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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 | |
| Δ9-tetrahydrocannabinol | 1362 | None | 15 | Human | Binding | EC50 | = | 960.00 | 6.02 | - | 9 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay | ChEMBL | 314.2 | 4 | 1 | 2 | 5.74 | CCCCCc1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21 | https://dx.doi.org/10.1039/C3MD00394A | |
| Δ9-tetrahydrocannabinol | 1362 | None | 15 | Human | Binding | EC50 | = | 4610.00 | 5.34 | - | 9 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 314.2 | 4 | 1 | 2 | 5.74 | CCCCCc1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21 | https://dx.doi.org/10.1039/C3MD00394A | |
| Δ9-tetrahydrocannabinol | 1362 | None | 15 | Human | Binding | EC50 | = | 4610.00 | 5.34 | - | 9 | Agonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assay | ChEMBL | 314.2 | 4 | 1 | 2 | 5.74 | CCCCCc1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21 | https://dx.doi.org/10.1021/jm4005175 | |
| CHEMBL1258979 | 17849 | None | 0 | Human | Binding | IC50 | = | 9910.00 | 5.00 | - | 3 | Inverse agonist activity at human GPR18 expressed in CHO cells assessed as inhibition of 7.5 uM THC-mediated beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay | ChEMBL | 403.3 | 1 | 1 | 1 | 6.94 | CC(C)=C[C@H]1C[C@]2(C)[C@H](CC[C@@]3(C)[C@H]2CC[C@H]2Cc4c([nH]c5ccccc45)[C@@]23C)O1 | https://dx.doi.org/10.1021/np400850g | |
| CHEMBL2177264 | 82541 | None | 0 | Human | Binding | IC50 | = | 8100.00 | 5.09 | - | 4 | Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay | ChEMBL | 378.2 | 8 | 1 | 3 | 6.34 | CCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3)c(=O)oc2c1 | https://dx.doi.org/10.1021/jm4005175 | |
| CHEMBL2181540 | 83067 | None | 0 | Human | Binding | IC50 | = | 15900.00 | 4.80 | - | 4 | Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay | ChEMBL | 394.2 | 8 | 2 | 4 | 6.04 | CCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3O)c(=O)oc2c1 | https://dx.doi.org/10.1021/jm4005175 | |
| CHEMBL2181542 | 83069 | None | 23 | Human | Binding | IC50 | = | 12500.00 | 4.90 | - | 4 | Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay | ChEMBL | 408.2 | 9 | 2 | 4 | 6.43 | CCCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3O)c(=O)oc2c1 | https://dx.doi.org/10.1021/jm4005175 | |
| CHEMBL2387530 | 90605 | None | 0 | Human | Binding | IC50 | = | 10000.00 | 5.00 | - | 4 | Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay | ChEMBL | 370.1 | 7 | 0 | 3 | 5.78 | CCCCCc1cc(OC)c2cc(Cc3ccc(Cl)cc3)c(=O)oc2c1 | https://dx.doi.org/10.1021/jm4005175 | |
| CHEMBL2387744 | 90654 | None | 0 | Human | Binding | IC50 | = | 11300.00 | 4.95 | - | 3 | Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay | ChEMBL | 322.2 | 4 | 0 | 3 | 4.82 | COc1ccccc1Cc1cc2c(C)ccc(C(C)C)c2oc1=O | https://dx.doi.org/10.1021/jm4005175 | |
| CHEMBL3120632 | 105513 | None | 0 | Human | Binding | IC50 | = | 13400.00 | 4.87 | - | 1 | Inverse agonist activity at human GPR18 expressed in CHO cells assessed as inhibition of 7.5 uM THC-mediated beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay | ChEMBL | 435.3 | 4 | 2 | 2 | 6.55 | COC(C)(C)/C=C/C[C@]1(C)[C@@H](O)CC[C@@]2(C)[C@H]1CC[C@H]1Cc3c([nH]c4ccccc34)[C@@]12C | https://dx.doi.org/10.1021/np400850g | |
| CHEMBL3217791 | 109288 | None | 0 | Human | Binding | IC50 | = | 14300.00 | 4.84 | - | 1 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 398.0 | 3 | 0 | 5 | 4.24 | O=C(Oc1cccc(/C=C2\N=C3SCCCN3C2=O)c1)c1ccc(Cl)cc1 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3220943 | 109547 | None | 0 | Human | Binding | IC50 | = | 6450.00 | 5.19 | - | 2 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 392.1 | 3 | 0 | 5 | 4.28 | Cc1ccc(C(=O)Oc2cccc(/C=C3\N=C4SCCCCN4C3=O)c2)cc1 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3221186 | 109560 | None | 0 | Human | Binding | IC50 | = | 10000.00 | 5.00 | - | 1 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 336.1 | 3 | 0 | 4 | 4.16 | O=C1/C(=C/c2cccc(Oc3ccccc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3221187 | 109561 | None | 0 | Human | Binding | IC50 | = | 7220.00 | 5.14 | - | 2 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 350.1 | 4 | 0 | 4 | 3.94 | O=C1/C(=C/c2cccc(OCc3ccccc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3221188 | 109562 | None | 22 | Human | Binding | IC50 | = | 279.00 | 6.55 | - | 2 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 384.1 | 4 | 0 | 4 | 4.59 | O=C1/C(=C/c2cccc(OCc3ccc(Cl)cc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3221189 | 109563 | None | 0 | Human | Binding | IC50 | = | 1650.00 | 5.78 | - | 1 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 384.1 | 4 | 0 | 4 | 4.59 | O=C1/C(=C/c2cccc(OCc3ccccc3Cl)c2)N=C2SCCCN12 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3221190 | 109564 | None | 0 | Human | Binding | IC50 | = | 2550.00 | 5.59 | - | 3 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 418.0 | 4 | 0 | 4 | 5.25 | O=C1/C(=C/c2cccc(OCc3ccc(Cl)cc3Cl)c2)N=C2SCCCN12 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3221191 | 109565 | None | 0 | Human | Binding | IC50 | = | 6160.00 | 5.21 | - | 2 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 418.0 | 4 | 0 | 4 | 5.25 | O=C1/C(=C/c2cccc(OCc3ccc(Cl)c(Cl)c3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3221192 | 109566 | None | 0 | Human | Binding | IC50 | = | 6350.00 | 5.20 | - | 1 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 364.1 | 3 | 0 | 5 | 3.58 | O=C(Oc1cccc(/C=C2\N=C3SCCCN3C2=O)c1)c1ccccc1 | https://dx.doi.org/10.1039/C3MD00394A | |
| CHEMBL3221196 | 109568 | None | 0 | Human | Binding | IC50 | = | 14100.00 | 4.85 | - | 2 | Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method | ChEMBL | 350.1 | 3 | 0 | 4 | 4.54 | O=C1/C(=C/c2cccc(Oc3ccccc3)c2)N=C2SCCCCN12 | https://dx.doi.org/10.1039/C3MD00394A | |
Showing 1 to 20 of 31 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 | |
| Δ9-tetrahydrocannabinol | 1362 | None | 15 | Human | Functional | pEC50 | = | - | 6.02 | -58 | 9 | Unclassified | Guide to Pharmacology | 314.2 | 4 | 1 | 2 | 5.74 | CCCCCc1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21 | https://pubmed.ncbi.nlm.nih.gov/21595653 | |
| Δ9-tetrahydrocannabinol | 1362 | None | 15 | Human | Functional | pEC50 | = | - | 6.02 | -58 | 9 | Unclassified | Guide to Pharmacology | 314.2 | 4 | 1 | 2 | 5.74 | CCCCCc1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21 | https://pubmed.ncbi.nlm.nih.gov/22014123 | |
| Δ9-tetrahydrocannabinol | 1362 | None | 15 | Human | Functional | pEC50 | = | 6.02 | 8.22 | -58 | 9 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay | Drug Central | 314.2 | 4 | 1 | 2 | 5.74 | CCCCCc1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=C[C@@H]21 | - | |
| abnormal cannabidiol | 224 | None | 24 | Human | Functional | pEC50 | = | - | 6.08 | -36 | 2 | Unclassified | Guide to Pharmacology | 314.2 | 6 | 2 | 2 | 5.85 | C=C(C)[C@@H]1CCC(C)=C[C@H]1c1c(O)cc(O)cc1CCCCC | https://pubmed.ncbi.nlm.nih.gov/21595653 | |
| AM251 | 379 | None | 59 | Human | Functional | pEC50 | = | - | 4.02 | -4466 | 7 | Unclassified | Guide to Pharmacology | 554.0 | 4 | 1 | 4 | 5.89 | Cc1c(C(=O)NN2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(I)cc1 | https://pubmed.ncbi.nlm.nih.gov/21595653 | |
| anandamide | 413 | None | 27 | Human | Functional | pEC50 | = | - | 5.42 | -208 | 7 | Unclassified | Guide to Pharmacology | 347.3 | 16 | 2 | 2 | 5.24 | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCCO | https://pubmed.ncbi.nlm.nih.gov/21595653 | |
| arachidonylcyclopropylamide | 459 | None | 20 | Human | Functional | pEC50 | = | - | 4.87 | - | 4 | Unclassified | Guide to Pharmacology | 343.3 | 15 | 1 | 1 | 6.41 | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1 | https://pubmed.ncbi.nlm.nih.gov/21595653 | |
| cannabidiol | 788 | None | 26 | Human | Functional | pEC50 | = | - | 4.29 | -7 | 23 | Unclassified | Guide to Pharmacology | 314.2 | 6 | 2 | 2 | 5.85 | C=C(C)[C@@H]1CCC(C)=C[C@H]1c1c(O)cc(CCCCC)cc1O | https://pubmed.ncbi.nlm.nih.gov/21595653 | |
| cannabidiol | 788 | None | 26 | Human | Functional | pEC50 | = | 4.29 | 8.37 | -7 | 23 | None | Drug Central | 314.2 | 6 | 2 | 2 | 5.85 | C=C(C)[C@@H]1CCC(C)=C[C@H]1c1c(O)cc(CCCCC)cc1O | - | |
| CHEMBL4159298 | 162086 | None | 0 | Human | Functional | IC50 | = | 1710.00 | 5.77 | - | 1 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 484.2 | 11 | 0 | 5 | 6.42 | O=C1/C(=C/c2cccc(OCCCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4159707 | 162115 | None | 1 | Human | Functional | IC50 | = | 33000.00 | 4.48 | -1 | 2 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 344.0 | 4 | 2 | 3 | 3.26 | O=C1NC(=S)N/C1=C\c1cccc(OCc2ccc(Cl)cc2)c1 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4160778 | 162173 | None | 0 | Human | Functional | IC50 | = | 10000.00 | 5.00 | - | 1 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 464.2 | 10 | 0 | 5 | 6.00 | Cc1cccc(C)c1OCCCCCCOc1cccc(/C=C2\N=C3SCCCN3C2=O)c1 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4161205 | 162200 | None | 0 | Human | Functional | IC50 | = | 3250.00 | 5.49 | - | 1 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 428.1 | 7 | 0 | 5 | 4.86 | O=C1/C(=C/c2cccc(OCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4161619 | 162230 | None | 0 | Human | Functional | IC50 | = | 5000.00 | 5.30 | 1 | 2 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 414.1 | 6 | 0 | 5 | 4.47 | O=C1/C(=C/c2cccc(OCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4162436 | 162269 | None | 0 | Human | Functional | IC50 | = | 2290.00 | 5.64 | - | 1 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 512.0 | 6 | 1 | 4 | 6.44 | O=C1NC(SCc2ccc(Br)cc2)=N/C1=C\c1cccc(OCc2ccc(Cl)cc2)c1 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4163505 | 162336 | None | 0 | Human | Functional | IC50 | = | 13800.00 | 4.86 | - | 3 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 358.1 | 4 | 1 | 4 | 4.11 | CSC1=NC(=O)/C(=C/c2cccc(OCc3ccc(Cl)cc3)c2)N1 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4164171 | 162386 | None | 0 | Human | Functional | IC50 | = | 25000.00 | 4.60 | - | 1 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 464.2 | 11 | 0 | 5 | 5.94 | CCc1ccc(OCCCCCCOc2cccc(/C=C3\N=C4SCCCN4C3=O)c2)cc1 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4168388 | 162652 | None | 0 | Human | Functional | IC50 | = | 1730.00 | 5.76 | 26 | 2 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 428.0 | 4 | 0 | 4 | 4.70 | O=C1/C(=C/c2cccc(OCc3ccc(Br)cc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4168457 | 162658 | None | 0 | Human | Functional | IC50 | = | 650.00 | 6.19 | - | 1 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 470.1 | 10 | 0 | 5 | 6.03 | O=C1/C(=C/c2cccc(OCCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
| CHEMBL4169536 | 162728 | None | 0 | Human | Functional | IC50 | = | 1490.00 | 5.83 | 4 | 2 | Antagonist activity at recombinant human GPR18 expressed in CHO cells assessed as inhibition of delta9-THC-induced beta-arrestin recruitment preincubated for 60 mins followed by delta9-THC addition for 90 mins measured for 1 sec by luminescence assay | ChEMBL | 378.1 | 6 | 0 | 4 | 4.37 | O=C1/C(=C/c2cccc(OCCCc3ccccc3)c2)N=C2SCCCN12 | https://dx.doi.org/10.1016/j.ejmech.2018.05.050 | |
Showing 1 to 20 of 34 entries