Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
3635 9511 44 None 1698 2 Human 7.7 pEC50 = 7.7 Functional
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 9511 44 None 1698 2 Human 7.7 pEC50 = 7.7 Functional
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 9511 44 None 1698 2 Human 7.7 pEC50 = 7.7 Functional
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 9511 44 None 1698 2 Human 7.4 pEC50 = 7.4 Functional
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 9511 44 None 1698 2 Human 7.4 pEC50 = 7.4 Functional
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 9511 44 None 1698 2 Human 7.4 pEC50 = 7.4 Functional
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 168858 0 None - 1 Human 5.0 pIC50 = 5 Functional
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 168858 0 None - 1 Human 5.0 pIC50 = 5 Functional
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 169837 0 None 3 2 Human 5.9 pIC50 = 5.9 Functional
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 169837 0 None 3 2 Human 5.9 pIC50 = 5.9 Functional
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 169439 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 169439 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 169021 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 169021 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 169412 0 None 4 2 Human 5.8 pIC50 = 5.8 Functional
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 169412 0 None 4 2 Human 5.8 pIC50 = 5.8 Functional
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 168771 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 168771 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 169336 0 None 26 2 Human 5.8 pIC50 = 5.8 Functional
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 169336 0 None 26 2 Human 5.8 pIC50 = 5.8 Functional
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 168954 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 168954 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 169740 0 None 12 2 Human 6.6 pIC50 = 6.6 Functional
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 169740 0 None 12 2 Human 6.6 pIC50 = 6.6 Functional
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 169546 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 169546 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 169071 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
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 169071 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
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 168885 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 168885 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 168800 1 None -1 2 Human 4.5 pIC50 = 4.5 Functional
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 168800 1 None -1 2 Human 4.5 pIC50 = 4.5 Functional
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 169628 0 None 2 2 Human 5.5 pIC50 = 5.5 Functional
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 169628 0 None 2 2 Human 5.5 pIC50 = 5.5 Functional
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 169888 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 169888 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 168915 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
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 168915 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
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 169342 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 169342 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 7575 39 None -7 15 Human 8.4 pEC50 = 8.4 Functional
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 7575 39 None -7 15 Human 8.4 pEC50 = 8.4 Functional
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 7575 39 None -7 15 Human 8.4 pEC50 = 8.4 Functional
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 7575 39 None -7 15 Human 8.4 pEC50 = 8.4 Functional
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 7575 39 None -7 15 Human 8.4 pEC50 = 8.4 Functional
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 8144 22 None -58 8 Human 8.2 pEC50 = 8.2 Functional
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 8144 22 None -58 8 Human 8.2 pEC50 = 8.2 Functional
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 8144 22 None -58 8 Human 8.2 pEC50 = 8.2 Functional
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 8144 22 None -58 8 Human 8.2 pEC50 = 8.2 Functional
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 8144 22 None -58 8 Human 8.2 pEC50 = 8.2 Functional
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 7167 85 None -4466 4 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 554 4 1 4 5.9 Ic1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 21595653
3317 7167 85 None -4466 4 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 554 4 1 4 5.9 Ic1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 21595653
CHEMBL285932 7167 85 None -4466 4 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 554 4 1 4 5.9 Ic1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 21595653
4150 7575 39 None -7 15 Human 4.3 pEC50 = 4.3 Functional
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 7575 39 None -7 15 Human 4.3 pEC50 = 4.3 Functional
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 7575 39 None -7 15 Human 4.3 pEC50 = 4.3 Functional
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 7575 39 None -7 15 Human 4.3 pEC50 = 4.3 Functional
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 7575 39 None -7 15 Human 4.3 pEC50 = 4.3 Functional
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 7247 26 None -33 2 Human 4.9 pEC50 = 4.9 Functional
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 7247 26 None -33 2 Human 4.9 pEC50 = 4.9 Functional
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 7247 26 None -33 2 Human 4.9 pEC50 = 4.9 Functional
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 7201 36 None -208 4 Human 5.4 pEC50 = 5.4 Functional
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 7201 36 None -208 4 Human 5.4 pEC50 = 5.4 Functional
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 7201 36 None -208 4 Human 5.4 pEC50 = 5.4 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 8144 22 None -58 8 Human 6.0 pEC50 = 6.0 Functional
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 7012 33 None -36 2 Human 6.1 pEC50 = 6.1 Functional
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 7012 33 None -36 2 Human 6.1 pEC50 = 6.1 Functional
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 7012 33 None -36 2 Human 6.1 pEC50 = 6.1 Functional
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 9991 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
44437220 9991 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
CHEMBL239232 9991 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
45073499 9675 38 None -22 2 Human 7.2 pEC50 = 7.2 Functional
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 9675 38 None -22 2 Human 7.2 pEC50 = 7.2 Functional
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 9675 38 None -22 2 Human 7.2 pEC50 = 7.2 Functional
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 9993 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 9993 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 9511 44 None 1698 2 Human 7.5 pEC50 = 7.5 Functional
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 9511 44 None 1698 2 Human 7.5 pEC50 = 7.5 Functional
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 9511 44 None 1698 2 Human 7.5 pEC50 = 7.5 Functional
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 9992 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 9992 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 10103 96 None -69 28 Human 8.3 pIC50 = 8.3 Functional
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 10103 96 None -69 28 Human 8.3 pIC50 = 8.3 Functional
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 10103 96 None -69 28 Human 8.3 pIC50 = 8.3 Functional
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 10103 96 None -69 28 Human 8.3 pIC50 = 8.3 Functional
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 10103 96 None -69 28 Human 8.3 pIC50 = 8.3 Functional
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 Assay information Chemical information
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name		 GPCRdb
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ligand		 Fold
selectivity		 # Tested
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 p-value
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104850 10103 96 None - 6 Human 5.0 pEC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pEC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pEC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pEC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pEC50 = 5 Binding
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 187719 1 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 187719 1 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 8144 22 None - 6 Human 5.3 pEC50 = 5.3 Binding
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 9991 5 None - 6 Human 6.3 pEC50 = 6.3 Binding
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 9991 5 None - 6 Human 6.3 pEC50 = 6.3 Binding
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 9991 5 None - 6 Human 6.3 pEC50 = 6.3 Binding
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 188811 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
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 188811 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
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 7967 25 None - 5 Human 5.2 pEC50 = 5.2 Binding
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 7967 25 None - 5 Human 5.2 pEC50 = 5.2 Binding
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 7967 25 None - 5 Human 5.2 pEC50 = 5.2 Binding
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 7967 25 None - 5 Human 5.2 pEC50 = 5.2 Binding
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 8144 22 None - 6 Human 6.0 pEC50 = 6.0 Binding
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 8144 22 None - 6 Human 6.0 pEC50 = 6.0 Binding
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 8144 22 None - 6 Human 6.0 pEC50 = 6.0 Binding
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 8144 22 None - 6 Human 6.0 pEC50 = 6.0 Binding
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 8144 22 None - 6 Human 6.0 pEC50 = 6.0 Binding
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 116281 1 None - 1 Human 5.0 pIC50 = 5 Binding
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 116281 1 None - 1 Human 5.0 pIC50 = 5 Binding
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 116290 0 None - 3 Human 5.0 pIC50 = 5 Binding
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 116290 0 None - 3 Human 5.0 pIC50 = 5 Binding
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 97346 0 None - 2 Human 5.0 pIC50 = 5 Binding
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 97346 0 None - 2 Human 5.0 pIC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pIC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pIC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pIC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pIC50 = 5 Binding
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 10103 96 None - 6 Human 5.0 pIC50 = 5 Binding
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 97395 0 None - 1 Human 5.0 pIC50 = 5.0 Binding
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 97395 0 None - 1 Human 5.0 pIC50 = 5.0 Binding
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 89812 21 None - 2 Human 4.9 pIC50 = 4.9 Binding
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 89812 21 None - 2 Human 4.9 pIC50 = 4.9 Binding
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 112234 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
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 112234 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
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 116289 0 None - 2 Human 4.9 pIC50 = 4.9 Binding
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 116289 0 None - 2 Human 4.9 pIC50 = 4.9 Binding
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 116009 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
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 116009 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
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 89810 0 None - 2 Human 4.8 pIC50 = 4.8 Binding
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 89810 0 None - 2 Human 4.8 pIC50 = 4.8 Binding
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 116284 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 116284 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 116285 0 None - 3 Human 5.6 pIC50 = 5.6 Binding
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 116285 0 None - 3 Human 5.6 pIC50 = 5.6 Binding
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 116283 21 None - 2 Human 6.6 pIC50 = 6.6 Binding
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 116283 21 None - 2 Human 6.6 pIC50 = 6.6 Binding
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 116294 0 None - 3 Human 5.3 pIC50 = 5.3 Binding
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 116294 0 None - 3 Human 5.3 pIC50 = 5.3 Binding
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 7967 25 None - 5 Human 5.2 pIC50 = 5.2 Binding
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 7967 25 None - 5 Human 5.2 pIC50 = 5.2 Binding
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 7967 25 None - 5 Human 5.2 pIC50 = 5.2 Binding
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 7967 25 None - 5 Human 5.2 pIC50 = 5.2 Binding
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 116286 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 116286 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 116287 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 116287 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 116268 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
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 116268 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
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 116293 0 None - 2 Human 5.2 pIC50 = 5.2 Binding
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 116293 0 None - 2 Human 5.2 pIC50 = 5.2 Binding
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 116282 0 None - 2 Human 5.1 pIC50 = 5.1 Binding
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 116282 0 None - 2 Human 5.1 pIC50 = 5.1 Binding
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 89284 0 None - 2 Human 5.1 pIC50 = 5.1 Binding
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 89284 0 None - 2 Human 5.1 pIC50 = 5.1 Binding
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 9991 5 None - 6 Human 6.0 pIC50 = 6.0 Binding
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 9991 5 None - 6 Human 6.0 pIC50 = 6.0 Binding
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 9991 5 None - 6 Human 6.0 pIC50 = 6.0 Binding
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 24614 0 None - 2 Human 5.0 pIC50 = 5 Binding
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 24614 0 None - 2 Human 5.0 pIC50 = 5 Binding
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