Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
164611580 183954 0 None 2454 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 395 3 1 6 2.1 O=C(NC12CCC(CC1)CC2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4847866 183954 0 None 2454 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 395 3 1 6 2.1 O=C(NC12CCC(CC1)CC2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
164625379 185654 0 None 831 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 391 3 1 6 2.7 O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2cnccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4873473 185654 0 None 831 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 391 3 1 6 2.7 O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2cnccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
138491556 162058 0 None 15 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 383 15 1 2 6.0 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC1CC1 10.1021/acs.jmedchem.8b00243
CHEMBL4169198 162058 0 None 15 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 383 15 1 2 6.0 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC1CC1 10.1021/acs.jmedchem.8b00243
15614389 167451 0 None 2 2 Rat 10.5 pEC50 = 10.5 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(CO)CC21 10.1021/jm970126f
CHEMBL432107 167451 0 None 2 2 Rat 10.5 pEC50 = 10.5 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(CO)CC21 10.1021/jm970126f
156248679 184909 0 None 14454 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 393 3 1 6 2.7 O=C(NC1(C(F)(F)F)CCC1)c1nn(-c2cnccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4862304 184909 0 None 14454 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 393 3 1 6 2.7 O=C(NC1(C(F)(F)F)CCC1)c1nn(-c2cnccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
156248933 185807 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 366 4 0 8 3.2 CCC(C)(C)c1noc(-c2nn(-c3cnccn3)c3c2CC2CCC3O2)n1 10.1021/acsmedchemlett.1c00331
CHEMBL4875720 185807 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 366 4 0 8 3.2 CCC(C)(C)c1noc(-c2nn(-c3cnccn3)c3c2CC2CCC3O2)n1 10.1021/acsmedchemlett.1c00331
164609298 183879 0 None 35481 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 353 3 1 6 1.0 O=C(NC12CC(C1)C2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4846759 183879 0 None 35481 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 353 3 1 6 1.0 O=C(NC12CC(C1)C2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
10500128 9344 0 None 3 2 Rat 10.3 pEC50 = 10.3 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
ChEMBL 382 7 2 3 6.4 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)c1ccc(CO)cc1-2 10.1021/jm970126f
CHEMBL111724 9344 0 None 3 2 Rat 10.3 pEC50 = 10.3 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
ChEMBL 382 7 2 3 6.4 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)c1ccc(CO)cc1-2 10.1021/jm970126f
164621737 185102 0 None 2187 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 384 2 0 8 2.5 CC(C)(C)c1nnc(-c2nn(-c3c[n+]([O-])ccn3)c3c2CC2CCC3O2)s1 10.1021/acsmedchemlett.1c00331
CHEMBL4865162 185102 0 None 2187 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 384 2 0 8 2.5 CC(C)(C)c1nnc(-c2nn(-c3c[n+]([O-])ccn3)c3c2CC2CCC3O2)s1 10.1021/acsmedchemlett.1c00331
138491578 162550 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 401 16 2 3 5.2 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC(C)CO 10.1021/acs.jmedchem.8b00243
CHEMBL4177060 162550 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 401 16 2 3 5.2 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC(C)CO 10.1021/acs.jmedchem.8b00243
164619069 185600 0 None 8 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 425 3 1 4 4.2 O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4872695 185600 0 None 8 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 425 3 1 4 4.2 O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL5091754 213550 0 None 4 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC(C)(CCCCCCC#N)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC[C@@H](CO)C[C@@H]21 10.1021/acs.jmedchem.0c02053
164620714 185502 0 None 4677 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 371 4 2 7 1.6 CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@H]1CC[C@@H]2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4871491 185502 0 None 4677 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 371 4 2 7 1.6 CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@H]1CC[C@@H]2O1 10.1021/acsmedchemlett.1c00331
CHEMBL5081770 212994 0 None 7 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC(C)(CCCCCCN=[N+]=[N-])c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC[C@@H](CO)C[C@@H]21 10.1021/acs.jmedchem.0c02053
104850 3278 93 None 1 6 Human 10.0 pEC50 = 10.0 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1016/j.ejmech.2009.12.018
4150 3278 93 None 1 6 Human 10.0 pEC50 = 10.0 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1016/j.ejmech.2009.12.018
743 3278 93 None 1 6 Human 10.0 pEC50 = 10.0 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1016/j.ejmech.2009.12.018
CHEMBL111 3278 93 None 1 6 Human 10.0 pEC50 = 10.0 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1016/j.ejmech.2009.12.018
DB06155 3278 93 None 1 6 Human 10.0 pEC50 = 10.0 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1016/j.ejmech.2009.12.018
4412255 1160 26 None 7 5 Rat 9.9 pEC50 = 9.9 Functional
cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)C1CC(O)CCC1CCCO)(C)C nan
5570 1160 26 None 7 5 Rat 9.9 pEC50 = 9.9 Functional
cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)C1CC(O)CCC1CCCO)(C)C nan
CHEMBL77520 1160 26 None 7 5 Rat 9.9 pEC50 = 9.9 Functional
cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)C1CC(O)CCC1CCCO)(C)C nan
104895 1161 23 None -22 9 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
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/jm800463f
730 1161 23 None -22 9 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
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/jm800463f
734 1161 23 None -22 9 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
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/jm800463f
CHEMBL559612 1161 23 None -22 9 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
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/jm800463f
10618930 8396 0 None 4 2 Rat 9.7 pEC50 = 9.7 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
ChEMBL 366 6 1 2 7.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)c1ccc(C)cc1-2 10.1021/jm970126f
CHEMBL109393 8396 0 None 4 2 Rat 9.7 pEC50 = 9.7 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
ChEMBL 366 6 1 2 7.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)c1ccc(C)cc1-2 10.1021/jm970126f
138491579 162274 0 None 38 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 401 17 2 3 5.2 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCCO 10.1021/acs.jmedchem.8b00243
CHEMBL4172580 162274 0 None 38 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 401 17 2 3 5.2 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCCO 10.1021/acs.jmedchem.8b00243
104895 1161 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
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/jm800463f
730 1161 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
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/jm800463f
734 1161 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
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/jm800463f
CHEMBL559612 1161 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level
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/jm800463f
104895 1161 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation
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/jm070317a
730 1161 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation
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/jm070317a
734 1161 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation
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/jm070317a
CHEMBL559612 1161 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation
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/jm070317a
118720555 115439 0 None -1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method
ChEMBL 389 5 1 3 4.4 CC(C)(NC(=O)c1nn(Cc2ccc(F)cc2)c2c1C[C@H]1C[C@@H]21)c1ccccc1 10.1016/j.bmcl.2014.11.040
CHEMBL3354941 115439 0 None -1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method
ChEMBL 389 5 1 3 4.4 CC(C)(NC(=O)c1nn(Cc2ccc(F)cc2)c2c1C[C@H]1C[C@@H]21)c1ccccc1 10.1016/j.bmcl.2014.11.040
145971834 164021 0 None - 1 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 357 15 1 1 6.7 CCCCC/C=C\[C@H](C)/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1 10.1021/acs.jmedchem.8b00611
CHEMBL4215369 164021 0 None - 1 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 357 15 1 1 6.7 CCCCC/C=C\[C@H](C)/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1 10.1021/acs.jmedchem.8b00611
24945480 186345 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 426 4 0 3 3.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccccc1 10.1021/jm900063x
CHEMBL490024 186345 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 426 4 0 3 3.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccccc1 10.1021/jm900063x
CHEMBL5071417 212487 0 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC1(C)Oc2cc(C3(CCCCCCC#N)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/acs.jmedchem.0c02053
162664878 181596 0 None 46 2 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assayAntagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assay
ChEMBL 432 5 1 3 5.5 Cc1c(-c2ccccc2)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
CHEMBL4782654 181596 0 None 46 2 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assayAntagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assay
ChEMBL 432 5 1 3 5.5 Cc1c(-c2ccccc2)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
76310146 104067 0 None - 1 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins
ChEMBL 398 5 1 4 5.8 CCCCOC(=O)C1(c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)CCC1 10.1021/jm501165d
CHEMBL3104362 104067 0 None - 1 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins
ChEMBL 398 5 1 4 5.8 CCCCOC(=O)C1(c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)CCC1 10.1021/jm501165d
76310146 104067 0 None - 1 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins
ChEMBL 398 5 1 4 5.8 CCCCOC(=O)C1(c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)CCC1 10.1021/jm4016075
CHEMBL3104362 104067 0 None - 1 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins
ChEMBL 398 5 1 4 5.8 CCCCOC(=O)C1(c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)CCC1 10.1021/jm4016075
145984226 164955 0 None 2 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
ChEMBL 411 5 1 4 6.1 CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCCC(F)(F)F)cc1OC2(C)C 10.1016/j.bmc.2018.08.003
CHEMBL4240671 164955 0 None 2 2 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
ChEMBL 411 5 1 4 6.1 CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCCC(F)(F)F)cc1OC2(C)C 10.1016/j.bmc.2018.08.003
CHEMBL5074603 212549 0 None -1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC1(C)Oc2cc(C3(CCCCCCCN=C=S)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/acs.jmedchem.0c02053
145957967 161604 7 None 52 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 387 16 2 3 4.8 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCO 10.1021/acs.jmedchem.8b00243
CHEMBL4161934 161604 7 None 52 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 387 16 2 3 4.8 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCO 10.1021/acs.jmedchem.8b00243
86274158 192089 13 None 26 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assay
ChEMBL 367 8 1 3 4.8 CC(C)(NC(=O)c1nn(CCCCCF)c2ccccc12)c1ccccc1 10.1021/acs.jmedchem.2c00969
CHEMBL5219235 192089 13 None 26 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assay
ChEMBL 367 8 1 3 4.8 CC(C)(NC(=O)c1nn(CCCCCF)c2ccccc12)c1ccccc1 10.1021/acs.jmedchem.2c00969
104895 1161 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation
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/acs.jmedchem.5b00579
730 1161 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation
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/acs.jmedchem.5b00579
734 1161 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation
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/acs.jmedchem.5b00579
CHEMBL559612 1161 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation
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/acs.jmedchem.5b00579
76324747 104066 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins
ChEMBL 386 5 1 4 5.6 CCCCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21 10.1021/jm501165d
CHEMBL3104360 104066 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins
ChEMBL 386 5 1 4 5.6 CCCCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21 10.1021/jm501165d
76324747 104066 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins
ChEMBL 386 5 1 4 5.6 CCCCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21 10.1021/jm4016075
CHEMBL3104360 104066 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins
ChEMBL 386 5 1 4 5.6 CCCCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21 10.1021/jm4016075
46239964 117120 1 None -12 2 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 396 3 1 5 4.4 CC(C)(C)c1cc(NC(=O)[C@]2(C)CCCN2c2ccc(C(F)(F)F)cn2)no1 10.1016/j.bmcl.2014.12.033
CHEMBL3400946 117120 1 None -12 2 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 396 3 1 5 4.4 CC(C)(C)c1cc(NC(=O)[C@]2(C)CCCN2c2ccc(C(F)(F)F)cn2)no1 10.1016/j.bmcl.2014.12.033
24945636 186198 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 5 0 3 4.5 O=C(CCc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
CHEMBL489031 186198 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 5 0 3 4.5 O=C(CCc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
24944972 186259 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 404 3 0 3 3.4 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
CHEMBL489429 186259 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 404 3 0 3 3.4 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
24945479 188925 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 480 4 0 3 4.1 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
CHEMBL514068 188925 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 480 4 0 3 4.1 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
24945635 189129 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 437 4 0 4 2.9 N#Cc1ccc(CC(=O)N2CCN(S(=O)(=O)c3cc(Cl)cc(Cl)c3)CC2)cc1 10.1021/jm900063x
CHEMBL515641 189129 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 437 4 0 4 2.9 N#Cc1ccc(CC(=O)N2CCN(S(=O)(=O)c3cc(Cl)cc(Cl)c3)CC2)cc1 10.1021/jm900063x
CHEMBL5092703 213608 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC1(C)Oc2cc(C3(CCCCCCN=C=S)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/acs.jmedchem.0c02053
164620733 185505 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 371 4 2 7 1.6 CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@@H]1CC[C@H]2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4871528 185505 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 371 4 2 7 1.6 CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@@H]1CC[C@H]2O1 10.1021/acsmedchemlett.1c00331
145984466 164967 0 None 15 2 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
ChEMBL 357 5 1 4 5.5 CCCCO/N=C(\C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(C)C[C@H]21 10.1016/j.bmc.2018.08.003
CHEMBL4240996 164967 0 None 15 2 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
ChEMBL 357 5 1 4 5.5 CCCCO/N=C(\C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(C)C[C@H]21 10.1016/j.bmc.2018.08.003
44339199 9241 0 None 1 2 Rat 9.2 pEC50 = 9.2 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
ChEMBL 370 6 1 2 7.3 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=CC21 10.1021/jm970126f
CHEMBL111148 9241 0 None 1 2 Rat 9.2 pEC50 = 9.2 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
ChEMBL 370 6 1 2 7.3 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=CC21 10.1021/jm970126f
107778 114715 30 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(CO)C[C@H]21 10.1021/jm0503906
CHEMBL334533 114715 30 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(CO)C[C@H]21 10.1021/jm0503906
145964903 163470 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 375 16 2 2 5.9 CCCCC/C=C\[C@H](C)/C=C\C/C=C\C/C=C\CCCC(=O)N[C@H](C)CO 10.1021/acs.jmedchem.8b00611
CHEMBL4208628 163470 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 375 16 2 2 5.9 CCCCC/C=C\[C@H](C)/C=C\C/C=C\C/C=C\CCCC(=O)N[C@H](C)CO 10.1021/acs.jmedchem.8b00611
24744027 189281 0 None -4 2 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at rat recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level
ChEMBL 520 5 0 3 4.7 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL516900 189281 0 None -4 2 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at rat recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level
ChEMBL 520 5 0 3 4.7 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
3868445 192563 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 386 3 0 3 3.3 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm900063x
CHEMBL523100 192563 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 386 3 0 3 3.3 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm900063x
24944801 192772 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 414 3 0 3 4.0 CC1(C)CN(S(=O)(=O)c2cccc3ccccc23)CCN1C(=O)C1CCCCC1 10.1021/jm900063x
CHEMBL525204 192772 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 414 3 0 3 4.0 CC1(C)CN(S(=O)(=O)c2cccc3ccccc23)CCN1C(=O)C1CCCCC1 10.1021/jm900063x
731 1916 22 None -2 4 Human 9.2 pEC50 = 9.2 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)CO)(C)C)(C)C 10.1021/jm050484f
9821569 1916 22 None -2 4 Human 9.2 pEC50 = 9.2 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)CO)(C)C)(C)C 10.1021/jm050484f
CHEMBL307696 1916 22 None -2 4 Human 9.2 pEC50 = 9.2 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)CO)(C)C)(C)C 10.1021/jm050484f
104895 1161 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2011.08.021
730 1161 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2011.08.021
734 1161 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2011.08.021
CHEMBL559612 1161 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2011.08.021
49855337 15834 0 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay
ChEMBL 395 6 1 2 5.9 CCCCCC1=NN(C(=O)N[C@H]2C[C@H]3CC[C@]2(C)C3(C)C)CC1c1ccccc1 10.1016/j.bmcl.2010.07.056
CHEMBL1223588 15834 0 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay
ChEMBL 395 6 1 2 5.9 CCCCCC1=NN(C(=O)N[C@H]2C[C@H]3CC[C@]2(C)C3(C)C)CC1c1ccccc1 10.1016/j.bmcl.2010.07.056
155907792 189310 2 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 6 2 4 2.5 CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21 10.1039/d1md00242b
CHEMBL5169682 189310 2 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 6 2 4 2.5 CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21 10.1039/d1md00242b
155907792 189310 2 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 6 2 4 2.5 CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21 10.1039/d1md00242b
CHEMBL5169682 189310 2 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 6 2 4 2.5 CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21 10.1039/d1md00242b
104895 1161 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding 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 10.1016/j.ejmech.2012.09.035
730 1161 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding 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 10.1016/j.ejmech.2012.09.035
734 1161 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding 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 10.1016/j.ejmech.2012.09.035
CHEMBL559612 1161 23 None -9 9 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding 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 10.1016/j.ejmech.2012.09.035
145985012 165054 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
ChEMBL 375 6 1 4 5.5 CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCCCF)cc1OC2(C)C 10.1016/j.bmc.2018.08.003
CHEMBL4242964 165054 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
ChEMBL 375 6 1 4 5.5 CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCCCF)cc1OC2(C)C 10.1016/j.bmc.2018.08.003
118733881 118073 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 mins
ChEMBL 453 3 2 5 5.7 CC1(C)Oc2cc([C@]34CC5CC(C[C@@](CN=C=S)(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](O)CC[C@H]21 10.1021/jm501960u
CHEMBL3416128 118073 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 mins
ChEMBL 453 3 2 5 5.7 CC1(C)Oc2cc([C@]34CC5CC(C[C@@](CN=C=S)(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](O)CC[C@H]21 10.1021/jm501960u
162662574 181322 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins
ChEMBL 455 3 2 6 5.1 CC1(C)Oc2cc(C34CC5CC(CC(CN=C=S)(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](O)CC[C@H]21 10.1016/j.bmcl.2021.127882
CHEMBL4779296 181322 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins
ChEMBL 455 3 2 6 5.1 CC1(C)Oc2cc(C34CC5CC(CC(CN=C=S)(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](O)CC[C@H]21 10.1016/j.bmcl.2021.127882
44177373 8363 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 459 4 1 2 6.1 Cc1ccc(C(c2ccc(Cl)cc2Cl)N2CCN(C(=O)NC3CCCCC3)CC2)cc1 10.1016/j.ejmech.2009.12.018
CHEMBL1093735 8363 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 459 4 1 2 6.1 Cc1ccc(C(c2ccc(Cl)cc2Cl)N2CCN(C(=O)NC3CCCCC3)CC2)cc1 10.1016/j.ejmech.2009.12.018
89994983 156298 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins
ChEMBL 397 5 1 5 5.1 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCC#N)cc1OC2(C)C 10.1021/jm501165d
CHEMBL4071389 156298 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins
ChEMBL 397 5 1 5 5.1 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCC#N)cc1OC2(C)C 10.1021/jm501165d
104895 1161 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based 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/acs.jmedchem.8b00243
730 1161 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based 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/acs.jmedchem.8b00243
734 1161 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based 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/acs.jmedchem.8b00243
CHEMBL559612 1161 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based 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/acs.jmedchem.8b00243
162657901 180510 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins
ChEMBL 469 4 2 6 5.3 CC1(C)Oc2cc(C34CC5CC(CC(CN=C=S)(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1016/j.bmcl.2021.127882
CHEMBL4760082 180510 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins
ChEMBL 469 4 2 6 5.3 CC1(C)Oc2cc(C34CC5CC(CC(CN=C=S)(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1016/j.bmcl.2021.127882
162668251 181956 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins
ChEMBL 453 4 2 5 5.5 CC1(C)Oc2cc(C34CC5CC(CC(CN=[N+]=[N-])(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1016/j.bmcl.2021.127882
CHEMBL4787347 181956 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins
ChEMBL 453 4 2 5 5.5 CC1(C)Oc2cc(C34CC5CC(CC(CN=[N+]=[N-])(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1016/j.bmcl.2021.127882
145983146 165339 0 None 56 2 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
ChEMBL 421 6 1 5 5.8 CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCOc3ccccc3)cc1OC2(C)C 10.1016/j.bmc.2018.08.003
CHEMBL4249729 165339 0 None 56 2 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
ChEMBL 421 6 1 5 5.8 CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCOc3ccccc3)cc1OC2(C)C 10.1016/j.bmc.2018.08.003
45101490 195435 0 None 301 2 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
ChEMBL 514 8 2 4 6.3 C[C@H](NC(=O)C(C)(C)Nc1cc(C(F)(F)F)ccn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1 10.1016/j.bmcl.2009.07.046
CHEMBL567679 195435 0 None 301 2 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
ChEMBL 514 8 2 4 6.3 C[C@H](NC(=O)C(C)(C)Nc1cc(C(F)(F)F)ccn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1 10.1016/j.bmcl.2009.07.046
24768473 97413 0 None 2 3 Mouse 9.0 pEC50 = 9 Functional
Activity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formationActivity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formation
ChEMBL 416 4 1 4 5.3 Cc1c(C(=O)NC2CCCCC2)nn(-c2ccc(Cl)c(Cl)c2)c1-n1cccc1 10.1021/jm070566z
CHEMBL272203 97413 0 None 2 3 Mouse 9.0 pEC50 = 9 Functional
Activity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formationActivity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formation
ChEMBL 416 4 1 4 5.3 Cc1c(C(=O)NC2CCCCC2)nn(-c2ccc(Cl)c(Cl)c2)c1-n1cccc1 10.1021/jm070566z
89994988 155532 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 411 6 1 5 5.5 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCCC#N)cc1OC2(C)C 10.1021/jm501165d
CHEMBL4062745 155532 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 411 6 1 5 5.5 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCCC#N)cc1OC2(C)C 10.1021/jm501165d
89994947 155618 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 423 6 1 5 5.7 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C3(C(=O)OCCCCC#N)CCC3)cc1OC2(C)C 10.1021/jm501165d
CHEMBL4063822 155618 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 423 6 1 5 5.7 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C3(C(=O)OCCCCC#N)CCC3)cc1OC2(C)C 10.1021/jm501165d
89994978 156435 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 358 3 1 4 4.8 CCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21 10.1021/jm501165d
CHEMBL4073011 156435 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 358 3 1 4 4.8 CCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21 10.1021/jm501165d
89994961 157832 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 399 6 2 3 5.6 CCCCCNC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21 10.1021/jm501165d
CHEMBL4089791 157832 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 399 6 2 3 5.6 CCCCCNC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21 10.1021/jm501165d
89994985 158639 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 438 6 1 6 5.1 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCn3ccnc3)cc1OC2(C)C 10.1021/jm501165d
CHEMBL4098428 158639 0 None - 1 Rat 9.0 pEC50 = 9 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 438 6 1 6 5.1 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCn3ccnc3)cc1OC2(C)C 10.1021/jm501165d
42625791 180727 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 548 4 0 3 4.8 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL476253 180727 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 548 4 0 3 4.8 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
42625463 180728 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 558 4 0 3 4.6 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Br)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL476254 180728 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 558 4 0 3 4.6 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Br)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
24945235 181920 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 538 5 0 5 3.6 COC(=O)c1cc(C(F)(F)F)cc(S(=O)(=O)N2CCN(C(=O)Cc3ccc(C(F)(F)F)cc3)CC2)c1 10.1021/jm900063x
CHEMBL478696 181920 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 538 5 0 5 3.6 COC(=O)c1cc(C(F)(F)F)cc(S(=O)(=O)N2CCN(C(=O)Cc3ccc(C(F)(F)F)cc3)CC2)c1 10.1021/jm900063x
2729564 186257 6 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 472 3 0 3 4.1 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL489425 186257 6 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 472 3 0 3 4.1 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
24744027 189281 0 None 4 2 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 520 5 0 3 4.7 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL516900 189281 0 None 4 2 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 520 5 0 3 4.7 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
24744027 189281 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level
ChEMBL 520 5 0 3 4.7 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL516900 189281 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level
ChEMBL 520 5 0 3 4.7 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
24944970 192540 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 364 3 0 3 2.7 Cc1cc(C)cc(S(=O)(=O)N2CCN(C(=O)C3CCCCC3)CC2)c1 10.1021/jm900063x
CHEMBL522930 192540 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 364 3 0 3 2.7 Cc1cc(C)cc(S(=O)(=O)N2CCN(C(=O)C3CCCCC3)CC2)c1 10.1021/jm900063x
162665228 181524 0 None 2 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assayAgonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assay
ChEMBL 390 4 1 3 4.5 Cc1c(Cl)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
CHEMBL4781952 181524 0 None 2 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assayAgonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assay
ChEMBL 390 4 1 3 4.5 Cc1c(Cl)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
104895 1161 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP 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/acs.jmedchem.0c02053
730 1161 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP 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/acs.jmedchem.0c02053
734 1161 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP 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/acs.jmedchem.0c02053
CHEMBL559612 1161 23 None -9 9 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP 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/acs.jmedchem.0c02053
10024106 95722 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 403 3 0 3 5.1 O=C(c1cc2c(cc1F)OC(c1ccccc1)(c1ccccc1)O2)N1CCCCC1 10.1021/jm701487t
CHEMBL260625 95722 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 403 3 0 3 5.1 O=C(c1cc2c(cc1F)OC(c1ccccc1)(c1ccccc1)O2)N1CCCCC1 10.1021/jm701487t
156248392 183798 0 None 89 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 361 2 1 4 3.5 CC(C)(C)NC(=O)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4845707 183798 0 None 89 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 361 2 1 4 3.5 CC(C)(C)NC(=O)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
162676369 182762 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)
ChEMBL 396 7 2 3 4.7 CN(C)c1ccc(CCNC(=O)c2[nH]c3ccc(Cl)cc3c2CN=[N+]=[N-])cc1 10.1016/j.ejmech.2016.05.044
CHEMBL4797581 182762 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)
ChEMBL 396 7 2 3 4.7 CN(C)c1ccc(CCNC(=O)c2[nH]c3ccc(Cl)cc3c2CN=[N+]=[N-])cc1 10.1016/j.ejmech.2016.05.044
104895 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release 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 10.1016/j.bmcl.2010.07.056
730 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release 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 10.1016/j.bmcl.2010.07.056
734 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release 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 10.1016/j.bmcl.2010.07.056
CHEMBL559612 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release 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 10.1016/j.bmcl.2010.07.056
71661716 87870 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 mins
ChEMBL 396 2 2 3 5.5 CC1(C)Oc2cc(C34CC5CC(CC(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/jm4000775
CHEMBL2348462 87870 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 mins
ChEMBL 396 2 2 3 5.5 CC1(C)Oc2cc(C34CC5CC(CC(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/jm4000775
42625862 192154 0 None 3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level
ChEMBL 506 4 0 3 4.7 O=C(c1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL522114 192154 0 None 3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level
ChEMBL 506 4 0 3 4.7 O=C(c1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
49781019 17987 0 None 20 2 Rat 8.9 pEC50 = 8.9 Functional
Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingAntagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 1023 26 3 7 15.1 Cc1c(C(=O)NCCCCCCCCCNCCCCCCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1021/jm1006676
CHEMBL1269767 17987 0 None 20 2 Rat 8.9 pEC50 = 8.9 Functional
Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingAntagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 1023 26 3 7 15.1 Cc1c(C(=O)NCCCCCCCCCNCCCCCCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1021/jm1006676
164887460 191543 1 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay
ChEMBL 395 6 1 4 5.9 CC1(C)Oc2cc(C3(CCCCCC#N)CCC3)cc(O)c2[C@@H]2CC(=O)CC[C@H]21 10.1016/j.ejmech.2021.114027
CHEMBL5203712 191543 1 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay
ChEMBL 395 6 1 4 5.9 CC1(C)Oc2cc(C3(CCCCCC#N)CCC3)cc(O)c2[C@@H]2CC(=O)CC[C@H]21 10.1016/j.ejmech.2021.114027
145959588 161796 0 None -1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 434 4 1 3 4.6 Cc1c(Br)cn(Cc2ccc(F)cc2)c(=O)c1C(=O)NC1CCCCCC1 10.1016/j.ejmech.2018.05.019
CHEMBL4164954 161796 0 None -1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 434 4 1 3 4.6 Cc1c(Br)cn(Cc2ccc(F)cc2)c(=O)c1C(=O)NC1CCCCCC1 10.1016/j.ejmech.2018.05.019
104895 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis
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/acs.jmedchem.9b01142
730 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis
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/acs.jmedchem.9b01142
734 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis
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/acs.jmedchem.9b01142
CHEMBL559612 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis
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/acs.jmedchem.9b01142
104895 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding 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 10.1016/j.bmc.2014.07.006
730 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding 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 10.1016/j.bmc.2014.07.006
734 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding 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 10.1016/j.bmc.2014.07.006
CHEMBL559612 1161 23 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding 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 10.1016/j.bmc.2014.07.006
104895 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET 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 10.1016/j.ejmech.2021.114027
730 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET 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 10.1016/j.ejmech.2021.114027
734 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET 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 10.1016/j.ejmech.2021.114027
CHEMBL559612 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET 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 10.1016/j.ejmech.2021.114027
104850 3278 93 None 1 6 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm4010708
4150 3278 93 None 1 6 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm4010708
743 3278 93 None 1 6 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm4010708
CHEMBL111 3278 93 None 1 6 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm4010708
DB06155 3278 93 None 1 6 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm4010708
24945315 186260 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 4 0 3 4.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1 10.1021/jm900063x
CHEMBL489437 186260 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 4 0 3 4.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1 10.1021/jm900063x
104895 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding 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 10.1016/j.ejmech.2021.113354
730 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding 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 10.1016/j.ejmech.2021.113354
734 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding 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 10.1016/j.ejmech.2021.113354
CHEMBL559612 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding 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 10.1016/j.ejmech.2021.113354
162672230 182265 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 351 8 1 5 3.3 CCCCCn1nc(C(=O)N[C@@H](C(=O)OC)C(C)C)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4791449 182265 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 351 8 1 5 3.3 CCCCCn1nc(C(=O)N[C@@H](C(=O)OC)C(C)C)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
118733874 118068 0 None 10 2 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 mins
ChEMBL 455 2 3 5 4.8 COC(=O)N[C@]12CC3CC(C1)C[C@](c1cc(O)c4c(c1)OC(C)(C)[C@@H]1CC[C@@H](O)C[C@@H]41)(C3)C2 10.1021/jm501960u
CHEMBL3416121 118068 0 None 10 2 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 mins
ChEMBL 455 2 3 5 4.8 COC(=O)N[C@]12CC3CC(C1)C[C@](c1cc(O)c4c(c1)OC(C)(C)[C@@H]1CC[C@@H](O)C[C@@H]41)(C3)C2 10.1021/jm501960u
104895 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting 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 10.1016/j.bmc.2020.115513
730 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting 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 10.1016/j.bmc.2020.115513
734 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting 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 10.1016/j.bmc.2020.115513
CHEMBL559612 1161 23 None -9 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting 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 10.1016/j.bmc.2020.115513
155541870 172482 0 None -2 2 Human 8.8 pEC50 = 8.8 Functional
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assay
ChEMBL 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4519310 172482 0 None -2 2 Human 8.8 pEC50 = 8.8 Functional
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assay
ChEMBL 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12 10.1021/acs.jmedchem.9b01142
49781021 17989 0 None 33 2 Rat 8.8 pEC50 = 8.8 Functional
Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingAntagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 925 18 2 7 12.4 Cc1c(C(=O)NCCCCCN(C)CCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1021/jm1006676
CHEMBL1269769 17989 0 None 33 2 Rat 8.8 pEC50 = 8.8 Functional
Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingAntagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 925 18 2 7 12.4 Cc1c(C(=O)NCCCCCN(C)CCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1021/jm1006676
57606063 74218 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 437 6 1 4 3.5 CCN(CC(=O)NC1CC1)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1 10.1016/j.bmcl.2012.04.128
CHEMBL2029727 74218 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 437 6 1 4 3.5 CCN(CC(=O)NC1CC1)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1 10.1016/j.bmcl.2012.04.128
145967019 163897 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 398 17 1 2 6.9 C[C@H](/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1)/C=C\CCCCCN=[N+]=[N-] 10.1021/acs.jmedchem.8b00611
CHEMBL4213900 163897 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 398 17 1 2 6.9 C[C@H](/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1)/C=C\CCCCCN=[N+]=[N-] 10.1021/acs.jmedchem.8b00611
45487312 196130 0 None 26 2 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
ChEMBL 496 8 2 4 6.5 C[C@H](NC(=O)C(C)(C)Nc1cc2ccccc2cn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1 10.1016/j.bmcl.2009.07.046
CHEMBL572097 196130 0 None 26 2 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
ChEMBL 496 8 2 4 6.5 C[C@H](NC(=O)C(C)(C)Nc1cc2ccccc2cn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1 10.1016/j.bmcl.2009.07.046
54580071 62772 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 461 9 1 6 5.2 CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO 10.1016/j.bmcl.2011.02.023
CHEMBL1762814 62772 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 461 9 1 6 5.2 CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO 10.1016/j.bmcl.2011.02.023
CHEMBL1789190 62772 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 461 9 1 6 5.2 CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO 10.1016/j.bmcl.2011.02.023
104895 1161 23 None -9 9 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assayAgonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based 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 10.1016/j.bmc.2021.116035
730 1161 23 None -9 9 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assayAgonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based 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 10.1016/j.bmc.2021.116035
734 1161 23 None -9 9 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assayAgonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based 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 10.1016/j.bmc.2021.116035
CHEMBL559612 1161 23 None -9 9 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assayAgonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based 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 10.1016/j.bmc.2021.116035
121283196 158642 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 383 6 1 5 4.8 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(CC(=O)OCCCCC#N)cc1OC2(C)C 10.1021/jm501165d
CHEMBL4098489 158642 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins
ChEMBL 383 6 1 5 4.8 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(CC(=O)OCCCCC#N)cc1OC2(C)C 10.1021/jm501165d
54752945 64958 34 None -1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 356 6 1 2 6.2 CCCCCn1cc(C(=O)Nc2cccc3ccccc23)c2ccccc21 10.1016/j.ejmech.2011.08.021
CHEMBL1828805 64958 34 None -1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 356 6 1 2 6.2 CCCCCn1cc(C(=O)Nc2cccc3ccccc23)c2ccccc21 10.1016/j.ejmech.2011.08.021
11453673 60707 9 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 8 1 6 5.0 CC(C)N(CCO)Cc1csc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)n1 10.1016/j.bmcl.2011.02.023
CHEMBL1762808 60707 9 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 8 1 6 5.0 CC(C)N(CCO)Cc1csc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)n1 10.1016/j.bmcl.2011.02.023
54582096 62774 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 8 1 6 5.7 CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl 10.1016/j.bmcl.2011.02.023
CHEMBL1762816 62774 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 8 1 6 5.7 CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl 10.1016/j.bmcl.2011.02.023
CHEMBL1789209 62774 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 8 1 6 5.7 CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl 10.1016/j.bmcl.2011.02.023
25195469 109501 0 None -10 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay
ChEMBL 420 4 1 4 3.8 O=C(NC1CCCC1)c1ccc2c(c1)N(S(=O)(=O)c1ccc(F)cc1)CCS2 10.1021/jm4005626
CHEMBL3234688 109501 0 None -10 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay
ChEMBL 420 4 1 4 3.8 O=C(NC1CCCC1)c1ccc2c(c1)N(S(=O)(=O)c1ccc(F)cc1)CCS2 10.1021/jm4005626
11201613 18794 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 407 2 0 4 4.5 O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1 10.1016/j.bmcl.2010.10.061
CHEMBL1287847 18794 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 407 2 0 4 4.5 O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1 10.1016/j.bmcl.2010.10.061
CHEMBL1287876 18794 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 407 2 0 4 4.5 O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1 10.1016/j.bmcl.2010.10.061
11589652 14946 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 411 5 0 4 4.8 CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C 10.1016/j.bmcl.2010.06.067
CHEMBL1209647 14946 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 411 5 0 4 4.8 CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C 10.1016/j.bmcl.2010.06.067
CHEMBL3347358 14946 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 411 5 0 4 4.8 CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C 10.1016/j.bmcl.2010.06.067
3929482 92991 11 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 0 5 3.9 Cc1ccc(C(=O)Oc2cccc3cccnc23)cc1S(=O)(=O)N1CCCCC1 10.1016/j.bmcl.2006.09.049
CHEMBL245876 92991 11 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 0 5 3.9 Cc1ccc(C(=O)Oc2cccc3cccnc23)cc1S(=O)(=O)N1CCCCC1 10.1016/j.bmcl.2006.09.049
5311501 4019 8 None -11 7 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assayAgonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1021/jm901214q
733 4019 8 None -11 7 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assayAgonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1021/jm901214q
CHEMBL188 4019 8 None -11 7 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assayAgonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1021/jm901214q
DB13950 4019 8 None -11 7 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assayAgonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1021/jm901214q
10717065 72315 1 None - 1 Rat 8.0 pEC50 = 8 Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
ChEMBL 420 5 1 2 6.8 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)CCCCBr)cc1OC2(C)C 10.1021/jm0505157
CHEMBL199561 72315 1 None - 1 Rat 8.0 pEC50 = 8 Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
ChEMBL 420 5 1 2 6.8 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)CCCCBr)cc1OC2(C)C 10.1021/jm0505157
44358262 116098 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
ChEMBL 367 5 1 3 6.4 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)CCCCC#N)cc1OC2(C)C 10.1021/jm0505157
CHEMBL336670 116098 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
ChEMBL 367 5 1 3 6.4 CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)CCCCC#N)cc1OC2(C)C 10.1021/jm0505157
118916083 180377 0 None 165 2 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay
ChEMBL 654 11 3 6 7.2 O=C(COc1nc(NCc2cccc(C(F)(F)F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2n1)NCCO 10.1021/acsmedchemlett.0c00495
CHEMBL4758427 180377 0 None 165 2 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay
ChEMBL 654 11 3 6 7.2 O=C(COc1nc(NCc2cccc(C(F)(F)F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2n1)NCCO 10.1021/acsmedchemlett.0c00495
118329970 148672 0 None 83 2 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 619 6 2 6 5.8 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL3943971 148672 0 None 83 2 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 619 6 2 6 5.8 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
155541870 172482 0 None 2 2 Rat 8.0 pEC50 = 8 Functional
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
ChEMBL 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4519310 172482 0 None 2 2 Rat 8.0 pEC50 = 8 Functional
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
ChEMBL 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12 10.1021/acs.jmedchem.9b01142
155532408 171197 0 None 3 2 Rat 8.0 pEC50 = 8 Functional
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
ChEMBL 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4467516 171197 0 None 3 2 Rat 8.0 pEC50 = 8 Functional
Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)
ChEMBL 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
118324097 145099 0 None 5 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 687 6 2 4 7.5 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)cc(Br)c2[nH]1 nan
CHEMBL3915692 145099 0 None 5 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 687 6 2 4 7.5 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)cc(Br)c2[nH]1 nan
118329970 148672 0 None 83 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 619 6 2 6 5.8 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1 nan
CHEMBL3943971 148672 0 None 83 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 619 6 2 6 5.8 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1 nan
118329975 151357 0 None 416 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 587 6 2 3 7.4 O=C(CC(F)(F)F)N1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1 nan
CHEMBL3965825 151357 0 None 416 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 587 6 2 3 7.4 O=C(CC(F)(F)F)N1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1 nan
118329979 153386 0 None - 1 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 522 5 2 2 8.6 O=c1cc(Nc2ccc(F)c(Cl)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
CHEMBL3983340 153386 0 None - 1 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 522 5 2 2 8.6 O=c1cc(Nc2ccc(F)c(Cl)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
104850 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm0503906
4150 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm0503906
743 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm0503906
CHEMBL111 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm0503906
DB06155 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm0503906
104850 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm050484f
4150 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm050484f
743 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm050484f
CHEMBL111 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm050484f
DB06155 3278 93 None 1 6 Human 8.0 pEC50 = 8 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1021/jm050484f
104895 1161 23 None -9 9 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assayInverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding 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/jm801353p
730 1161 23 None -9 9 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assayInverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding 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/jm801353p
734 1161 23 None -9 9 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assayInverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding 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/jm801353p
CHEMBL559612 1161 23 None -9 9 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assayInverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding 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/jm801353p
145970762 164239 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 355 15 1 1 6.1 C#CCNC(=O)CCC/C=C\C/C=C\C/C=C\[C@@H](C)/C=C\CCCCC 10.1021/acs.jmedchem.8b00611
CHEMBL4218304 164239 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 355 15 1 1 6.1 C#CCNC(=O)CCC/C=C\C/C=C\C/C=C\[C@@H](C)/C=C\CCCCC 10.1021/acs.jmedchem.8b00611
118323946 142451 0 None 371 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 555 6 2 5 6.9 O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL3894411 142451 0 None 371 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 555 6 2 5 6.9 O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
118324060 145984 0 None 602 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 610 6 2 5 6.1 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL3922599 145984 0 None 602 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 610 6 2 5 6.1 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
56642428 64948 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 342 6 0 3 5.6 CCCCCn1cc(C(=O)c2cccc3ccccc23)c2ccncc21 10.1016/j.ejmech.2011.08.021
CHEMBL1828632 64948 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 342 6 0 3 5.6 CCCCCn1cc(C(=O)c2cccc3ccccc23)c2ccncc21 10.1016/j.ejmech.2011.08.021
155535617 171500 1 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 8 2 4 2.5 CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21 10.1039/d1md00242b
CHEMBL4472094 171500 1 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 8 2 4 2.5 CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21 10.1039/d1md00242b
52944884 18821 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3CCN4CCCC[C@@H]4C3)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1288054 18821 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3CCN4CCCC[C@@H]4C3)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
52943703 18828 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1288114 18828 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
52944916 18836 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 423 4 0 4 4.9 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4CC3(C)C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1288176 18836 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 423 4 0 4 4.9 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4CC3(C)C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
49862566 14930 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 367 2 0 4 3.5 CN1CCN(C(=O)c2cn3c4c(cccc24)OC[C@H]3C2CCCCC2)CC1 10.1016/j.bmcl.2010.06.067
CHEMBL1209576 14930 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 367 2 0 4 3.5 CN1CCN(C(=O)c2cn3c4c(cccc24)OC[C@H]3C2CCCCC2)CC1 10.1016/j.bmcl.2010.06.067
53326154 57944 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 400 5 0 6 4.4 Clc1cccc2c(-c3noc(CN4CCCC4)n3)cn(CC3CCOCC3)c12 10.1016/j.bmcl.2011.01.082
CHEMBL1682271 57944 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 400 5 0 6 4.4 Clc1cccc2c(-c3noc(CN4CCCC4)n3)cn(CC3CCOCC3)c12 10.1016/j.bmcl.2011.01.082
24863396 15836 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay
ChEMBL 399 6 1 2 5.6 CCCCC1=NN(C(=O)NC(C)(C)c2ccc(F)cc2)CC1c1cccc(F)c1 10.1016/j.bmcl.2010.07.056
CHEMBL1223590 15836 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay
ChEMBL 399 6 1 2 5.6 CCCCC1=NN(C(=O)NC(C)(C)c2ccc(F)cc2)CC1c1cccc(F)c1 10.1016/j.bmcl.2010.07.056
104895 1161 23 None -22 9 Rat 7.0 pEC50 = 7 Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
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/jm0505157
730 1161 23 None -22 9 Rat 7.0 pEC50 = 7 Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
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/jm0505157
734 1161 23 None -22 9 Rat 7.0 pEC50 = 7 Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
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/jm0505157
CHEMBL559612 1161 23 None -22 9 Rat 7.0 pEC50 = 7 Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
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/jm0505157
CHEMBL5092514 213599 0 None - 1 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins in presence of forskolin by HitHunter chemiluminescence based assayPositive allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins in presence of forskolin by HitHunter chemiluminescence based assay
ChEMBL None None None O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccoc2)[nH]c2ccccc12 10.1016/j.bmc.2021.116421
118323987 149713 0 None 2 2 Human 7.0 pEC50 = 7 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 623 7 1 5 7.5 COc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
CHEMBL3952365 149713 0 None 2 2 Human 7.0 pEC50 = 7 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 623 7 1 5 7.5 COc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
162668450 182142 0 None -10 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 295 6 2 4 2.5 CCCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4789723 182142 0 None -10 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 295 6 2 4 2.5 CCCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
70683294 73246 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at CB1 receptorAgonist activity at CB1 receptor
ChEMBL 549 8 2 9 2.5 O=C(NCCO)C1CCN(Cc2nc(-c3cn(CC4CCS(=O)(=O)CC4)c4c(Cl)cccc34)no2)CC1 10.1016/j.bmcl.2012.02.048
CHEMBL2017689 73246 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at CB1 receptorAgonist activity at CB1 receptor
ChEMBL 549 8 2 9 2.5 O=C(NCCO)C1CCN(Cc2nc(-c3cn(CC4CCS(=O)(=O)CC4)c4c(Cl)cccc34)no2)CC1 10.1016/j.bmcl.2012.02.048
71454145 83341 0 None -70 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay
ChEMBL 456 3 1 4 4.9 O=C(Nc1sc2c(c1C(=O)N1CCCCC1)CCOC2)c1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2012.10.087
CHEMBL2205617 83341 0 None -70 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay
ChEMBL 456 3 1 4 4.9 O=C(Nc1sc2c(c1C(=O)N1CCCCC1)CCOC2)c1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2012.10.087
52941290 55014 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1288145 55014 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1618454 55014 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
11510814 188521 0 None 20 2 Human 6.0 pEC50 = 6 Functional
Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity
ChEMBL 454 4 1 5 5.6 Cc1c(C(=O)NN2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1 10.1016/j.bmcl.2009.03.046
CHEMBL510262 188521 0 None 20 2 Human 6.0 pEC50 = 6 Functional
Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity
ChEMBL 454 4 1 5 5.6 Cc1c(C(=O)NN2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1 10.1016/j.bmcl.2009.03.046
118728139 117114 0 None -707 2 Human 6.0 pEC50 = 6 Functional
Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 450 2 1 4 4.1 O=C(Nc1cc(C(F)(F)F)on1)N1CCCN(C(=O)c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2014.12.033
CHEMBL3400938 117114 0 None -707 2 Human 6.0 pEC50 = 6 Functional
Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 450 2 1 4 4.1 O=C(Nc1cc(C(F)(F)F)on1)N1CCCN(C(=O)c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2014.12.033
5282280 54 38 None -331 4 Rat 6.0 pEC50 = 6 Functional
Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay
ChEMBL 378 17 2 4 5.0 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)OC(CO)CO 10.1016/j.bmcl.2006.01.101
729 54 38 None -331 4 Rat 6.0 pEC50 = 6 Functional
Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay
ChEMBL 378 17 2 4 5.0 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)OC(CO)CO 10.1016/j.bmcl.2006.01.101
CHEMBL122972 54 38 None -331 4 Rat 6.0 pEC50 = 6 Functional
Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay
ChEMBL 378 17 2 4 5.0 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)OC(CO)CO 10.1016/j.bmcl.2006.01.101
141463776 161102 0 None -63 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assayAgonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay
ChEMBL 370 7 2 4 4.5 CCCCNc1cc(C(C)C)c(C(=O)NC23CC4CC(CC(C4)C2)C3)nn1 10.1016/j.ejmech.2017.05.060
CHEMBL4130290 161102 0 None -63 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assayAgonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay
ChEMBL 370 7 2 4 4.5 CCCCNc1cc(C(C)C)c(C(=O)NC23CC4CC(CC(C4)C2)C3)nn1 10.1016/j.ejmech.2017.05.060
118722160 115631 0 None -478 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 464 5 2 7 1.7 CC(C)(C)Cc1nc2cc(S(=O)(=O)C3CN(C(N)=O)C3)ccc2n1CC1(O)CCOCC1 10.1016/j.bmcl.2014.11.062
CHEMBL3357387 115631 0 None -478 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 464 5 2 7 1.7 CC(C)(C)Cc1nc2cc(S(=O)(=O)C3CN(C(N)=O)C3)ccc2n1CC1(O)CCOCC1 10.1016/j.bmcl.2014.11.062
45486215 195940 0 None -125 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 433 3 0 4 4.9 O=C(c1cc(-c2cccc(Cl)c2Cl)cnc1N1CCCCCC1)N1CCOCC1 10.1016/j.bmcl.2009.10.041
CHEMBL570683 195940 0 None -125 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 433 3 0 4 4.9 O=C(c1cc(-c2cccc(Cl)c2Cl)cnc1N1CCCCCC1)N1CCOCC1 10.1016/j.bmcl.2009.10.041
45486166 196634 0 None -251 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 320 2 0 2 5.4 Clc1cccc(-c2ccc(N3CCCCCC3)nc2)c1Cl 10.1016/j.bmcl.2009.10.041
CHEMBL576079 196634 0 None -251 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 320 2 0 2 5.4 Clc1cccc(-c2ccc(N3CCCCCC3)nc2)c1Cl 10.1016/j.bmcl.2009.10.041
45375898 196635 0 None -100 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 345 2 0 3 5.3 N#Cc1cc(N2CCCCCC2)ncc1-c1cccc(Cl)c1Cl 10.1016/j.bmcl.2009.10.041
CHEMBL576087 196635 0 None -100 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 345 2 0 3 5.3 N#Cc1cc(N2CCCCCC2)ncc1-c1cccc(Cl)c1Cl 10.1016/j.bmcl.2009.10.041
44475348 195348 0 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry
ChEMBL 384 3 1 5 3.8 Cc1cn(C)c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12 10.1021/jm9009857
CHEMBL567087 195348 0 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry
ChEMBL 384 3 1 5 3.8 Cc1cn(C)c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12 10.1021/jm9009857
11689242 195480 0 None -912 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry
ChEMBL 370 3 2 4 3.7 Cc1c[nH]c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12 10.1021/jm9009857
CHEMBL567911 195480 0 None -912 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry
ChEMBL 370 3 2 4 3.7 Cc1c[nH]c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12 10.1021/jm9009857
44410687 137842 0 None - 1 Rat 5.0 pEC50 = 5 Functional
Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay
ChEMBL 392 17 2 4 5.3 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CC[C@@H](C)C(=O)OC(CO)CO 10.1016/j.bmcl.2006.01.101
CHEMBL377180 137842 0 None - 1 Rat 5.0 pEC50 = 5 Functional
Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay
ChEMBL 392 17 2 4 5.3 CCCCC/C=C\C/C=C\C/C=C\C/C=C\CC[C@@H](C)C(=O)OC(CO)CO 10.1016/j.bmcl.2006.01.101
71105652 150791 0 None -776 2 Human 5.0 pEC50 = 5 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 419 8 1 7 2.9 Cc1nc(C(NC(=O)c2ccc(N3CC(F)(F)C3)c(OCC3CC3)n2)C2CC2)no1 nan
CHEMBL3960990 150791 0 None -776 2 Human 5.0 pEC50 = 5 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 419 8 1 7 2.9 Cc1nc(C(NC(=O)c2ccc(N3CC(F)(F)C3)c(OCC3CC3)n2)C2CC2)no1 nan
162643760 181110 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 315 4 2 4 2.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4776615 181110 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 315 4 2 4 2.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccc2)n1 10.1021/acs.jmedchem.0c01023
162644317 181194 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 361 7 1 3 5.0 CCCCCn1nc(C(=O)NCc2ccc(Cl)cc2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4777738 181194 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 361 7 1 3 5.0 CCCCCn1nc(C(=O)NCc2ccc(Cl)cc2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
162663645 181460 0 None -144 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 333 4 2 4 2.8 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4781040 181460 0 None -144 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 333 4 2 4 2.8 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2)n1 10.1021/acs.jmedchem.0c01023
162664518 181500 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 317 4 2 6 1.5 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncccn2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4781576 181500 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 317 4 2 6 1.5 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncccn2)n1 10.1021/acs.jmedchem.0c01023
162664931 181517 0 None -57 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 351 4 2 4 2.9 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2F)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4781800 181517 0 None -57 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 351 4 2 4 2.9 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2F)n1 10.1021/acs.jmedchem.0c01023
162665007 181539 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 347 6 1 3 5.3 CCCCCn1nc(C(C)(C)C)cc1C(=O)Nc1ccc(Cl)cc1 10.1021/acs.jmedchem.0c01023
CHEMBL4782074 181539 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 347 6 1 3 5.3 CCCCCn1nc(C(C)(C)C)cc1C(=O)Nc1ccc(Cl)cc1 10.1021/acs.jmedchem.0c01023
162666213 181703 0 None -512 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 329 4 2 4 3.0 Cc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01023
CHEMBL4783974 181703 0 None -512 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 329 4 2 4 3.0 Cc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01023
162666580 181752 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 345 5 2 5 2.7 COc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01023
CHEMBL4784418 181752 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 345 5 2 5 2.7 COc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01023
162666392 181802 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 361 7 1 3 5.0 CCCCCn1nc(C(C)(C)C)cc1C(=O)NCc1ccc(Cl)cc1 10.1021/acs.jmedchem.0c01023
CHEMBL4785185 181802 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 361 7 1 3 5.0 CCCCCn1nc(C(C)(C)C)cc1C(=O)NCc1ccc(Cl)cc1 10.1021/acs.jmedchem.0c01023
162665956 181807 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 371 6 1 3 5.1 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c01023
CHEMBL4785295 181807 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 371 6 1 3 5.1 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c01023
162667222 181879 0 None -489 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 349 4 2 4 3.3 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4786352 181879 0 None -489 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 349 4 2 4 3.3 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cc2)n1 10.1021/acs.jmedchem.0c01023
162669636 181984 0 None -549 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 299 6 2 4 2.0 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(CCCF)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4787759 181984 0 None -549 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 299 6 2 4 2.0 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(CCCF)n1 10.1021/acs.jmedchem.0c01023
162623028 182042 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 383 4 2 4 3.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(C(F)(F)F)cc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4788470 182042 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 383 4 2 4 3.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(C(F)(F)F)cc2)n1 10.1021/acs.jmedchem.0c01023
162668533 182063 0 None -33 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 365 8 2 4 3.5 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1-c1ccc(F)cc1F 10.1021/acs.jmedchem.0c01023
CHEMBL4788749 182063 0 None -33 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 365 8 2 4 3.5 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1-c1ccc(F)cc1F 10.1021/acs.jmedchem.0c01023
162668965 182198 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 335 8 2 4 3.6 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CCCCC1 10.1021/acs.jmedchem.0c01023
CHEMBL4790368 182198 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 335 8 2 4 3.6 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CCCCC1 10.1021/acs.jmedchem.0c01023
162671037 182220 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 316 4 2 5 2.1 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2cccnc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4790704 182220 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 316 4 2 5 2.1 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2cccnc2)n1 10.1021/acs.jmedchem.0c01023
162671764 182240 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 387 6 2 4 4.2 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(O)(C3)C1)C2 10.1021/acs.jmedchem.0c01023
CHEMBL4791040 182240 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 387 6 2 4 4.2 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(O)(C3)C1)C2 10.1021/acs.jmedchem.0c01023
162671765 182248 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 293 8 2 4 2.5 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CC1 10.1021/acs.jmedchem.0c01023
CHEMBL4791212 182248 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 293 8 2 4 2.5 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CC1 10.1021/acs.jmedchem.0c01023
162671780 182258 0 None -13 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 350 4 2 5 2.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cn2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4791388 182258 0 None -13 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 350 4 2 5 2.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cn2)n1 10.1021/acs.jmedchem.0c01023
141747275 182311 0 None -331 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 293 5 1 3 3.9 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4792134 182311 0 None -331 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 293 5 1 3 3.9 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)C 10.1021/acs.jmedchem.0c01023
162671856 182390 0 None -316 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 309 7 2 4 2.9 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)CO 10.1021/acs.jmedchem.0c01023
CHEMBL4793164 182390 0 None -316 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 309 7 2 4 2.9 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)CO 10.1021/acs.jmedchem.0c01023
162672350 182456 0 None -741 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 334 4 2 5 2.2 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cn2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4793976 182456 0 None -741 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 334 4 2 5 2.2 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cn2)n1 10.1021/acs.jmedchem.0c01023
162673695 182590 0 None -42 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 347 6 1 3 5.3 CCCCCn1nc(C(=O)Nc2ccc(Cl)cc2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4795529 182590 0 None -42 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 347 6 1 3 5.3 CCCCCn1nc(C(=O)Nc2ccc(Cl)cc2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
162623029 182604 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 399 5 2 5 3.6 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(OC(F)(F)F)cc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4795667 182604 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 399 5 2 5 3.6 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(OC(F)(F)F)cc2)n1 10.1021/acs.jmedchem.0c01023
162675834 182683 0 None -25 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 316 4 2 5 2.1 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccn2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4796542 182683 0 None -25 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 316 4 2 5 2.1 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccn2)n1 10.1021/acs.jmedchem.0c01023
162676075 182718 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 418 4 2 5 3.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncc(C(F)(F)F)cc2Cl)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4797039 182718 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 418 4 2 5 3.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncc(C(F)(F)F)cc2Cl)n1 10.1021/acs.jmedchem.0c01023
162676388 182797 0 None -478 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 281 5 2 4 2.1 CCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4797941 182797 0 None -478 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 281 5 2 4 2.1 CCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
162675814 182865 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 297 6 2 5 1.3 COCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4798902 182865 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 297 6 2 5 1.3 COCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
57606070 74228 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 455 7 2 5 2.7 CNC(=O)CC[C@@H](CO)N(C)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1 10.1016/j.bmcl.2012.04.128
CHEMBL2029737 74228 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 455 7 2 5 2.7 CNC(=O)CC[C@@H](CO)N(C)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1 10.1016/j.bmcl.2012.04.128
155535617 171500 1 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 8 2 4 2.5 CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21 10.1039/d1md00242b
CHEMBL4472094 171500 1 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 8 2 4 2.5 CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21 10.1039/d1md00242b
60155823 76643 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 340 5 2 1 4.7 CCc1c(C(=O)NCCc2ccc(C)cc2)[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.5b00579
CHEMBL2071064 76643 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 340 5 2 1 4.7 CCc1c(C(=O)NCCc2ccc(C)cc2)[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.5b00579
164624856 184956 0 None -5 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 337 7 0 4 4.5 CCCCCc1cc(OC)c2cc(Cc3ccccn3)c(=O)oc2c1 10.1016/j.ejmech.2021.113354
CHEMBL4862930 184956 0 None -5 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 337 7 0 4 4.5 CCCCCc1cc(OC)c2cc(Cc3ccccn3)c(=O)oc2c1 10.1016/j.ejmech.2021.113354
67953300 115193 0 None -1288 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins
ChEMBL 291 4 1 4 2.8 CC(C)(C)c1cc(NC(=O)[C@@H]2CCCN2CC2CC2)no1 10.1016/j.bmcl.2014.12.019
CHEMBL3353867 115193 0 None -1288 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins
ChEMBL 291 4 1 4 2.8 CC(C)(C)c1cc(NC(=O)[C@@H]2CCCN2CC2CC2)no1 10.1016/j.bmcl.2014.12.019
118324104 149893 0 None - 1 Human 6.0 pEC50 = 6 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 572 10 3 4 8.0 O=C(O)CCCOc1ccc(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)cc1 nan
CHEMBL3953885 149893 0 None - 1 Human 6.0 pEC50 = 6 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 572 10 3 4 8.0 O=C(O)CCCOc1ccc(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)cc1 nan
118323970 146910 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 722 12 2 6 7.7 CC(=O)NCCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
CHEMBL3930097 146910 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 722 12 2 6 7.7 CC(=O)NCCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
71087679 159431 0 None -25 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 389 7 2 5 2.4 CNC(=O)[C@@H](NC(=O)c1ccc(C2CC2)c(OCC2CCCO2)n1)C(C)(C)C nan
CHEMBL4107610 159431 0 None -25 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 389 7 2 5 2.4 CNC(=O)[C@@H](NC(=O)c1ccc(C2CC2)c(OCC2CCCO2)n1)C(C)(C)C nan
57403187 70297 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 427 5 0 3 5.3 C=CCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2011.12.124
CHEMBL1950331 70297 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 427 5 0 3 5.3 C=CCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2011.12.124
11856745 70306 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 423 4 0 4 4.5 CCCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCOCC1)CC2 10.1016/j.bmcl.2011.12.124
CHEMBL1950341 70306 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 423 4 0 4 4.5 CCCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCOCC1)CC2 10.1016/j.bmcl.2011.12.124
118324125 143686 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 605 8 2 5 7.6 CC(C)(C)OC(=O)CCN1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1 nan
CHEMBL3904458 143686 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 605 8 2 5 7.6 CC(C)(C)OC(=O)CCN1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1 nan
162677250 182949 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 319 6 1 3 4.4 CCCCCn1nc(C(=O)NC2CCCCC2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4799912 182949 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 319 6 1 3 4.4 CCCCCn1nc(C(=O)NC2CCCCC2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
10141893 373 48 None -72 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 503 5 0 5 4.9 CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O 10.1016/j.bmcl.2014.11.003
3316 373 48 None -72 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 503 5 0 5 4.9 CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O 10.1016/j.bmcl.2014.11.003
CHEMBL408430 373 48 None -72 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 503 5 0 5 4.9 CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O 10.1016/j.bmcl.2014.11.003
72948611 172345 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1R expressed in CHO cells by Ca2+ flux assayAgonist activity at human CB1R expressed in CHO cells by Ca2+ flux assay
ChEMBL 359 6 0 2 6.4 CCCCCn1cc(C(=O)c2cccc3ccccc23)c2cccc(F)c21 10.1021/acs.jmedchem.6b00516
CHEMBL4516360 172345 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1R expressed in CHO cells by Ca2+ flux assayAgonist activity at human CB1R expressed in CHO cells by Ca2+ flux assay
ChEMBL 359 6 0 2 6.4 CCCCCn1cc(C(=O)c2cccc3ccccc23)c2cccc(F)c21 10.1021/acs.jmedchem.6b00516
168297756 191898 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assayAgonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay
ChEMBL 364 8 2 4 2.7 CCCCn1cc(C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c2cccnc21 10.1039/d1md00242b
CHEMBL5209051 191898 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assayAgonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay
ChEMBL 364 8 2 4 2.7 CCCCn1cc(C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c2cccnc21 10.1039/d1md00242b
118720565 115452 0 None -87 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method
ChEMBL 359 4 2 4 2.5 O=C(NC1(CO)CCC1)c1nn(-c2ccc(F)cc2F)c2c1C[C@H]1C[C@@H]21 10.1016/j.bmcl.2014.11.040
CHEMBL3354954 115452 0 None -87 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method
ChEMBL 359 4 2 4 2.5 O=C(NC1(CO)CCC1)c1nn(-c2ccc(F)cc2F)c2c1C[C@H]1C[C@@H]21 10.1016/j.bmcl.2014.11.040
11524275 84619 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 404 4 2 1 6.6 O=C(Nc1ccc(Cl)cc1)NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm0503906
CHEMBL224113 84619 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 404 4 2 1 6.6 O=C(Nc1ccc(Cl)cc1)NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm0503906
53324282 56767 0 None -104 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 351 4 1 2 5.4 Clc1cccc(-c2c[nH]c(-c3cccc(CN4CCCCC4)c3)n2)c1 10.1016/j.bmcl.2010.11.044
CHEMBL1644739 56767 0 None -104 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 351 4 1 2 5.4 Clc1cccc(-c2c[nH]c(-c3cccc(CN4CCCCC4)c3)n2)c1 10.1016/j.bmcl.2010.11.044
44828492 2918 72 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 409 6 2 2 5.3 CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1 10.1021/acs.jmedchem.5b00579
7851 2918 72 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 409 6 2 2 5.3 CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1 10.1021/acs.jmedchem.5b00579
CHEMBL1553629 2918 72 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 409 6 2 2 5.3 CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1 10.1021/acs.jmedchem.5b00579
71093593 142319 0 None -12 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 356 7 1 6 3.1 Cc1nc(C(C)(C)NC(=O)c2ccc(C3CC3)c(OCC3CC3)n2)no1 nan
CHEMBL3893213 142319 0 None -12 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 356 7 1 6 3.1 Cc1nc(C(C)(C)NC(=O)c2ccc(C3CC3)c(OCC3CC3)n2)no1 nan
118323971 145127 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 709 12 2 6 8.1 O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 10.1021/acs.jmedchem.8b01467
CHEMBL3915918 145127 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 709 12 2 6 8.1 O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 10.1021/acs.jmedchem.8b01467
118323971 145127 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 709 12 2 6 8.1 O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
CHEMBL3915918 145127 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 709 12 2 6 8.1 O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
22475020 95557 15 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 491 3 0 4 5.4 O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1 10.1021/jm701487t
CHEMBL259656 95557 15 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 491 3 0 4 5.4 O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1 10.1021/jm701487t
22475055 158996 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 513 4 0 5 4.1 O=S(=O)(c1cc2c(cc1F)OC(c1ccc(F)cc1F)(c1ccc(F)cc1F)O2)N1CCOCC1 10.1021/jm701487t
CHEMBL410247 158996 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 513 4 0 5 4.1 O=S(=O)(c1cc2c(cc1F)OC(c1ccc(F)cc1F)(c1ccc(F)cc1F)O2)N1CCOCC1 10.1021/jm701487t
11853844 70315 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 457 4 0 5 4.0 CCS(=O)(=O)n1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCCC1)CC2 10.1016/j.bmcl.2011.12.124
CHEMBL1950350 70315 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 457 4 0 5 4.0 CCS(=O)(=O)n1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCCC1)CC2 10.1016/j.bmcl.2011.12.124
16078 1335 19 None -3 7 Rat 8.0 pEC50 = 8.0 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
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/jm970126f
2424 1335 19 None -3 7 Rat 8.0 pEC50 = 8.0 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
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/jm970126f
4109 1335 19 None -3 7 Rat 8.0 pEC50 = 8.0 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
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/jm970126f
CHEMBL465 1335 19 None -3 7 Rat 8.0 pEC50 = 8.0 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
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/jm970126f
DB00470 1335 19 None -3 7 Rat 8.0 pEC50 = 8.0 Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
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/jm970126f
134146936 149593 0 None 177 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor transfected in HEK293 cells assessed as increase of forskolin-induced cAMP production incubated for 30 mins followed by d2 labeled cAMP addition measured after 60 mins by HTRF assayInverse agonist activity at human CB1 receptor transfected in HEK293 cells assessed as increase of forskolin-induced cAMP production incubated for 30 mins followed by d2 labeled cAMP addition measured after 60 mins by HTRF assay
ChEMBL 619 8 2 7 5.4 COc1ccc(/C=C2\CN(C(=O)CC(=O)O)Cc3c(C(=O)N[C@H](C)c4ccccn4)nn(-c4ccc(Cl)cc4Cl)c32)cc1 10.1016/j.bmcl.2016.09.026
CHEMBL3951226 149593 0 None 177 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor transfected in HEK293 cells assessed as increase of forskolin-induced cAMP production incubated for 30 mins followed by d2 labeled cAMP addition measured after 60 mins by HTRF assayInverse agonist activity at human CB1 receptor transfected in HEK293 cells assessed as increase of forskolin-induced cAMP production incubated for 30 mins followed by d2 labeled cAMP addition measured after 60 mins by HTRF assay
ChEMBL 619 8 2 7 5.4 COc1ccc(/C=C2\CN(C(=O)CC(=O)O)Cc3c(C(=O)N[C@H](C)c4ccccn4)nn(-c4ccc(Cl)cc4Cl)c32)cc1 10.1016/j.bmcl.2016.09.026
134155808 150956 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human cannabinoid receptor 1 expressed in HEK293 cells assessed as increase in forskolin-induced cAMP production preincubated with cells followed by forskolin stimulation measured after 30 mins in presence of D2-labeled cAMP and Eu3+-TBP-NHS cryptate by HTRF assayInverse agonist activity at human cannabinoid receptor 1 expressed in HEK293 cells assessed as increase in forskolin-induced cAMP production preincubated with cells followed by forskolin stimulation measured after 30 mins in presence of D2-labeled cAMP and Eu3+-TBP-NHS cryptate by HTRF assay
ChEMBL 588 5 1 5 8.0 O=C(NC1(c2ccccn2)CC1)c1nn(-c2ccc(C(F)(F)F)cc2Cl)c2c1CCC/C2=C\c1ccc(Cl)s1 10.1016/j.bmcl.2016.09.025
CHEMBL3962373 150956 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human cannabinoid receptor 1 expressed in HEK293 cells assessed as increase in forskolin-induced cAMP production preincubated with cells followed by forskolin stimulation measured after 30 mins in presence of D2-labeled cAMP and Eu3+-TBP-NHS cryptate by HTRF assayInverse agonist activity at human cannabinoid receptor 1 expressed in HEK293 cells assessed as increase in forskolin-induced cAMP production preincubated with cells followed by forskolin stimulation measured after 30 mins in presence of D2-labeled cAMP and Eu3+-TBP-NHS cryptate by HTRF assay
ChEMBL 588 5 1 5 8.0 O=C(NC1(c2ccccn2)CC1)c1nn(-c2ccc(C(F)(F)F)cc2Cl)c2c1CCC/C2=C\c1ccc(Cl)s1 10.1016/j.bmcl.2016.09.025
24945315 186260 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 4 0 3 4.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1 10.1021/jm900063x
CHEMBL489437 186260 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 4 0 3 4.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1 10.1021/jm900063x
118323946 142451 0 None 371 2 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 555 6 2 5 6.9 O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
CHEMBL3894411 142451 0 None 371 2 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 555 6 2 5 6.9 O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
118329983 143221 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 522 5 2 2 8.6 O=c1cc(Nc2ccc(Cl)c(F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
CHEMBL3900808 143221 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 522 5 2 2 8.6 O=c1cc(Nc2ccc(Cl)c(F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
118324060 145984 0 None 602 2 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 610 6 2 5 6.1 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1 nan
CHEMBL3922599 145984 0 None 602 2 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 610 6 2 5 6.1 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1 nan
11951302 104365 0 None 3981 2 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
ChEMBL 404 7 2 5 3.5 COCCOc1ncc(C(=O)N[C@@H]2CCCC[C@H]2O)cc1-c1ccc(Cl)cc1 10.1021/jm4010708
CHEMBL3109772 104365 0 None 3981 2 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
ChEMBL 404 7 2 5 3.5 COCCOc1ncc(C(=O)N[C@@H]2CCCC[C@H]2O)cc1-c1ccc(Cl)cc1 10.1021/jm4010708
67953431 115211 0 None -575 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins
ChEMBL 396 3 1 5 3.5 CC(C)(C)c1cc(NC(=O)[C@@H]2CCC(=O)N2c2ccc(C(F)(F)F)cn2)on1 10.1016/j.bmcl.2014.12.019
CHEMBL3353885 115211 0 None -575 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins
ChEMBL 396 3 1 5 3.5 CC(C)(C)c1cc(NC(=O)[C@@H]2CCC(=O)N2c2ccc(C(F)(F)F)cn2)on1 10.1016/j.bmcl.2014.12.019
155553407 173556 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay
ChEMBL 360 5 1 2 5.4 O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4546004 173556 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay
ChEMBL 360 5 1 2 5.4 O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
76284483 149562 0 None -77 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated as follows: FRET=T730-Alexa730-P(T645-B645) with P=Ru730-B730/Ru645-B645, where T730 is the test well measured at 730 nM, T645 is the test well measured at 645 nm, B730 and B645 are the buffer controls at 730 nm and 645 nm, respectively. cAMP content is determined from the function of a standard curve spanning from 10 μM to 0.13 nM cAMP.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated as follows: FRET=T730-Alexa730-P(T645-B645) with P=Ru730-B730/Ru645-B645, where T730 is the test well measured at 730 nM, T645 is the test well measured at 645 nm, B730 and B645 are the buffer controls at 730 nm and 645 nm, respectively. cAMP content is determined from the function of a standard curve spanning from 10 μM to 0.13 nM cAMP.
ChEMBL 475 7 1 7 3.6 Cc1nc(C(C)(NC(=O)c2cc(O[C@@H](C)C(F)(F)F)c(N3CC(F)(F)C3)cn2)C2CC2)no1 nan
CHEMBL3950922 149562 0 None -77 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated as follows: FRET=T730-Alexa730-P(T645-B645) with P=Ru730-B730/Ru645-B645, where T730 is the test well measured at 730 nM, T645 is the test well measured at 645 nm, B730 and B645 are the buffer controls at 730 nm and 645 nm, respectively. cAMP content is determined from the function of a standard curve spanning from 10 μM to 0.13 nM cAMP.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated as follows: FRET=T730-Alexa730-P(T645-B645) with P=Ru730-B730/Ru645-B645, where T730 is the test well measured at 730 nM, T645 is the test well measured at 645 nm, B730 and B645 are the buffer controls at 730 nm and 645 nm, respectively. cAMP content is determined from the function of a standard curve spanning from 10 μM to 0.13 nM cAMP.
ChEMBL 475 7 1 7 3.6 Cc1nc(C(C)(NC(=O)c2cc(O[C@@H](C)C(F)(F)F)c(N3CC(F)(F)C3)cn2)C2CC2)no1 nan
67953920 115212 0 None -912 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins
ChEMBL 353 3 1 6 2.4 CC(C)(C)c1cc(NC(=O)[C@@H]2CCC(=O)N2c2ccc(C#N)cn2)on1 10.1016/j.bmcl.2014.12.019
CHEMBL3353886 115212 0 None -912 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins
ChEMBL 353 3 1 6 2.4 CC(C)(C)c1cc(NC(=O)[C@@H]2CCC(=O)N2c2ccc(C#N)cn2)on1 10.1016/j.bmcl.2014.12.019
123627357 162394 0 None -912 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in HEK293 cells assessed as increase in beta arrestin recruitment measured after 2 to 3 hrs by PathHunter assayAgonist activity at recombinant human CB1 receptor expressed in HEK293 cells assessed as increase in beta arrestin recruitment measured after 2 to 3 hrs by PathHunter assay
ChEMBL 359 4 1 5 1.7 CC(C)(C)[C@@H](CF)NC(=O)c1nn(-c2c[n+]([O-])ccn2)c2c1C[C@@H]1C[C@H]21 10.1021/acsmedchemlett.7b00396
CHEMBL4174510 162394 0 None -912 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in HEK293 cells assessed as increase in beta arrestin recruitment measured after 2 to 3 hrs by PathHunter assayAgonist activity at recombinant human CB1 receptor expressed in HEK293 cells assessed as increase in beta arrestin recruitment measured after 2 to 3 hrs by PathHunter assay
ChEMBL 359 4 1 5 1.7 CC(C)(C)[C@@H](CF)NC(=O)c1nn(-c2c[n+]([O-])ccn2)c2c1C[C@@H]1C[C@H]21 10.1021/acsmedchemlett.7b00396
11591162 176342 0 None 18 2 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity
ChEMBL 482 4 1 5 6.4 Cc1c(C(=O)NN2CCCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1 10.1016/j.bmcl.2009.03.046
CHEMBL461862 176342 0 None 18 2 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity
ChEMBL 482 4 1 5 6.4 Cc1c(C(=O)NN2CCCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1 10.1016/j.bmcl.2009.03.046
4346308 193486 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayInverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay
ChEMBL 453 5 0 3 5.4 Cc1ccc(C2c3cccn3-c3ccccc3N2C(=O)CN(C(=O)C2CCCC2)C2CC2)cc1 10.1016/j.bmcl.2009.05.114
CHEMBL550309 193486 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayInverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay
ChEMBL 453 5 0 3 5.4 Cc1ccc(C2c3cccn3-c3ccccc3N2C(=O)CN(C(=O)C2CCCC2)C2CC2)cc1 10.1016/j.bmcl.2009.05.114
5031403 193513 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayInverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay
ChEMBL 461 5 0 3 5.7 CC(C)N(CC(=O)N1c2ccccc2-n2cccc2C1c1ccc(F)cc1)C(=O)CC(C)(C)C 10.1016/j.bmcl.2009.05.114
CHEMBL550514 193513 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayInverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay
ChEMBL 461 5 0 3 5.7 CC(C)N(CC(=O)N1c2ccccc2-n2cccc2C1c1ccc(F)cc1)C(=O)CC(C)(C)C 10.1016/j.bmcl.2009.05.114
118323979 147389 0 None 6 2 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 607 7 2 4 6.4 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(Cc3ccc(F)cc3)c3ccc(Cl)cc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL3933648 147389 0 None 6 2 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 607 7 2 4 6.4 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(Cc3ccc(F)cc3)c3ccc(Cl)cc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
155544651 172770 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay
ChEMBL 343 5 1 3 4.6 O=[N+]([O-])CC(c1ccccc1)c1c(-c2cccnc2)[nH]c2ccccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4526885 172770 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay
ChEMBL 343 5 1 3 4.6 O=[N+]([O-])CC(c1ccccc1)c1c(-c2cccnc2)[nH]c2ccccc12 10.1021/acs.jmedchem.9b01142
155561427 175071 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay
ChEMBL 343 5 1 3 4.6 O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2ncccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4581106 175071 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay
ChEMBL 343 5 1 3 4.6 O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2ncccc12 10.1021/acs.jmedchem.9b01142
118323979 147389 0 None 6 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 607 7 2 4 6.4 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(Cc3ccc(F)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
CHEMBL3933648 147389 0 None 6 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 607 7 2 4 6.4 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(Cc3ccc(F)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
71105569 149730 0 None -10 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 391 4 1 4 5.2 CC(C)(NC(=O)c1ccc(Cl)c(-c2cccc(Cl)c2)n1)c1nccs1 nan
CHEMBL3952505 149730 0 None -10 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 391 4 1 4 5.2 CC(C)(NC(=O)c1ccc(Cl)c(-c2cccc(Cl)c2)n1)c1nccs1 nan
118329984 149286 0 None 33 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 544 5 2 2 8.5 O=c1cc(NC2CCC(C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
CHEMBL3948754 149286 0 None 33 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 544 5 2 2 8.5 O=c1cc(NC2CCC(C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
11690547 140162 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 430 3 0 2 6.4 O=C1C(c2ccc(Cl)cc2)N(c2ccc(Cl)cc2)C(=O)N1c1ccc(Cl)cc1 10.1021/jm050484f
CHEMBL381560 140162 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay
ChEMBL 430 3 0 2 6.4 O=C1C(c2ccc(Cl)cc2)N(c2ccc(Cl)cc2)C(=O)N1c1ccc(Cl)cc1 10.1021/jm050484f
5311501 4019 8 None -8 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1016/j.bmcl.2012.04.128
733 4019 8 None -8 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1016/j.bmcl.2012.04.128
CHEMBL188 4019 8 None -8 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1016/j.bmcl.2012.04.128
DB13950 4019 8 None -8 7 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1016/j.bmcl.2012.04.128
164617205 183959 0 None -251 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 342 6 1 3 5.8 CCCCC1(c2cc(O)c3cc(CCC)c(=O)oc3c2)CCCCC1 10.1016/j.ejmech.2021.113354
CHEMBL4847976 183959 0 None -251 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 342 6 1 3 5.8 CCCCC1(c2cc(O)c3cc(CCC)c(=O)oc3c2)CCCCC1 10.1016/j.ejmech.2021.113354
117923246 137133 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assayNegative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assay
ChEMBL 450 8 2 3 5.6 [N-]=[N+]=NCCc1c(C(=O)NCCc2ccc(N3CCCCC3)cc2)[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.5b01303
CHEMBL3758424 137133 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assayNegative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assay
ChEMBL 450 8 2 3 5.6 [N-]=[N+]=NCCc1c(C(=O)NCCc2ccc(N3CCCCC3)cc2)[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.5b01303
118324039 142320 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 738 12 3 7 7.5 CCOC(=O)CCCNc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)cc(=O)[nH]c12 nan
CHEMBL3893217 142320 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 738 12 3 7 7.5 CCOC(=O)CCCNc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)cc(=O)[nH]c12 nan
71450465 83235 0 None -23 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay
ChEMBL 398 3 1 3 4.9 CC(C)(C)CC(=O)Nc1sc2c(c1C(=O)N1CCC(F)(F)CC1)CCCC2 10.1016/j.bmcl.2012.10.087
CHEMBL2204905 83235 0 None -23 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay
ChEMBL 398 3 1 3 4.9 CC(C)(C)CC(=O)Nc1sc2c(c1C(=O)N1CCC(F)(F)CC1)CCCC2 10.1016/j.bmcl.2012.10.087
145982249 166160 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 509 6 1 4 6.5 O=c1cc(Cc2ccc(OC(F)(F)F)cc2)c2cc(C(c3ccc(Cl)cc3)n3ccnc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL4282821 166160 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 509 6 1 4 6.5 O=c1cc(Cc2ccc(OC(F)(F)F)cc2)c2cc(C(c3ccc(Cl)cc3)n3ccnc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
118324113 144568 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 667 8 3 6 7.0 O=C(O)c1ccc(S(=O)(=O)N2CCC(Nc3cc(=O)[nH]c4ccc(C(c5ccc(Cl)cc5)c5ccc(Cl)cc5)cc34)CC2)s1 nan
CHEMBL3911735 144568 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 667 8 3 6 7.0 O=C(O)c1ccc(S(=O)(=O)N2CCC(Nc3cc(=O)[nH]c4ccc(C(c5ccc(Cl)cc5)c5ccc(Cl)cc5)cc34)CC2)s1 nan
71105611 148180 0 None -1412 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 396 9 2 5 2.0 CC(C)C[C@H](NC(=O)c1ccc(N2CC(F)(F)C2)c(OCC2CC2)n1)C(N)=O nan
CHEMBL3940084 148180 0 None -1412 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 396 9 2 5 2.0 CC(C)C[C@H](NC(=O)c1ccc(N2CC(F)(F)C2)c(OCC2CC2)n1)C(N)=O nan
60155819 76640 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay
ChEMBL 371 6 2 3 4.3 CCc1c(C(=O)NCCc2ccc([N+](=O)[O-])cc2)[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.5b00579
CHEMBL2071060 76640 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay
ChEMBL 371 6 2 3 4.3 CCc1c(C(=O)NCCc2ccc([N+](=O)[O-])cc2)[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.5b00579
71525480 143853 0 None -12 2 Human 5.9 pEC50 = 5.9 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively.
ChEMBL 397 5 1 6 4.0 Cc1nc(C(C)(C)NC(=O)c2cnc(C3CC3)c(-c3cccc(Cl)c3)n2)no1 nan
CHEMBL3905931 143853 0 None -12 2 Human 5.9 pEC50 = 5.9 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was ex