Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | 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 (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | 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
| |
| 3635 | 2734 | None | 34 | Human | Functional | pEC50 | = | 7.7 | 7.7 | 1698 | 2 | Agonist activity at recombinant full length human GPR18 expressed in CHO cells assessed as forskolin-stimulated cAMP accumulation after 10 mins by enzyme immunoassayAgonist activity at recombinant full length human GPR18 expressed in CHO cells assessed as forskolin-stimulated cAMP accumulation after 10 mins by enzyme immunoassay |
ChEMBL | 361 | 16 | 2 | 2 | 5.3 | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O | 10.1016/j.ejmech.2018.05.050 | ||
| 5283389 | 2734 | None | 34 | Human | Functional | pEC50 | = | 7.7 | 7.7 | 1698 | 2 | Agonist activity at recombinant full length human GPR18 expressed in CHO cells assessed as forskolin-stimulated cAMP accumulation after 10 mins by enzyme immunoassayAgonist activity at recombinant full length human GPR18 expressed in CHO cells assessed as forskolin-stimulated cAMP accumulation after 10 mins by enzyme immunoassay |
ChEMBL | 361 | 16 | 2 | 2 | 5.3 | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL161343 | 2734 | None | 34 | Human | Functional | pEC50 | = | 7.7 | 7.7 | 1698 | 2 | Agonist activity at recombinant full length human GPR18 expressed in CHO cells assessed as forskolin-stimulated cAMP accumulation after 10 mins by enzyme immunoassayAgonist activity at recombinant full length human GPR18 expressed in CHO cells assessed as forskolin-stimulated cAMP accumulation after 10 mins by enzyme immunoassay |
ChEMBL | 361 | 16 | 2 | 2 | 5.3 | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O | 10.1016/j.ejmech.2018.05.050 | ||
| 3635 | 2734 | None | 34 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 1698 | 2 | Agonist activity at recombinant human GPR18 expressed in HEK293 cells assessed as induction of p44/42 MAPK phosphorylation after 5 mins by Western blot analysisAgonist activity at recombinant human GPR18 expressed in HEK293 cells assessed as induction of p44/42 MAPK phosphorylation after 5 mins by Western blot analysis |
ChEMBL | 361 | 16 | 2 | 2 | 5.3 | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O | 10.1016/j.ejmech.2018.05.050 | ||
| 5283389 | 2734 | None | 34 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 1698 | 2 | Agonist activity at recombinant human GPR18 expressed in HEK293 cells assessed as induction of p44/42 MAPK phosphorylation after 5 mins by Western blot analysisAgonist activity at recombinant human GPR18 expressed in HEK293 cells assessed as induction of p44/42 MAPK phosphorylation after 5 mins by Western blot analysis |
ChEMBL | 361 | 16 | 2 | 2 | 5.3 | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL161343 | 2734 | None | 34 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 1698 | 2 | Agonist activity at recombinant human GPR18 expressed in HEK293 cells assessed as induction of p44/42 MAPK phosphorylation after 5 mins by Western blot analysisAgonist activity at recombinant human GPR18 expressed in HEK293 cells assessed as induction of p44/42 MAPK phosphorylation after 5 mins by Western blot analysis |
ChEMBL | 361 | 16 | 2 | 2 | 5.3 | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O | 10.1016/j.ejmech.2018.05.050 | ||
| 145958405 | 162173 | None | 0 | Human | Functional | pIC50 | = | 5 | 5.0 | - | 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 assayAntagonist 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 | 10 | 0 | 5 | 6.0 | Cc1cccc(C)c1OCCCCCCOc1cccc(/C=C2\N=C3SCCCN3C2=O)c1 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4160778 | 162173 | None | 0 | Human | Functional | pIC50 | = | 5 | 5.0 | - | 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 assayAntagonist 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 | 10 | 0 | 5 | 6.0 | Cc1cccc(C)c1OCCCCCCOc1cccc(/C=C2\N=C3SCCCN3C2=O)c1 | 10.1016/j.ejmech.2018.05.050 | ||
| 145974549 | 163153 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | 3 | 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 assayAntagonist 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 | 456 | 9 | 0 | 5 | 5.6 | O=C1/C(=C/c2cccc(OCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4176317 | 163153 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | 3 | 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 assayAntagonist 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 | 456 | 9 | 0 | 5 | 5.6 | O=C1/C(=C/c2cccc(OCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 145954189 | 162755 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 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 assayAntagonist 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 | 498 | 12 | 0 | 5 | 6.8 | O=C1/C(=C/c2cccc(OCCCCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4169939 | 162755 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 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 assayAntagonist 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 | 498 | 12 | 0 | 5 | 6.8 | O=C1/C(=C/c2cccc(OCCCCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 145958034 | 162336 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 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 assayAntagonist 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 | 4 | 1 | 4 | 4.1 | CSC1=NC(=O)/C(=C/c2cccc(OCc3ccc(Cl)cc3)c2)N1 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4163505 | 162336 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 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 assayAntagonist 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 | 4 | 1 | 4 | 4.1 | CSC1=NC(=O)/C(=C/c2cccc(OCc3ccc(Cl)cc3)c2)N1 | 10.1016/j.ejmech.2018.05.050 | ||
| 145952824 | 162728 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 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 assayAntagonist 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 | 6 | 0 | 4 | 4.4 | O=C1/C(=C/c2cccc(OCCCc3ccccc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4169536 | 162728 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 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 assayAntagonist 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 | 6 | 0 | 4 | 4.4 | O=C1/C(=C/c2cccc(OCCCc3ccccc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 145956612 | 162086 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 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 assayAntagonist 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 | 11 | 0 | 5 | 6.4 | O=C1/C(=C/c2cccc(OCCCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4159298 | 162086 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 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 assayAntagonist 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 | 11 | 0 | 5 | 6.4 | O=C1/C(=C/c2cccc(OCCCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 145954816 | 162652 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 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 assayAntagonist 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 | 4 | 0 | 4 | 4.7 | O=C1/C(=C/c2cccc(OCc3ccc(Br)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4168388 | 162652 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 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 assayAntagonist 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 | 4 | 0 | 4 | 4.7 | O=C1/C(=C/c2cccc(OCc3ccc(Br)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 145958480 | 162269 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 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 assayAntagonist 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 | 6 | 1 | 4 | 6.4 | O=C1NC(SCc2ccc(Br)cc2)=N/C1=C\c1cccc(OCc2ccc(Cl)cc2)c1 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4162436 | 162269 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 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 assayAntagonist 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 | 6 | 1 | 4 | 6.4 | O=C1NC(SCc2ccc(Br)cc2)=N/C1=C\c1cccc(OCc2ccc(Cl)cc2)c1 | 10.1016/j.ejmech.2018.05.050 | ||
| 145951064 | 163056 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | 12 | 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 assayAntagonist 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 | 450 | 10 | 0 | 5 | 5.7 | Cc1ccc(OCCCCCCOc2cccc(/C=C3\N=C4SCCCN4C3=O)c2)cc1 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4174825 | 163056 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | 12 | 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 assayAntagonist 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 | 450 | 10 | 0 | 5 | 5.7 | Cc1ccc(OCCCCCCOc2cccc(/C=C3\N=C4SCCCN4C3=O)c2)cc1 | 10.1016/j.ejmech.2018.05.050 | ||
| 145950071 | 162862 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 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 assayAntagonist 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 | 442 | 8 | 0 | 5 | 5.3 | O=C1/C(=C/c2cccc(OCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4171815 | 162862 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 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 assayAntagonist 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 | 442 | 8 | 0 | 5 | 5.3 | O=C1/C(=C/c2cccc(OCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 145958551 | 162386 | None | 0 | Human | Functional | pIC50 | = | 4.6 | 4.6 | - | 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 assayAntagonist 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 | 11 | 0 | 5 | 5.9 | CCc1ccc(OCCCCCCOc2cccc(/C=C3\N=C4SCCCN4C3=O)c2)cc1 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4164171 | 162386 | None | 0 | Human | Functional | pIC50 | = | 4.6 | 4.6 | - | 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 assayAntagonist 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 | 11 | 0 | 5 | 5.9 | CCc1ccc(OCCCCCCOc2cccc(/C=C3\N=C4SCCCN4C3=O)c2)cc1 | 10.1016/j.ejmech.2018.05.050 | ||
| 145958428 | 162200 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 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 assayAntagonist 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 | 7 | 0 | 5 | 4.9 | O=C1/C(=C/c2cccc(OCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4161205 | 162200 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 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 assayAntagonist 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 | 7 | 0 | 5 | 4.9 | O=C1/C(=C/c2cccc(OCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 10871668 | 162115 | None | 1 | Human | Functional | pIC50 | = | 4.5 | 4.5 | -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 assayAntagonist 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 | 4 | 2 | 3 | 3.3 | O=C1NC(=S)N/C1=C\c1cccc(OCc2ccc(Cl)cc2)c1 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4159707 | 162115 | None | 1 | Human | Functional | pIC50 | = | 4.5 | 4.5 | -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 assayAntagonist 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 | 4 | 2 | 3 | 3.3 | O=C1NC(=S)N/C1=C\c1cccc(OCc2ccc(Cl)cc2)c1 | 10.1016/j.ejmech.2018.05.050 | ||
| 145951404 | 162944 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | 2 | 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 assayAntagonist 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 | 364 | 4 | 0 | 4 | 4.3 | Cc1ccc(COc2cccc(/C=C3\N=C4SCCCN4C3=O)c2)cc1 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4172931 | 162944 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | 2 | 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 assayAntagonist 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 | 364 | 4 | 0 | 4 | 4.3 | Cc1ccc(COc2cccc(/C=C3\N=C4SCCCN4C3=O)c2)cc1 | 10.1016/j.ejmech.2018.05.050 | ||
| 145971274 | 163204 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 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 assayAntagonist 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 | 448 | 7 | 1 | 4 | 5.7 | O=C1NC(SCCc2ccccc2)=N/C1=C\c1cccc(OCc2ccc(Cl)cc2)c1 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4177155 | 163204 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 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 assayAntagonist 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 | 448 | 7 | 1 | 4 | 5.7 | O=C1NC(SCCc2ccccc2)=N/C1=C\c1cccc(OCc2ccc(Cl)cc2)c1 | 10.1016/j.ejmech.2018.05.050 | ||
| 145960178 | 162230 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | 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 assayAntagonist 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 | 6 | 0 | 5 | 4.5 | O=C1/C(=C/c2cccc(OCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4161619 | 162230 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | 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 assayAntagonist 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 | 6 | 0 | 5 | 4.5 | O=C1/C(=C/c2cccc(OCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 145953879 | 162658 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 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 assayAntagonist 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 | 10 | 0 | 5 | 6.0 | O=C1/C(=C/c2cccc(OCCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| CHEMBL4168457 | 162658 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 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 assayAntagonist 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 | 10 | 0 | 5 | 6.0 | O=C1/C(=C/c2cccc(OCCCCCCOc3ccc(Cl)cc3)c2)N=C2SCCCN12 | 10.1016/j.ejmech.2018.05.050 | ||
| 4150 | 788 | None | 26 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -7 | 16 | NoneNone |
Drug Central | 314 | 6 | 2 | 2 | 5.8 | CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C | None | ||
| 5288 | 788 | None | 26 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -7 | 16 | NoneNone |
Drug Central | 314 | 6 | 2 | 2 | 5.8 | CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C | None | ||
| 644019 | 788 | None | 26 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -7 | 16 | NoneNone |
Drug Central | 314 | 6 | 2 | 2 | 5.8 | CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C | None | ||
| 644019.0 | 788 | None | 26 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -7 | 16 | NoneNone |
Drug Central | 314 | 6 | 2 | 2 | 5.8 | CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C | None | ||
| CHEMBL190461 | 788 | None | 26 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -7 | 16 | NoneNone |
Drug Central | 314 | 6 | 2 | 2 | 5.8 | CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C | None | ||
| DB09061 | 788 | None | 26 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -7 | 16 | NoneNone |
Drug Central | 314 | 6 | 2 | 2 | 5.8 | CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C | None | ||
| 16078 | 1362 | None | 15 | Human | Functional | pEC50 | = | 8.2 | 8.2 | -58 | 7 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
Drug Central | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | None | ||
| 16078.0 | 1362 | None | 15 | Human | Functional | pEC50 | = | 8.2 | 8.2 | -58 | 7 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
Drug Central | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | None | ||
| 2424 | 1362 | None | 15 | Human | Functional | pEC50 | = | 8.2 | 8.2 | -58 | 7 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
Drug Central | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | None | ||
| 4109 | 1362 | None | 15 | Human | Functional | pEC50 | = | 8.2 | 8.2 | -58 | 7 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
Drug Central | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | None | ||
Showing 1 to 50 of 100 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | 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 (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | 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
| |
| 104850 | 3330 | None | 58 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1039/C3MD00394A | ||
| 4150 | 3330 | None | 58 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1039/C3MD00394A | ||
| 743 | 3330 | None | 58 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1039/C3MD00394A | ||
| CHEMBL111 | 3330 | None | 58 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1039/C3MD00394A | ||
| DB06155 | 3330 | None | 58 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1039/C3MD00394A | ||
| 162656142 | 181046 | None | 2 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysisAgonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis |
ChEMBL | 392 | 3 | 1 | 7 | 1.8 | Cn1c(=O)c2c(nc3n2CCCCN3CCc2c[nH]c3ccccc23)n(C)c1=O | 10.1021/acsmedchemlett.0c00208 | ||
| CHEMBL4758188 | 181046 | None | 2 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysisAgonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis |
ChEMBL | 392 | 3 | 1 | 7 | 1.8 | Cn1c(=O)c2c(nc3n2CCCCN3CCc2c[nH]c3ccccc23)n(C)c1=O | 10.1021/acsmedchemlett.0c00208 | ||
| 16078 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| 16078.0 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| 2424 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| 4109 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| CHEMBL465 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| DB00470 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| 16078 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assayAgonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1021/jm4005175 | ||
| 16078.0 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assayAgonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1021/jm4005175 | ||
| 2424 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assayAgonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1021/jm4005175 | ||
| 4109 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assayAgonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1021/jm4005175 | ||
| CHEMBL465 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assayAgonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1021/jm4005175 | ||
| DB00470 | 1362 | None | 15 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 6 | Agonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assayAgonist activity at human GPR18 transfected in CHO cells after 90 mins by beta-arrestin translocation assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1021/jm4005175 | ||
| 11081 | 3217 | None | 6 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 6 | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysisAgonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis |
ChEMBL | 378 | 3 | 1 | 7 | 1.4 | Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 | 10.1021/acsmedchemlett.0c00208 | ||
| 44437220 | 3217 | None | 6 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 6 | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysisAgonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis |
ChEMBL | 378 | 3 | 1 | 7 | 1.4 | Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 | 10.1021/acsmedchemlett.0c00208 | ||
| CHEMBL239232 | 3217 | None | 6 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 6 | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysisAgonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis |
ChEMBL | 378 | 3 | 1 | 7 | 1.4 | Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 | 10.1021/acsmedchemlett.0c00208 | ||
| 162663623 | 182138 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysisAgonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis |
ChEMBL | 364 | 3 | 1 | 7 | 1.0 | Cn1c(=O)c2c(nc3n2CCN3CCc2c[nH]c3ccccc23)n(C)c1=O | 10.1021/acsmedchemlett.0c00208 | ||
| CHEMBL4780863 | 182138 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysisAgonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis |
ChEMBL | 364 | 3 | 1 | 7 | 1.0 | Cn1c(=O)c2c(nc3n2CCN3CCc2c[nH]c3ccccc23)n(C)c1=O | 10.1021/acsmedchemlett.0c00208 | ||
| 104895 | 1184 | None | 15 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 4 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 376 | 10 | 3 | 3 | 5.7 | CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C | 10.1039/C3MD00394A | ||
| 730 | 1184 | None | 15 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 4 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 376 | 10 | 3 | 3 | 5.7 | CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C | 10.1039/C3MD00394A | ||
| 734 | 1184 | None | 15 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 4 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 376 | 10 | 3 | 3 | 5.7 | CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C | 10.1039/C3MD00394A | ||
| CHEMBL559612 | 1184 | None | 15 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 4 | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation methodAgonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method |
ChEMBL | 376 | 10 | 3 | 3 | 5.7 | CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C | 10.1039/C3MD00394A | ||
| 16078 | 1362 | None | 15 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 6 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| 16078.0 | 1362 | None | 15 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 6 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| 2424 | 1362 | None | 15 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 6 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| 4109 | 1362 | None | 15 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 6 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| CHEMBL465 | 1362 | None | 15 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 6 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| DB00470 | 1362 | None | 15 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 6 | Agonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assayAgonist activity at human GPR18 expressed in HEK203 cells by MAP kinase assay |
ChEMBL | 314 | 4 | 1 | 2 | 5.7 | CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C | 10.1039/C3MD00394A | ||
| 1281706 | 109560 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | 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 methodAntagonist 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 | 3 | 0 | 4 | 4.2 | O=C1/C(=C/c2cccc(Oc3ccccc3)c2)N=C2SCCCN12 | 10.1039/C3MD00394A | ||
| CHEMBL3221186 | 109560 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | 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 methodAntagonist 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 | 3 | 0 | 4 | 4.2 | O=C1/C(=C/c2cccc(Oc3ccccc3)c2)N=C2SCCCN12 | 10.1039/C3MD00394A | ||
| 90667660 | 109569 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 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 methodAntagonist 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 | 4 | 0 | 4 | 4.3 | O=C1/C(=C/c2cccc(OCc3ccccc3)c2)N=C2SCCCCN12 | 10.1039/C3MD00394A | ||
| CHEMBL3221197 | 109569 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 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 methodAntagonist 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 | 4 | 0 | 4 | 4.3 | O=C1/C(=C/c2cccc(OCc3ccccc3)c2)N=C2SCCCCN12 | 10.1039/C3MD00394A | ||
| 71682799 | 90605 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 2 | 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 assayAntagonist 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 | 7 | 0 | 3 | 5.8 | CCCCCc1cc(OC)c2cc(Cc3ccc(Cl)cc3)c(=O)oc2c1 | 10.1021/jm4005175 | ||
| CHEMBL2387530 | 90605 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 2 | 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 assayAntagonist 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 | 7 | 0 | 3 | 5.8 | CCCCCc1cc(OC)c2cc(Cc3ccc(Cl)cc3)c(=O)oc2c1 | 10.1021/jm4005175 | ||
| 104850 | 3330 | None | 58 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 6 | 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 assayAntagonist 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 | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1021/jm4005175 | ||
| 4150 | 3330 | None | 58 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 6 | 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 assayAntagonist 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 | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1021/jm4005175 | ||
| 743 | 3330 | None | 58 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 6 | 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 assayAntagonist 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 | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1021/jm4005175 | ||
| CHEMBL111 | 3330 | None | 58 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 6 | 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 assayAntagonist 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 | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1021/jm4005175 | ||
| DB06155 | 3330 | None | 58 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 6 | 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 assayAntagonist 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 | 462 | 4 | 1 | 4 | 5.9 | Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 | 10.1021/jm4005175 | ||
| 71682637 | 90654 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 1 | 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 assayAntagonist 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 | 4 | 0 | 3 | 4.8 | COc1ccccc1Cc1cc2c(C)ccc(C(C)C)c2oc1=O | 10.1021/jm4005175 | ||
| CHEMBL2387744 | 90654 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 1 | 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 assayAntagonist 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 | 4 | 0 | 3 | 4.8 | COc1ccccc1Cc1cc2c(C)ccc(C(C)C)c2oc1=O | 10.1021/jm4005175 | ||
| 70678101 | 83069 | None | 23 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 2 | 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 assayAntagonist 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 | 9 | 2 | 4 | 6.4 | CCCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3O)c(=O)oc2c1 | 10.1021/jm4005175 | ||
| CHEMBL2181542 | 83069 | None | 23 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 2 | 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 assayAntagonist 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 | 9 | 2 | 4 | 6.4 | CCCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3O)c(=O)oc2c1 | 10.1021/jm4005175 | ||
| 76325292 | 105513 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | 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 assayInverse 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 | 4 | 2 | 2 | 6.5 | 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 | 10.1021/np400850g | ||
Showing 1 to 50 of 86 entries