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | ChEMBL | 241.1 | 4 | 2 | 4 | 2.36 | c1coc(-c2ccccc2NCC2=NCCN2)c1 | https://dx.doi.org/10.1016/s0960-894x(01)00822-8 | |
| CHEMBL152693 | 45369 | None | 0 | Human | Functional | EC50 | = | 48.98 | 7.31 | -57 | 3 | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | ChEMBL | 271.1 | 4 | 2 | 4 | 3.14 | Cc1ccsc1-c1ccccc1NCC1=NCCN1 | https://dx.doi.org/10.1016/s0960-894x(01)00822-8 | |
| CHEMBL154298 | 47169 | None | 0 | Human | Functional | EC50 | = | 41.69 | 7.38 | -3 | 3 | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | ChEMBL | 252.1 | 4 | 2 | 4 | 2.16 | c1ccc(-c2ccccc2NCC2=NCCN2)nc1 | https://dx.doi.org/10.1016/s0960-894x(01)00822-8 | |
| CHEMBL155326 | 48288 | None | 0 | Human | Functional | EC50 | = | 5.01 | 8.30 | -2 | 3 | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | ChEMBL | 242.1 | 4 | 2 | 5 | 1.75 | c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 | https://dx.doi.org/10.1016/s0960-894x(01)00822-8 | |
| CHEMBL155327 | 48289 | None | 0 | Human | Functional | EC50 | = | 2.88 | 8.54 | -1 | 3 | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | ChEMBL | 242.1 | 4 | 2 | 5 | 1.75 | c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 | https://dx.doi.org/10.1016/s0960-894x(01)00822-8 | |
| CHEMBL156661 | 49702 | None | 0 | Human | Functional | EC50 | = | 81.28 | 7.09 | -4 | 3 | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | ChEMBL | 253.1 | 4 | 2 | 5 | 1.56 | c1cnc(-c2ccccc2NCC2=NCCN2)nc1 | https://dx.doi.org/10.1016/s0960-894x(01)00822-8 | |
| CHEMBL156893 | 49987 | None | 0 | Human | Functional | EC50 | = | 28.84 | 7.54 | 1 | 2 | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | ChEMBL | 268.1 | 4 | 3 | 6 | 1.14 | Nc1nccc(-c2ccccc2NCC2=NCCN2)n1 | https://dx.doi.org/10.1016/s0960-894x(01)00822-8 | |
| CHEMBL17151 | 59529 | None | 0 | Human | Functional | EC50 | = | 3162.28 | 5.50 | -501 | 2 | Agonism of recombinant human alpha-1D adrenergic receptor, expressed in rat 1 fibroblast cells | ChEMBL | 284.2 | 5 | 2 | 6 | 1.94 | CC(C)n1ncnc1-c1ccccc1NCC1=NCCN1 | https://dx.doi.org/10.1016/s0960-894x(03)00050-7 | |
Showing 1 to 20 of 159 entries