Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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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
CHEMBL465 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
DB00470 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
2125 379 None 59 Human Functional pEC50 = 4.0 4.0 -4466 4
UnclassifiedUnclassified
Guide to Pharmacology 554 4 1 4 5.9 Ic1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 21595653
3317 379 None 59 Human Functional pEC50 = 4.0 4.0 -4466 4
UnclassifiedUnclassified
Guide to Pharmacology 554 4 1 4 5.9 Ic1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 21595653
CHEMBL285932 379 None 59 Human Functional pEC50 = 4.0 4.0 -4466 4
UnclassifiedUnclassified
Guide to Pharmacology 554 4 1 4 5.9 Ic1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 21595653
4150 788 None 26 Human Functional pEC50 = 4.3 4.3 -7 16
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 21595653
5288 788 None 26 Human Functional pEC50 = 4.3 4.3 -7 16
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 21595653
644019 788 None 26 Human Functional pEC50 = 4.3 4.3 -7 16
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 21595653
644019.0 788 None 26 Human Functional pEC50 = 4.3 4.3 -7 16
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 21595653
CHEMBL190461 788 None 26 Human Functional pEC50 = 4.3 4.3 -7 16
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 21595653
DB09061 788 None 26 Human Functional pEC50 = 4.3 4.3 -7 16
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 21595653
5311007 459 None 20 Human Functional pEC50 = 4.9 4.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 343 15 1 1 6.4 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1 21595653
739 459 None 20 Human Functional pEC50 = 4.9 4.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 343 15 1 1 6.4 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1 21595653
CHEMBL418353 459 None 20 Human Functional pEC50 = 4.9 4.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 343 15 1 1 6.4 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1 21595653
2364 413 None 27 Human Functional pEC50 = 5.4 5.4 -208 3
UnclassifiedUnclassified
Guide to Pharmacology 347 16 2 2 5.2 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCCO 21595653
5281969 413 None 27 Human Functional pEC50 = 5.4 5.4 -208 3
UnclassifiedUnclassified
Guide to Pharmacology 347 16 2 2 5.2 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCCO 21595653
CHEMBL15848 413 None 27 Human Functional pEC50 = 5.4 5.4 -208 3
UnclassifiedUnclassified
Guide to Pharmacology 347 16 2 2 5.2 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCCO 21595653
16078 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 21595653
16078 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 22014123
16078.0 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 21595653
16078.0 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 22014123
2424 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 21595653
2424 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 22014123
4109 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 21595653
4109 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 22014123
CHEMBL465 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 21595653
CHEMBL465 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 22014123
DB00470 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 21595653
DB00470 1362 None 15 Human Functional pEC50 = 6.0 6.0 -58 7
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 22014123
5526 224 None 24 Human Functional pEC50 = 6.1 6.1 -36 2
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)cc(c1[C@@H]1C=C(C)CC[C@H]1C(=C)C)O 21595653
89949 224 None 24 Human Functional pEC50 = 6.1 6.1 -36 2
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)cc(c1[C@@H]1C=C(C)CC[C@H]1C(=C)C)O 21595653
CHEMBL499876 224 None 24 Human Functional pEC50 = 6.1 6.1 -36 2
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)cc(c1[C@@H]1C=C(C)CC[C@H]1C(=C)C)O 21595653
11081 3217 None 6 Human Functional pEC50 = 6.3 6.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
44437220 3217 None 6 Human Functional pEC50 = 6.3 6.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
CHEMBL239232 3217 None 6 Human Functional pEC50 = 6.3 6.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
45073499 2900 None 27 Human Functional pEC50 = 7.2 7.2 -22 2
UnclassifiedUnclassified
Guide to Pharmacology 258 2 2 2 4.4 CC1=C[C@H]([C@@H](CC1)C(=C)C)c1c(C)cc(cc1O)O 21595653
5525 2900 None 27 Human Functional pEC50 = 7.2 7.2 -22 2
UnclassifiedUnclassified
Guide to Pharmacology 258 2 2 2 4.4 CC1=C[C@H]([C@@H](CC1)C(=C)C)c1c(C)cc(cc1O)O 21595653
CHEMBL3402654 2900 None 27 Human Functional pEC50 = 7.2 7.2 -22 2
UnclassifiedUnclassified
Guide to Pharmacology 258 2 2 2 4.4 CC1=C[C@H]([C@@H](CC1)C(=C)C)c1c(C)cc(cc1O)O 21595653
13424 3219 None 0 Human Functional pEC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 446 6 2 7 2.8 N1C=C(C2=CC=CC=C12)CCNC3=NC=4N(C(N(C(C4N3CC5=CC=C(C=C5)F)=O)C)=O)C 38885438
4874768 3219 None 0 Human Functional pEC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 446 6 2 7 2.8 N1C=C(C2=CC=CC=C12)CCNC3=NC=4N(C(N(C(C4N3CC5=CC=C(C=C5)F)=O)C)=O)C 38885438
3635 2734 None 34 Human Functional pEC50 = 7.5 7.5 1698 2
UnclassifiedUnclassified
Guide to Pharmacology 361 16 2 2 5.3 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O 21595653
5283389 2734 None 34 Human Functional pEC50 = 7.5 7.5 1698 2
UnclassifiedUnclassified
Guide to Pharmacology 361 16 2 2 5.3 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O 21595653
CHEMBL161343 2734 None 34 Human Functional pEC50 = 7.5 7.5 1698 2
UnclassifiedUnclassified
Guide to Pharmacology 361 16 2 2 5.3 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O 21595653
13425 3218 None 0 Human Functional pEC50 = 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 462 6 2 7 3.3 N1C=C(C2=CC=CC=C12)CCNC3=NC=4N(C(N(C(C4N3CC5=CC=C(C=C5)Cl)=O)C)=O)C 38885438
4874764 3218 None 0 Human Functional pEC50 = 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 462 6 2 7 3.3 N1C=C(C2=CC=CC=C12)CCNC3=NC=4N(C(N(C(C4N3CC5=CC=C(C=C5)Cl)=O)C)=O)C 38885438
104850 3330 None 58 Human Functional pIC50 = 8.3 8.3 -72 28
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
Drug Central 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 None
4150 3330 None 58 Human Functional pIC50 = 8.3 8.3 -72 28
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
Drug Central 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 None
743 3330 None 58 Human Functional pIC50 = 8.3 8.3 -72 28
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
Drug Central 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 None
CHEMBL111 3330 None 58 Human Functional pIC50 = 8.3 8.3 -72 28
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
Drug Central 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 None
DB06155 3330 None 58 Human Functional pIC50 = 8.3 8.3 -72 28
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
Drug Central 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 None


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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

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 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
CHEMBL3120632 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
11152300 109568 None 0 Human Binding pIC50 = 4.9 4.9 - 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 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 350 3 0 4 4.5 O=C1/C(=C/c2cccc(Oc3ccccc3)c2)N=C2SCCCCN12 10.1039/C3MD00394A
CHEMBL3221196 109568 None 0 Human Binding pIC50 = 4.9 4.9 - 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 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 350 3 0 4 4.5 O=C1/C(=C/c2cccc(Oc3ccccc3)c2)N=C2SCCCCN12 10.1039/C3MD00394A
90667659 109288 None 0 Human Binding pIC50 = 4.8 4.8 - 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 398 3 0 5 4.2 O=C(Oc1cccc(/C=C2\N=C3SCCCN3C2=O)c1)c1ccc(Cl)cc1 10.1039/C3MD00394A
CHEMBL3217791 109288 None 0 Human Binding pIC50 = 4.8 4.8 - 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 398 3 0 5 4.2 O=C(Oc1cccc(/C=C2\N=C3SCCCN3C2=O)c1)c1ccc(Cl)cc1 10.1039/C3MD00394A
70678099 83067 None 0 Human Binding pIC50 = 4.8 4.8 - 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 394 8 2 4 6.0 CCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3O)c(=O)oc2c1 10.1021/jm4005175
CHEMBL2181540 83067 None 0 Human Binding pIC50 = 4.8 4.8 - 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 394 8 2 4 6.0 CCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3O)c(=O)oc2c1 10.1021/jm4005175
90667655 109563 None 0 Human Binding pIC50 = 5.8 5.8 - 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 384 4 0 4 4.6 O=C1/C(=C/c2cccc(OCc3ccccc3Cl)c2)N=C2SCCCN12 10.1039/C3MD00394A
CHEMBL3221189 109563 None 0 Human Binding pIC50 = 5.8 5.8 - 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 384 4 0 4 4.6 O=C1/C(=C/c2cccc(OCc3ccccc3Cl)c2)N=C2SCCCN12 10.1039/C3MD00394A
90667656 109564 None 0 Human Binding pIC50 = 5.6 5.6 - 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 418 4 0 4 5.2 O=C1/C(=C/c2cccc(OCc3ccc(Cl)cc3Cl)c2)N=C2SCCCN12 10.1039/C3MD00394A
CHEMBL3221190 109564 None 0 Human Binding pIC50 = 5.6 5.6 - 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 418 4 0 4 5.2 O=C1/C(=C/c2cccc(OCc3ccc(Cl)cc3Cl)c2)N=C2SCCCN12 10.1039/C3MD00394A
85469571 109562 None 22 Human Binding pIC50 = 6.6 6.6 - 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 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 384 4 0 4 4.6 O=C1/C(=C/c2cccc(OCc3ccc(Cl)cc3)c2)N=C2SCCCN12 10.1039/C3MD00394A
CHEMBL3221188 109562 None 22 Human Binding pIC50 = 6.6 6.6 - 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 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 384 4 0 4 4.6 O=C1/C(=C/c2cccc(OCc3ccc(Cl)cc3)c2)N=C2SCCCN12 10.1039/C3MD00394A
11475997 109573 None 0 Human Binding pIC50 = 5.3 5.3 - 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 432 4 0 4 5.6 O=C1/C(=C/c2cccc(OCc3ccc(Cl)cc3Cl)c2)N=C2SCCCCN12 10.1039/C3MD00394A
CHEMBL3221201 109573 None 0 Human Binding pIC50 = 5.3 5.3 - 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 432 4 0 4 5.6 O=C1/C(=C/c2cccc(OCc3ccc(Cl)cc3Cl)c2)N=C2SCCCCN12 10.1039/C3MD00394A
104895 1184 None 15 Human Binding pIC50 = 5.2 5.2 - 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 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 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/jm4005175
730 1184 None 15 Human Binding pIC50 = 5.2 5.2 - 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 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 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/jm4005175
734 1184 None 15 Human Binding pIC50 = 5.2 5.2 - 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 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 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/jm4005175
CHEMBL559612 1184 None 15 Human Binding pIC50 = 5.2 5.2 - 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 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 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/jm4005175
90667657 109565 None 0 Human Binding pIC50 = 5.2 5.2 - 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 418 4 0 4 5.2 O=C1/C(=C/c2cccc(OCc3ccc(Cl)c(Cl)c3)c2)N=C2SCCCN12 10.1039/C3MD00394A
CHEMBL3221191 109565 None 0 Human Binding pIC50 = 5.2 5.2 - 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 418 4 0 4 5.2 O=C1/C(=C/c2cccc(OCc3ccc(Cl)c(Cl)c3)c2)N=C2SCCCN12 10.1039/C3MD00394A
90667658 109566 None 0 Human Binding pIC50 = 5.2 5.2 - 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 364 3 0 5 3.6 O=C(Oc1cccc(/C=C2\N=C3SCCCN3C2=O)c1)c1ccccc1 10.1039/C3MD00394A
CHEMBL3221192 109566 None 0 Human Binding pIC50 = 5.2 5.2 - 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 364 3 0 5 3.6 O=C(Oc1cccc(/C=C2\N=C3SCCCN3C2=O)c1)c1ccccc1 10.1039/C3MD00394A
90667465 109547 None 0 Human Binding pIC50 = 5.2 5.2 - 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 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 392 3 0 5 4.3 Cc1ccc(C(=O)Oc2cccc(/C=C3\N=C4SCCCCN4C3=O)c2)cc1 10.1039/C3MD00394A
CHEMBL3220943 109547 None 0 Human Binding pIC50 = 5.2 5.2 - 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 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 392 3 0 5 4.3 Cc1ccc(C(=O)Oc2cccc(/C=C3\N=C4SCCCCN4C3=O)c2)cc1 10.1039/C3MD00394A
90667662 109572 None 0 Human Binding pIC50 = 5.2 5.2 - 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 398 4 0 4 5.0 O=C1/C(=C/c2cccc(OCc3ccccc3Cl)c2)N=C2SCCCCN12 10.1039/C3MD00394A
CHEMBL3221200 109572 None 0 Human Binding pIC50 = 5.2 5.2 - 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 398 4 0 4 5.0 O=C1/C(=C/c2cccc(OCc3ccccc3Cl)c2)N=C2SCCCCN12 10.1039/C3MD00394A
90667654 109561 None 0 Human Binding pIC50 = 5.1 5.1 - 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 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 350 4 0 4 3.9 O=C1/C(=C/c2cccc(OCc3ccccc3)c2)N=C2SCCCN12 10.1039/C3MD00394A
CHEMBL3221187 109561 None 0 Human Binding pIC50 = 5.1 5.1 - 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 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 350 4 0 4 3.9 O=C1/C(=C/c2cccc(OCc3ccccc3)c2)N=C2SCCCN12 10.1039/C3MD00394A
70678097 82541 None 0 Human Binding pIC50 = 5.1 5.1 - 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 378 8 1 3 6.3 CCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3)c(=O)oc2c1 10.1021/jm4005175
CHEMBL2177264 82541 None 0 Human Binding pIC50 = 5.1 5.1 - 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 378 8 1 3 6.3 CCCCCCC(C)(C)c1cc(O)c2cc(Cc3ccccc3)c(=O)oc2c1 10.1021/jm4005175
11081 3217 None 6 Human Binding pIC50 = 6.0 6.0 - 6
Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment by measuring 2-(3-(6-(4-chlorophenoxy)hexyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one IC50 at 1 uM 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 by measuring 2-(3-(6-(4-chlorophenoxy)hexyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one IC50 at 1 uM 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 pIC50 = 6.0 6.0 - 6
Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment by measuring 2-(3-(6-(4-chlorophenoxy)hexyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one IC50 at 1 uM 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 by measuring 2-(3-(6-(4-chlorophenoxy)hexyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one IC50 at 1 uM 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 pIC50 = 6.0 6.0 - 6
Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment by measuring 2-(3-(6-(4-chlorophenoxy)hexyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one IC50 at 1 uM 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 by measuring 2-(3-(6-(4-chlorophenoxy)hexyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one IC50 at 1 uM 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
23643046 17849 None 0 Human Binding pIC50 = 5 5.0 - 2
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 403 1 1 1 6.9 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 10.1021/np400850g
CHEMBL1258979 17849 None 0 Human Binding pIC50 = 5 5.0 - 2
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 403 1 1 1 6.9 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 10.1021/np400850g